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Triptolide Hsp90 Middle Domain Inhibitor

Name: Triptolide
Brand: Selleck Chemicals
SKU: S3604
Rating: 5 (47 reviews)

Réf. CatalogueS3604

Triptolide est un triépoxyde de diterpène, un agent immunosuppresseur extrait de la plante chinoise Tripterygium wilfordii. Il agit comme un inhibiteur de NF-κB avec une double action par perturbation de l'interaction p65/CBP et par réduction de la protéine p65. Triptolide (PG490) abroge la fonction de transactivation du facteur de transcription de choc thermique 1 (HSF1). Triptolide inhibe MDM2 et induit l'apoptose via une voie indépendante de p53.

Triptolide ADC Cytotoxin Produit chimique Chemical Structure

Structure chimique

Poids moléculaire: 360.4

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.95%

99.95

Cibles apparentées	NF-κB HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Autre ADC Cytotoxin Inhibiteurs	SN-38 Luteolin (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Luteoloside Sacituzumab-govitecan Lappaconite HBr

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

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Description de l'activité	PMID
HT-29	Cytotoxicity against			Cytotoxicity against human HT-29 cells, IC50=0.0021μM	21470864
HCT116	Cytotoxicity against			Cytotoxicity against human HCT116 cells assessed as decrease in cell viability, IC50=0.0047μM	31121546
SKOV3	Antiproliferative activity against		72 hrs	Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay, IC50=0.006μM	20833543
SKOV3	Cytotoxicity against		72 hrs	Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay, IC50=0.006μM	24378709
SKOV3	Cytotoxic activity against		72 hrs	Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0072μM	28011223
KBM5	Cytotoxicity against		72 hrs	Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.0083μM	20149665
SKOV3	Cytotoxicity against			Cytotoxicity against human SKOV3 cells by SRB assay, IC50=0.009μM	19637874
MDA-MB-468	Cytotoxicity against			Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=0.01μM	19637874
HCT116	Cytotoxicity against		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.01μM	19637874
SKOV3	Cytotoxicity against		72 hrs	Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay, IC50=0.01μM	19637874
KBM5	Cytotoxicity against		72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.0103μM	20149665
Rh30	Cytotoxicity against		72 hrs	Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay, IC50=0.014μM	19637874
A549	Antagonist activity at			Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay, IC50=0.014μM	23895492
SGC7901	Cytotoxicity against		72 hrs	Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay, IC50=0.015μM	19637874
MOLT4	Cytotoxicity against		72 hrs	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=0.017μM	19637874
A549	Cytotoxic activity against		72 hrs	Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0175μM	28011223
SMMC7721	Cytotoxicity against		72 hrs	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=0.018μM	19637874
PC3	Cytotoxic activity against		72 hrs	Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0183μM	28011223
MCF7	Cytotoxicity against		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=0.019μM	19637874
A549	Cytotoxicity against			Cytotoxicity against human A549 cells, IC50=0.019μM	21470864
PC3	Cytotoxicity against			Cytotoxicity against human PC3 cells by SRB assay, IC50=0.02μM	19637874
Bel7402	Cytotoxicity against		72 hrs	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay, IC50=0.02μM	19637874
PC3	Antiproliferative activity against		72 hrs	Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay, IC50=0.02μM	20833543
PC3	Cytotoxicity against		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay, IC50=0.02μM	24378709
PC3	Cytotoxicity against			Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.02μM	25467158
786-O	Cytotoxicity against		72 hrs	Cytotoxicity against human 786-O cells after 72 hrs by MTT assay, IC50=0.022μM	19637874
A549	Antagonist activity at			Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA, IC50=0.023μM	23895492
MDA-MB-231	Cytotoxicity against		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.024μM	19637874
DU145	Cytotoxicity against		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=0.024μM	19637874
HO8910	Cytotoxicity against		72 hrs	Cytotoxicity against human HO8910 cells after 72 hrs by MTT assay, IC50=0.028μM	19637874
HCT15	Cytotoxicity against		72 hrs	Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay, IC50=0.029μM	19637874
A549	Growth inhibition of human			Growth inhibition of human A549 cells, IC50=0.03μM	28814374
32D	Cytotoxicity against		72 hrs	Cytotoxicity against mouse 32D cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.032μM	20149665
U251	Cytotoxicity against			Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.033μM	25467158
32D	Cytotoxicity against		72 hrs	Cytotoxicity against imatinib-resistant mouse 32D cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.034μM	20149665
PC3	Cytotoxicity against		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=0.043μM	19637874
KB	Cytotoxicity against		72 hrs	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=0.043μM	19637874
HepG2	Cytotoxicity against		48 hrs	Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay, IC50=0.0433μM	30613335
HeLa	Cytotoxicity against		72 hrs	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.047μM	19637874
U251	Cytotoxicity against		72 hrs	Cytotoxicity against human U251 cells after 72 hrs by MTT assay, IC50=0.049μM	19637874
K562	Cytotoxicity against		72 hrs	Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=0.05μM	19637874
NIH/3T3	Cytotoxicity against			Cytotoxicity against mouse NIH/3T3 cells assessed as decrease in cell viability, IC50=0.05μM	31121546
SW1116	Cytotoxicity against		72 hrs	Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay, IC50=0.052μM	19637874
A549	Cytotoxicity against		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.059μM	19637874
HeLa	Cytotoxicity against			Cytotoxicity against human HeLa cells assessed as decrease in cell viability, IC50=0.087μM	31121546
Jurkat	Cytotoxicity against			Cytotoxicity against human Jurkat cells assessed as decrease in cell viability, IC50=0.14μM	31121546
MKN28	Cytotoxicity against		72 hrs	Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay, IC50=0.2μM	19637874
MDCK	Cytotoxicity against			Cytotoxicity against MDCK cells assessed as decrease in cell viability, IC50=1.2μM	31121546
Pkd1-/-	Induction of			Induction of cell growth arrest in mouse Pkd1-/- cells in presence of calcium	17360534
Pkd1-/-	Increase in	100 nM	96 hrs	Increase in p21CIP/WAF expression in mouse Pkd1-/- cells at 100 nM after 96 hrs by Western blot analysis	17360534
Pkd1+/-	Increase in	100 nM		Increase in PC2 dependent calcium release in mouse Pkd1+/- cells at 100 nM	17360534
Pkd1-/-	Increase in	100 nM		Increase in PC2 dependent calcium release in mouse Pkd1-/- cells at 100 nM	17360534
Pkd1-/-	Increase in	50 uM		Increase in calcium release in mouse Pkd1-/- cells at 50 uM in presence of RyR antagonist dantrolene	17360534
Pkd2+/-	Growth inhibition of PC2 expressing mouse	100 nM	24 hrs	Growth inhibition of PC2 expressing mouse Pkd2+/- cells as cell death at 100 nM after 24 hrs	17360534
KBM5	Cytotoxicity against	0.001 to 17 uM	72 hrs	Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl at 0.001 to 17 uM after 72 hrs by MTS assay	20149665
KBM5	Cytotoxicity against	0.001 to 17 uM	72 hrs	Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant at 0.001 to 17 uM after 72 hrs by MTS assay	20149665
LNCAP	Antagonist activity at	5 uM	24 hrs	Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay	27994731
LNCAP	Antagonist activity at	500 nM	24 hrs	Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 500 nM after 24 hrs by dual luciferase reporter gene assay	27994731
HepG2	Antitumor activity against	0.2 mg/kg	15 days	Antitumor activity against human HepG2 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.2 mg/kg, ip administered once daily for 15 days	30613335
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	360.4	Formule	C₂₀H₂₄O₆	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	38748-32-2	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant

Solubilité (Solubility)

In vitro
Lot:

DMSO : 72 mg/mL (199.77 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:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	3.000mg/ml (8.32mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

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	NF-κB HSF1 MDM2
In vitro	Triptolide est un triépoxyde diterpénique doté de puissantes propriétés immunosuppressives et anti-inflammatoires. Ce composé est montré pour inhiber l'expression d'IL-2 dans les cellules T activées au niveau du facteur purine-box/nucléaire et de l'activation de la transcription médiatisée par NF-κB. Il inhibe la prolifération et la formation de colonies de cellules tumorales à des concentrations extrêmement faibles (2–10 ng/mL). Ce produit chimique a une activité inhibitrice sur les cellules des lignées cellulaires de cancer du sein, de l'estomac et de leucémie HL-60. Il induit l'apoptose dans les cellules tumorales en bloquant l'activation de NF-κB et en sensibilisant les cellules tumorales à la mort cellulaire programmée induite par le TNF-α.
In vivo	Triptolide synergie avec la cyclosporine A pour promouvoir la survie des greffes dans des modèles animaux et pour la suppression de la maladie du greffon contre l'hôte dans les greffes de moelle osseuse allogéniques. De plus, il induit l'apoptose dans les cellules tumorales et potentialise l'induction de l'apoptose par le facteur de nécrose tumorale (TNF-α) en partie par la suppression de l'induction de c-IAP2 et c-IAP1. Le traitement avec ce composé pendant 2 à 3 semaines inhibe la croissance des xénogreffes formées par quatre lignées cellulaires tumorales différentes (mélanome B16, cancer du sein MDA-435, cancer de la vessie TSU et carcinome gastrique MGC80-3), indiquant que le TPL a un large spectre d'activité contre les tumeurs qui contiennent à la fois des formes sauvages et mutantes de p53. De plus, il inhibe la métastase expérimentale des cellules B16F10 vers les poumons et les rates des souris. Il a des activités in vitro et in vivo contre des modèles murins de maladie rénale polykystique. DL50 : Souris 0,83 mg/kg (i.v.).
Références	[1] https://pubmed.ncbi.nlm.nih.gov/10224109/ [2] https://pubmed.ncbi.nlm.nih.gov/12533674/ [3] https://pubmed.ncbi.nlm.nih.gov/10224110/ [4] https://pubmed.ncbi.nlm.nih.gov/17360534/ [5] https://pubmed.ncbi.nlm.nih.gov/23583804/

Applications (Applications)

Méthodes	Biomarqueurs	Images	PMID
Western blot	c-Jun MDM2 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 p-PI3K / PI3K / p85 / p110		22666381
Growth inhibition assay	Cell viability		22666381

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