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Tubastatin A HDAC Inhibiteur

Réf. CatalogueS8049

Tububastatin A est un inhibiteur puissant et sélectif de HDAC6 avec une IC50 de 15 nM dans un essai sans cellules. Il est sélectif contre toutes les autres isozymes (1000 fois) sauf HDAC8 (57 fois). Ce composé favorise l'autophagy et augmente l'apoptosis.
Tubastatin A HDAC Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 335.4

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.63%
99.63

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
Sf9 Function assay 2 hrs Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay, IC50 = 0.0035 μM. 27541357
Sf9 Function assay Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate by fluorescence assay, IC50 = 0.011 μM. 27541357
Sf9 Function assay 30 mins Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 0.013 μM. 29549837
Sf9 Function assay 90 mins Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using RHKK(Ac) as substrate after 90 mins by fluorimetric method, IC50 = 0.0137 μM. 28038324
Sf9 Function assay 2 hrs Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 0.015 μM. 23009203
Sf9 Function assay Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.015 μM. 23905680
Sf9 Function assay 90 mins Inhibition of human recombinant N-terminal GST-tagged full length HDAC6 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 0.0304 μM. 30092367
HeLaS3 Function assay 15 mins Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 0.031 μM. 28337317
insect cells Function assay 4 hrs Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0349 μM. 27650925
SHSY5Y Function assay 8 hrs Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0943 μM. 27650925
SHSY5Y Function assay 8 hrs Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.1221 μM. 27650925
Sf9 Function assay 4 hrs Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 4 hrs fluorescence assay, IC50 = 0.718 μM. 29549837
Sf9 Function assay Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate, IC50 = 0.854 μM. 23905680
Sf9 Function assay 1 hr Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 1 hr fluorescence assay, IC50 = 0.967 μM. 29549837
SHSY5Y Function assay 8 hrs Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 1.1097 μM. 27650925
Sf9 Function assay 30 mins Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 1.54 μM. 29549837
Sf9 Function assay 90 mins Inhibition of human recombinant C-terminal His/FLAG-tagged full length HDAC1 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 1.91 μM. 30092367
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2 μM. 27541357
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells, IC50 = 2 μM. 29945795
Sf9 Function assay 30 mins Inhibition of full length human recombinant C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (95 to 489 residues) expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 2.26 μM. 29549837
HeLa Function assay 6 hrs Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay, IC50 = 2.5 μM. 25454270
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
HeLaS3 Function assay 15 mins Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.7 μM. 28337317
HeLaS3 Function assay 15 mins Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.9 μM. 28337317
Jurkat Cytotoxicity assay 72 hrs Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 3.38 μM. 24304348
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. 27541357
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells, IC50 = 3.7 μM. 29945795
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
HeLaS3 Function assay 15 mins Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 3.9 μM. 28337317
CAL27 Antiproliferative assay 72 hrs Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay, IC50 = 4.6 μM. 28581289
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 8.6 μM. 27541357
PC3 Antiproliferative assay Antiproliferative activity against human PC3 cells, IC50 = 8.6 μM. 29945795
Sf9 Function assay 30 mins Inhibition of full length human recombinant C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 9.97 μM. 29549837
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. 27541357
MDA-MB-231 Antiproliferative assay Antiproliferative activity against human MDA-MB-231 cells, IC50 = 10.4 μM. 29945795
Cal27CisR Antiproliferative assay 72 hrs Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay, IC50 = 10.8 μM. 28581289
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 10.88 μM. 24304348
Cal27CisR Function assay 18 hrs Inhibition of HDAC in human Cal27CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 12.1 μM. 28581289
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by MTS assay, IC50 = 14.81 μM. 25899338
THLE2 Cytotoxicity assay 72 hrs Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay, LC50 = 15.1 μM. 29549837
CAL27 Function assay 18 hrs Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 16.1 μM. 28581289
Sf9 Function assay 2 hrs Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 16.4 μM. 23009203
Sf9 Function assay Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 16.4 μM. 23905680
B16 Growth inhibition assay 48 hrs Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay, GI50 = 40.5 μM. 23009203
KB Function assay 14 uM 24 hrs Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation at 14 uM after 24 hrs by Western blotting analysis 25899338
KMS-12-BM Function assay 15 uM up to 48 hrs Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method 27541357
MOLM14 Function assay 15 uM up to 48 hrs Inhibition of HDAC6 in human MOLM14 cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method 27541357
U937 Function assay 2 uM 18 hrs Inhibition of HDAC6 in human U937 cells assessed as increase in alpha-tubulin acetylation at Lys-40 residue at 2 uM after 18 hrs by Western blot method 28337317
LNCAP Function assay 24 hrs Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation measured after 24 hrs relative to control 27717544
human Function assay 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level measured after 24 hrs relative to control 27717544
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
HEL Cell cycle assay 1 to 5 uM 48 hrs Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 5 uM after 48 hrs propidium iodide staining based flow cytometry 29940115
HeLa Function assay 2 uM 12 hrs Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis 29533873
HEK293 Function assay 10 uM 24 hrs Inhibition of HDAC1 in HEK293 cells assessed as increase in histone H3 acetylation at 10 uM after 24 hrs by Western blot method 28523102
MV4-11 Function assay 200 nM 24 hrs Inhibition of HDAC6 in human MV4-11 cells assessed as accumulation of acetylated alpha-tubulin at 200 nM after 24 hrs by Western blot analysis 29738953
HCT116 Cell cycle assay 5 uM 48 hrs Cell cycle arrest in human HCT116 cells assessed as accumulation at sub-G1 phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric method 28038324
PC12 Neuroprotective assay 10 uM 24 hrs Neuroprotective activity against H2O2-induced toxicity in rat PC12 cells assessed as cell viability at 10 uM pretreated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by MTT assay relative to control 30385227
PC12 Neuroprotective assay 5 uM 24 hrs Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay 30385227
PC12 Neuroprotective assay 10 uM 24 hrs Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay 30385227
PC12 Cytoprotective assay 24 hrs Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based fluorescence analysis 30385227
PC12 Cytoprotective assay 24 hrs Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based inverted fluorescence microscopic analysis 30385227
PC12 Neuroprotective assay 5 to 10 uM 24 hrs Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 to 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs coincubated with ebselen by MTT assay 30385227
PC12 Antioxidant assay 5 uM 24 hrs Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by DCFH-DA dye-based fluorescence analysis 30385227
PC12 Antioxidant assay 5 uM 24 hrs Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with ebselen by DCFH-DA dye-based fluore 30385227
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire 335.4 Formule

C20H21N3O2

Stockage (À compter de la date de réception)
N° CAS 1252003-15-8 Télécharger le SDF Stockage des solutions mères

Synonymes N/A Smiles CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO

Solubilité (Solubility)

In vitro
Lot:

DMSO : 16.7 mg/mL (49.79 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)

Targets/IC50/Ki
HDAC6
(Cell-free assay)
15 nM
In vitro
Tubastatin A est sélectif pour toutes les isozymes sauf HDAC8 et maintient une sélectivité plus de 1000 fois supérieure à toutes les isoformes, à l'exception de HDAC8, où il présente une sélectivité d'environ 57 fois. Ce composé induit préférentiellement l'hyperacétylation de l'α-tubuline à 2,5 μM. Une légère induction de l'hyperacétylation des histones est observée pour cette substance chimique à 10 μM. Il présente une protection dose-dépendante contre la mort cellulaire neuronale induite par l'acide homocystéique, commençant à 5 μM avec une protection presque complète à 10 μM. Ce composé (10 μM) induit une augmentation des niveaux d'α-tubuline acétylée et la restauration de l'expression des cils primaires dans les lignées cellulaires de cholangiocarcinome (18 fois) ; et la restauration des cils primaires est corrélée à la régulation négative des voies de signalisation Hedgehog (Hh) et MAPK, ainsi qu'à une diminution des taux de prolifération cellulaire (en moyenne de 50 %) et de l'invasion (de 40 %). Il montre une inhibition significative du TNF-α et de l'IL-6 dans les macrophages THP-1 humains stimulés par le LPS avec une IC50 de 272 nM et 712 nM. Cet inhibiteur inhibe la sécrétion d'oxyde nitrique (NO) dans les macrophages murins Raw 264.7 de manière dose-dépendante avec une IC50 de 4,2 μM.
Essai kinase
Essais enzymatiques HDAC
Tubastatin A est dissous et dilué dans un tampon d'essai (50 mM HEPES, pH 7,4, 100 mM KCl, 0,001 % Tween-20, 0,05 % BSA et 20 μM tris(2-carboxyéthyl)phosphine) à 6 fois la concentration finale. Les enzymes HDAC sont diluées à 1,5 fois la concentration finale dans le tampon d'essai et pré-incubées avec ce composé pendant 10 minutes avant l'addition du substrat. La quantité de FTS (HDAC1, HDAC2, HDAC3 et HDAC6) ou de MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8 et HDAC9) utilisée pour chaque enzyme est égale à la constante de Michaelis (Km), telle que déterminée par une courbe de titration. Le FTS ou le MAZ-1675 est dilué dans le tampon d'essai à 6 fois la concentration finale avec 0,3 μM de trypsine de qualité séquençage. Le mélange substrat/trypsine est ajouté au mélange enzyme/composé et la plaque est agitée pendant 60 secondes puis placée dans un lecteur de microplaques SpectraMax M5. La réaction enzymatique est surveillée pour la libération de 7-amino-4-méthoxy-coumarine pendant 30 minutes, après désacétylation de la chaîne latérale de lysine dans le substrat peptidique, et la vitesse linéaire de la réaction est calculée.
In vivo
Tubastatin A réduit la croissance du cholangiocarcinome in vivo. Ce composé (10 mg/kg) induit des poids tumoraux moyens 6 fois inférieurs dans un modèle orthotopique de rat syngénique de cholangiocarcinome, et une réduction des rapports poids tumoral/poids hépatique et poids corporel (5 et 5,6 fois, respectivement), ainsi qu'une plus grande fréquence de cholangiocytes ciliés par rapport aux contrôles (29 % vs 1,4 %). Il diminue significativement la quantité de cellules PCNA-positives dans les tumeurs traitées par rapport aux contrôles véhiculés (34 % vs 65 %). Ce produit chimique montre une inhibition significative du volume de la patte à 30 mg/kg i.p. dans un modèle animal d'inflammation induite par l'adjuvant complet de Freund (FCA). Il (30 mg/kg i.p.) atténue significativement les scores cliniques (~ 70 %) et l'expression de l'IL-6 dans les tissus de la patte de souris DBA1 atteintes d'arthrite induite par le collagène.
Références
  • [4] https://pubmed.ncbi.nlm.nih.gov/22262760/

Applications (Applications)

Méthodes Biomarqueurs Images PMID
Western blot EGFR / p-AKT / AKT / p-ERK / ERK
S8049-WB1
29665050
Immunofluorescence α-tubulin / Acetylated tubulin HDAC6
S8049-IF1
23798680

Foire aux questions (Frequently Asked Questions)

Question 1:
We are planning to order some, but I found out there are two versions of it. One has HCl and one does not. Which one do you recommend for live cell use? Will the HCl containing version significantly change the pH?

Réponse :
S8049 and S2627 have the same molecular structure. The only difference is S2627 containing HCl and has higher solubility in DMSO (74 mg/mL vs. S8049 9 mg/mL). Since they are the same molecule, its biological function should be similar. I would recommend to use S2627 for cell culture study.

Question 2:
What vehicle do you recommend to dissolve it for in vivo experiments?

Réponse :
It can be dissolved in 2% DMSO/30% PEG 300/PBS at 2.5 mg/mL as a clear solution, and is also a clear solution in 2% DMSO/ corn oil at 2.5 mg/mL. This compound in 2% DMSO/0.5% Tween 80/PBS is a homogeneous suspension at 2.5 mg/mL at first. After stay for a while, the precipitation goes out at the bottom of the tube.