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Romidepsin (FK228) HDAC Inhibiteur

Réf. CatalogueS3020

Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176) est un inhibiteur puissant de HDAC1 et HDAC2 avec des IC50 de 36 nM et 47 nM dans des essais sans cellules, respectivement. Ce composé contrôle la croissance et induit l'apoptose dans les cellules tumorales de neuroblastome.
Romidepsin (FK228) HDAC Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 540.7

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.95%
99.95

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires Type d'essai Concentration Temps d'incubation Formulation Description de l'activité PMID
SU-DHL4 Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner  25790907
U2932  Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner  25790907
OCI-LY7 Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner  25790907
Farage Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner  25790907
LY7/EBV Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner  25790907
U2932/EBV Cell Viability Assay 2.5-15 nM 72 h induces cytotoxicity in a concentration-dependent manner  25790907
HCT116 Growth Inhibition Assay 5-5000 nM 24 h DMSO induces cell death in a concentration-dependent manner 25492515
ACH-2 Function Assay 1-9 nM 24 h induces HIV-1 Env expression 25149467
MCF-10A Growth Inhibition Assay IC50=0.17±0.01 nM 24954856
MCF-7 Growth Inhibition Assay IC50=1.10±0.20 nM 24954856
SK-BR-3 Growth Inhibition Assay IC50=1.00±0.35 nM 24954856
MDA-MB-231 Growth Inhibition Assay IC50=0.68±0.14 nM 24954856
PC3 Growth Inhibition Assay IC50=1.65±0.35 nM 24954856
HCT116 Growth Inhibition Assay IC50=1.00±0.00 nM 24954856
HCT116-p21-/- Growth Inhibition Assay IC50=1.26±0.37 nM 24954856
S1 Growth Inhibition Assay IC50=7.67±0.29 nM 24954856
SW620 Growth Inhibition Assay IC50=0.93±0.29 nM 24954856
LOX-IMVI Growth Inhibition Assay IC50=0.87±0.03 nM 24954856
UACC-62 Growth Inhibition Assay IC50=0.56±0.16 nM 24954856
MDA-MB-435 Growth Inhibition Assay IC50=0.90±0.06 nM 24954856
SF-295 Growth Inhibition Assay IC50=0.88±0.15 nM 24954856
A549 Growth Inhibition Assay IC50=1.26±0.24 nM 24954856
H460 Growth Inhibition Assay IC50=2.58±0.80 nM 24954856
EKVX Growth Inhibition Assay IC50=1.33±0.34 nM 24954856
H146 Growth Inhibition Assay IC50=0.22±0.07 nM 24954856
H526 Growth Inhibition Assay IC50=0.15±0.03 nM 24954856
HuT-78 Growth Inhibition Assay IC50=1.73±0.44 nM 24954856
HA Growth Inhibition Assay 0.625-10nM 48 h induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib 24771510
MS-275 Growth Inhibition Assay 0.625-10nM 48 h induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib 24771510
CD4 T Growth Inhibition Assay 48 h EC50=4.5±1.0 nM 24722454
CD4 T Growth Inhibition Assay 48 h CC50=107±126 nM 24722454
CD4+ T Growth Inhibition Assay EC50=3 nM 24495105
A549 Growth Inhibition Assay 10–100 nM 24/36/48 h inhibits cell growth in both concentration- and time-dependent manner 24485799
JJN3 Growth Inhibition Assay 24/48 h EC50<1 nM; 48 h 24030150
OPM-2 Growth Inhibition Assay 24/48 h EC50s=1 nM; 48 h 24030150
RPMI-8226 Growth Inhibition Assay 24/48 h EC50s=1.8 nM; 48 h 24030150
U266 Growth Inhibition Assay 24/48 h EC50s=10 nM; 48 h 24030150
CA46 Apoptosis Assay 6 h induces blunt apoptosis 23966164
DG75 Apoptosis Assay 6 h induces no apoptosis 23966164
Ramos Apoptosis Assay 6 h induces extensive apoptosis 23966164
ST486 Apoptosis Assay 6 h induces extensive apoptosis 23966164
HuT78 Apoptosis Assay 1/10/100 nM 48 h induces apoptosis at 1 nM 23532732
DpVp35 Apoptosis Assay 1/10/100 nM 48 h induces blunt apoptosis 23532732
DpVp50 Apoptosis Assay 1/10/100 nM 48 h induces blunt apoptosis 23532732
DpP75  Apoptosis Assay 1/10/100 nM 48 h induces blunt apoptosis 23532732
SKOV-3 Growth Inhibition Assay 1–20nM 72 h DMSO reduces cell viability alone and combined with cisplatin 23010348
Brca1 WT Growth Inhibition Assay 1–20nM 72 h DMSO reduces cell viability alone and combined with cisplatin 23010348
Brca1 Null Growth Inhibition Assay 1–20nM 72 h DMSO reduces cell viability alone and combined with cisplatin 23010348
OVCAR-8  Growth Inhibition Assay 1–20nM 72 h DMSO reduces cell viability alone and combined with cisplatin 23010348
NCI/ADR-RES Growth Inhibition Assay 1–20nM 72 h DMSO reduces cell viability alone and combined with cisplatin 23010348
HCT116 Growth Inhibition Assay 5 nM-50 μM 24 h DMSO inhibits cell growth in a concentration-dependent manner 22924958
RKO Growth Inhibition Assay 5 nM-50 μM 24 h DMSO inhibits cell growth in a concentration-dependent manner 22924958
CO115 Growth Inhibition Assay 5 nM-50 μM 24 h DMSO inhibits cell growth in a concentration-dependent manner 22924958
HFS Growth Inhibition Assay 5 nM 24/48/72 h inhibits cell growth time-dependently 22106282
LNCaP Growth Inhibition Assay 5 nM 24/48/72 h inhibits cell growth time-dependently 22106282
A549 Growth Inhibition Assay 5 nM 24/48/72 h inhibits cell growth time-dependently 22106282
697  Growth Inhibition Assay IC50 = 2.5 nM 21538216
697-R Growth Inhibition Assay IC50 = 8.6 nM  21538216
HUT78 Growth Inhibition Assay IC50=1 nM 21198545
THJ-16T Growth Inhibition Assay 1 nM 24 h inhibits cell growth 20810568
HCT116 Function Assay 20 nM 8 h modulates transcript levels for hundreds of genes in either direction 20739454
B104  Function Assay 2 nM 24/48/72 h increases the surface expression of CD20  20686505
HL-60  Cytotoxicity Assay 1-500 nM 24 h induces cytotoxicity in a concentration-dependent manner  20624163
HP100 Cytotoxicity Assay 1-500 nM 24 h induces cytotoxicity in a concentration-dependent manner  20624163
HL-60  Function Assay 10 nM 4/6/16 h induces the generation of hydrogen peroxide from 4h 20624163
HP100 Function Assay 10 nM 4/6/16 h induces the generation of hydrogen peroxide from 4h 20624163
HL-60  Function Assay 10-500 nM 4 h decreases the histone deacetylase (HDAC) activity  20624163
HP100 Function Assay 10-500 nM 4 h decreases the histone deacetylase (HDAC) activity  20624163
11z Kinase Assay 3-100 nM reduces HDAC enzymatic activity (IC50 = 6.5 ± 0.6 nmol/L) 20605144
SKOV-3 Growth Inhibition Assay 4/8/16 nM 48 h inhibits cell growth in a concentration-dependent manner 20404564
OVCAR-3 Growth Inhibition Assay 4/8/16 nM 48 h inhibits cell growth in a concentration-dependent manner 20404564
HBL-2 Growth Inhibition Assay 2-10 nM 24 h IC50=4.3 nM 20068080
Jeko-1 Growth Inhibition Assay 2-50 nM 24 h IC50=11 nM 20068080
Granta-519 Growth Inhibition Assay 5-40 nM 24 h IC50=58.5 nM 20068080
L1236 Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.07 μM 19233470
L428 Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.43 μM 19233470
KM-H2 Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.58 μM 19233470
L540Cy Cytotoxicity Assay 1 nM-100 μM 48 h EC50=0.16 μM 19233470
G401 Function Assay 10 nM 24/48/72 h DMSO increases CDKN1C expression 19221586
STM91-01 Function Assay 10 nM 24/48/72 h DMSO increases CDKN1C expression 19221586
SJSC  Function Assay 10 nM 24/48/72 h DMSO increases CDKN1C expression 19221586
BT16  Function Assay 10 nM 24/48/72 h DMSO increases CDKN1C expression 19221586
NCI-H1299 Growth Inhibition Assay IC50=4.6±0.2 ng/ml 19179890
NCI-2882 Growth Inhibition Assay IC50=1.6±0.04 ng/ml 19179890
HCC95 Growth Inhibition Assay IC50=2.5±0.05 ng/ml 19179890
NCI-H23 Growth Inhibition Assay IC50=2.9±0.2 ng/ml 19179890
NCI-H157 Growth Inhibition Assay IC50=1.6±0.02 ng/ml 19179890
NCI-H460 Growth Inhibition Assay IC50=2.1±0.07 ng/ml 19179890
NCI-H1975 Growth Inhibition Assay IC50=1.3±0.04 ng/ml 19179890
NCI-H820 Growth Inhibition Assay IC50=2.4±0.1 ng/ml 19179890
NCI-H1650 Growth Inhibition Assay IC50=4.9±0.3 ng/ml 19179890
DTC1 Growth Inhibition Assay IC50=0.51 nM 18566246
KAO Growth Inhibition Assay IC50=0.91 nM 18566246
SU-CCS-1 Growth Inhibition Assay IC50=0.89 nM 18566246
SYO-1 Growth Inhibition Assay IC50=0.67 nM 18566246
FUJI Growth Inhibition Assay IC50=1.31 nM 18566246
SKNMC Growth Inhibition Assay IC50=1.17 nM 18566246
402-91 Growth Inhibition Assay IC50=1.26 nM 18566246
1765-92 Growth Inhibition Assay IC50=1.77 nM 18566246
JN-DSRCT-1 Growth Inhibition Assay IC50=1.25 nM 18566246
NMS-2PC Growth Inhibition Assay IC50=0.81 nM 18566246
HL60 Growth Inhibition Assay IC50=1.86 nM 18566246
A549 Growth Inhibition Assay IC50=3.24 nM 18566246
SW480 Growth Inhibition Assay IC50=2.69 nM 18566246
MCF7 Growth Inhibition Assay IC50=3.55 nM 18566246
PC-3 Growth Inhibition Assay IC50=2.51 nM 18566246
MMRU Growth Inhibition Assay IC50=2.57 nM 18566246
Hs68 Growth Inhibition Assay IC50=>10 nM 18566246
hMSC-001F Growth Inhibition Assay IC50=>10 nM 18566246
mammalian cells Function assay Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM. 14584932
mammalian cells Function assay Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM. 14584932
MCF7 Growth inhibition assay Growth inhibition of MCF7 cells, IC50 = 0.00075 μM. 17958342
A498 Cytotoxicity assay 6 days Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM. 21967146
COLO205 Cytotoxicity assay 6 days Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM. 21967146
U251 Cytotoxicity assay 6 days Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM. 21967146
RXF393 Cytotoxicity assay 6 days Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM. 21967146
MDA-MB-468 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM. 21967146
COLO205 Cytotoxicity assay 6 days Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM. 21967146
UACC257 Cytotoxicity assay 6 days Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM. 21967146
U251 Cytotoxicity assay 6 days Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM. 21967146
A498 Cytotoxicity assay 6 days Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM. 21967146
NCI-H322M Cytotoxicity assay 6 days Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM. 21967146
SF295 Cytotoxicity assay 6 days Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM. 21967146
RXF393 Cytotoxicity assay 6 days Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM. 21967146
NCI60 Cytotoxicity assay 6 days Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM. 21967146
SN12C Cytotoxicity assay 6 days Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM. 21967146
MDA-MB-231 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM. 21967146
ACHN Cytotoxicity assay 6 days Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM. 21967146
SN12C Cytotoxicity assay 6 days Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM. 21967146
UO31 Cytotoxicity assay 6 days Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM. 21967146
Caki1 Cytotoxicity assay 6 days Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM. 21967146
NCI60 Cytotoxicity assay 6 days Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM. 21967146
MDA-MB-231 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM. 21967146
MDA-MB-468 Cytotoxicity assay 6 days Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM. 21967146
ACHN Cytotoxicity assay 6 days Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM. 21967146
UACC257 Cytotoxicity assay 6 days Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM. 21967146
NCI-H322M Cytotoxicity assay 6 days Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM. 21967146
SF295 Cytotoxicity assay 6 days Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM. 21967146
Caki1 Cytotoxicity assay 6 days Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM. 21967146
NCI-H23 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
NCI-H522 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
OVCAR5 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
SW620 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
MDA-MB-435 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
COLO205 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
LOXIMVI Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
UACC62 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
MDA-MB-231 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
SF295 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
U251 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
OVRAC3 Antitumor assay 1.6 to 2.4 mg/kg up to 5 days Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay 21967146
LLC Function assay Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM. 22305612
NCI-H522 Growth inhibition assay Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM. 23313638
LOXIMVI Growth inhibition assay Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM. 23313638
A549 Growth inhibition assay Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM. 23313638
OVCAR5 Growth inhibition assay Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM. 23313638
MKN74 Growth inhibition assay Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. 23313638
NCI-H460 Growth inhibition assay Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. 23313638
HCT116 Growth inhibition assay Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. 23313638
HCC2998 Growth inhibition assay Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. 23313638
MKN1 Growth inhibition assay Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM. 23313638
SKOV3 Growth inhibition assay Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. 23313638
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. 23313638
KM12 Growth inhibition assay Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM. 23313638
DMS114 Growth inhibition assay Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. 23313638
SF539 Growth inhibition assay Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. 23313638
U251 Growth inhibition assay Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM. 23313638
SF295 Growth inhibition assay Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM. 23313638
MCF7 Growth inhibition assay Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM. 23313638
NCI-H23 Growth inhibition assay Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. 23313638
OVCAR3 Growth inhibition assay Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. 23313638
MKN7 Growth inhibition assay Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. 23313638
SF268 Growth inhibition assay Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. 23313638
MDA-MB-231 Growth inhibition assay Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. 23313638
OVCAR8 Growth inhibition assay Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. 23313638
DMS273 Growth inhibition assay Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM. 23313638
DU145 Growth inhibition assay Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM. 23313638
RXF631L Growth inhibition assay Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM. 23313638
HBC4 Growth inhibition assay Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM. 23313638
SNB75 Growth inhibition assay Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM. 23313638
BSY1 Growth inhibition assay Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM. 23313638
NCI-H226 Growth inhibition assay Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM. 23313638
SNB78 Growth inhibition assay Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM. 23313638
HBC5 Growth inhibition assay Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM. 23313638
MKN45 Growth inhibition assay Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM. 23313638
MKN28 Growth inhibition assay Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM. 23313638
PC3 Growth inhibition assay Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM. 23313638
ACHN Growth inhibition assay Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. 23313638
OVCAR4 Growth inhibition assay Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. 23313638
St-4 Growth inhibition assay Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM. 23313638
HCT15 Growth inhibition assay Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM. 23313638
CD4+ T Function assay 7 days Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM. 24495105
NCI-H522 Cytotoxicity assay Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM. 24589486
LOXIMVI Cytotoxicity assay Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM. 24589486
A549 Cytotoxicity assay Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM. 24589486
OVCAR5 Cytotoxicity assay Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM. 24589486
NCI-H460 Cytotoxicity assay Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM. 24589486
MKN74 Cytotoxicity assay Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM. 24589486
HCC2998 Cytotoxicity assay Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM. 24589486
HCT116 Cytotoxicity assay Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM. 24589486
MKN1 Cytotoxicity assay Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM. 24589486
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM. 24589486
SKOV3 Cytotoxicity assay Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM. 24589486
KM12 Cytotoxicity assay Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM. 24589486
SF539 Cytotoxicity assay Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM. 24589486
293T Function assay 30 mins Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM. 24589486
DMS114 Cytotoxicity assay Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM. 24589486
U251 Cytotoxicity assay Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM. 24589486
SF295 Cytotoxicity assay Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM. 24589486
MCF7 Cytotoxicity assay Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM. 24589486
OVCAR3 Cytotoxicity assay Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM. 24589486
NCI-H23 Cytotoxicity assay Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM. 24589486
SF268 Cytotoxicity assay Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM. 24589486
MKN7 Cytotoxicity assay Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM. 24589486
OVCAR8 Cytotoxicity assay Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM. 24589486
MDA-MB-231 Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM. 24589486
DMS273 Cytotoxicity assay Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM. 24589486
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM. 24589486
RXF631L Cytotoxicity assay Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM. 24589486
HBC4 Cytotoxicity assay Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM. 24589486
SNB75 Cytotoxicity assay Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM. 24589486
BSY1 Cytotoxicity assay Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM. 24589486
NCI-H226 Cytotoxicity assay Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM. 24589486
SNB78 Cytotoxicity assay Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM. 24589486
HBC5 Cytotoxicity assay Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM. 24589486
MKN45 Cytotoxicity assay Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM. 24589486
MKN28 Cytotoxicity assay Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM. 24589486
PC3 Cytotoxicity assay Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM. 24589486
ACHN Cytotoxicity assay Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM. 24589486
OVCAR4 Cytotoxicity assay Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM. 24589486
St-4 Cytotoxicity assay Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM. 24589486
293T Function assay 30 mins Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM. 24589486
HCT15 Cytotoxicity assay Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM. 24589486
mink Mv1Lu Function assay 24 hrs Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM. 24997578
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM. 25147612
MOLT4 Antiproliferative assay 72 hrs Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM. 26331334
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM. 26331334
U937 Antiproliferative assay 72 hrs Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM. 26331334
HLF Antiproliferative assay 72 hrs Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM. 26331334
WI38 Antiproliferative assay 72 hrs Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM. 26331334
U937 Function assay 24 hrs Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis 26331334
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM. 26481659
IGROV1/Pt1 Antiproliferative assay 72 hrs Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM. 26481659
IGROV1 Antiproliferative assay 72 hrs Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM. 26481659
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire 540.7 Formule

C24H36N4O6S2

 Stockage (À compter de la date de réception)
N° CAS 128517-07-7 -- Stockage des solutions mères

Synonymes FK228, Depsipeptide, FR 901228, NSC 630176, Smiles CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

Solubilité (Solubility)

In vitro
Lot:

DMSO : 10 mg/mL (18.49 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

mg/kg g μL

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Caractéristiques
More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
Targets/IC50/Ki
HDAC1
(Cell-free assay)
36 nM
HDAC2
(Cell-free assay)
47 nM
In vitro
Contrairement au TSA, la forme active redFK de Romidepsin inhibe fortement HDAC1 et HDAC2 avec des IC50 de 1,6 nM et 3,9 nM, respectivement, mais est relativement faible pour inhiber HDAC4 et HDAC6 avec des IC50 de 25 nM et 790 nM, respectivement. Ce composé est 17 à 23 fois plus faible que le redFK pour inhiber ces HDACs avec des IC50 de 36 nM, 47 nM, 510 nM et 14 μM, respectivement. Le traitement avec ce produit chimique dans les cellules HeLa induit l'acétylation des histones et l'expression de p21 avec une EC50 de 3,0 nM, plus fortement que le redFK avec une EC50 de 11 nM en raison de l'instabilité du redFK. En plus de l'arrêt en G2/M, ce composé provoque une régulation négative de la cycline D1 et une induction de p21 indépendante de p53, entraînant l'inhibition de la CDK et la déphosphorylation de Rb, ce qui conduit à un arrêt de la croissance en phase G1 précoce. Il est 100 fois plus puissant que le TSA et 1 000 000 de fois plus puissant que le butyrate pour inhiber la prolifération des cellules A549. Cet agent inhibe la croissance des cellules U-937, K562 et CCRF-CEM avec des IC50 de 5,92 nM, 8,36 nM et 6,95 nM, respectivement. Il favorise l'apoptose dans les cellules de leucémie lymphoïde chronique (LLC) à une concentration correspondant à celle à laquelle se produisent l'acétylation de H3 et H4 et l'inhibition de HDAC, impliquant sélectivement l'activation de la caspase 8 et de la caspase effectrice 3, ainsi qu'une régulation négative de la protéine c-FLIP. Dans 11 des 13 (85 %) lignées cellulaires de carcinome rénal et dans 16 des 37 (43 %) autres lignées cellulaires cancéreuses, ce composé régule à la hausse les récepteurs de mort tumorale et potentialise la destruction tumorale médiée par les cellules tueuses naturelles (NK). Il présente une cytotoxicité dépendante de la concentration contre un panel de lignées cellulaires de lymphome à cellules du manteau (LCM).
Essai kinase
Activité inhibitrice de HDAC
Pour le dosage enzymatique, 10 μL d'histones marquées au [3H]-acétyle (25 000 cpm/10 μg) sont ajoutés à 90 μL de la fraction enzymatique HDAC extraite de cellules 293T surexprimant HDAC1 ou HDAC2 en présence de concentrations croissantes de Romidepsin, et le mélange est incubé à 37 °C pendant 15 minutes. La réaction enzymatique est linéaire pendant au moins 1 heure. La réaction est arrêtée par l'ajout de 10 μL de HCl concentré. L'acide [3H]-acétique libéré est extrait avec 1 mL d'acétate d'éthyle, et 0,9 mL de la couche de solvant est prélevé dans 5 mL de solution de scintillant aqueux II pour la détermination de la radioactivité. Les valeurs IC50 sont déterminées à partir d'au moins trois courbes dose-réponse indépendantes.
In vivo
Le traitement par Romidepsin inhibe puissamment la néovascularisation de l'embryon de poulet et celle des souris adultes dans le test du plug Matrigel. L'administration de ce composé à 0,1-1 mg/kg deux fois par semaine prolonge significativement la survie des souris porteuses d'un lymphome U-937, avec des temps de survie médians de 30,5 (0,56 mg/kg) et 33 jours (0,32 mg/kg), respectivement (contre 20 jours chez les souris témoins).
Références
  • [4] https://pubmed.ncbi.nlm.nih.gov/11774279/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12234611/
  • [6] https://pubmed.ncbi.nlm.nih.gov/12649137/
  • [7] https://pubmed.ncbi.nlm.nih.gov/16849582/
  • [8] https://pubmed.ncbi.nlm.nih.gov/18223231/
  • [9] https://pubmed.ncbi.nlm.nih.gov/20068080/

Applications (Applications)

Méthodes Biomarqueurs Images PMID
Western blot p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT
S3020-WB0
19682393
Growth inhibition assay Cell viability
S3020-viability1
27444036
Immunofluorescence SS18/TLE1 Cleaved caspase-3
S3020-IF1
27120803

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT Recrutement Conditions Promoteur/Collaborateurs Date de début Phases
NCT03770000 Completed
T Cell Lymphoma
Rhizen Pharmaceuticals SA
 March 12 2019 Phase 1|Phase 2
NCT02616965 Active not recruiting
Cutaneous T-cell Lymphoma (CTCL)
Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation
 February 22 2017 Phase 1
NCT02616874 Completed
HIV
IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint
 February 2016 Phase 1