Home NF-κB ADC Cytotoxin Chemikalie Triptolide

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Triptolide Hsp90 Middle Domain Inhibitor

Kat.-Nr.: S3604

Triptolide ist ein Diterpen-Triepoxid, ein immunsuppressives Mittel, das aus der chinesischen Heilpflanze Tripterygium wilfordii extrahiert wird. Es fungiert als NF-κB-Inhibitor mit doppelter Wirkung durch Störung der p65/CBP-Interaktion und durch Reduktion des p65-Proteins. Triptolide (PG490) hebt die Transaktivierungsfunktion des Hitzeschock-Transkriptionsfaktors 1 (HSF1) auf. Triptolide hemmt MDM2 und induziert Apoptose über einen p53-unabhängigen Signalweg.
Triptolide ADC Cytotoxin Chemikalie Chemical Structure

Chemische Struktur

Molekulargewicht: 360.4

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.95%
99.95

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung 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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Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 360.4 Formel

C20H24O6

 Lagerung (Ab Erhaltdatum)
CAS-Nr. 38748-32-2 SDF herunterladen Lagerung von Stammlösungen

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 72 mg/mL (199.77 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewicht-Rechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie unten die Informationen ein (Empfohlen: Ein zusätzliches Tier einplanen, um Verluste während des Experiments auszugleichen)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, nicht die Formulierung. Bitte kontaktieren Sie uns zuerst, wenn im Abschnitt Löslichkeit keine In-vivo-Formulierung angegeben ist.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammflüssigkeit: mg Wirkstoff voraufgelöst in μL DMSO ( Konzentration der Stammflüssigkeit mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der jeweiligen Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzuμL PEG300, mischen und aufklären, fügen Sie als Nächstes hinzuμL Tween 80, mischen und aufklären, fügen Sie als Nächstes hinzu μL ddH2O, mischen und aufklären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzu μL Maisöl, mischen und aufklären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, die Lösungsmittel in der richtigen Reihenfolge hinzuzufügen. Sie müssen sicherstellen, dass die im vorherigen Schritt erhaltene Lösung klar ist, bevor Sie das nächste Lösungsmittel hinzufügen. Physikalische Methoden wie Vortexen, Ultraschall oder ein warmes Wasserbad können zur Unterstützung des Lösungsvorgangs verwendet werden.

Wirkungsmechanismus (Mechanism of Action)

Targets/IC50/Ki
NF-κB
HSF1
MDM2
In vitro
Triptolide is a diterpene triepoxide with potent immunosuppressive and antiinflammatory properties. This compound is shown to inhibit the expression of IL-2 in activated T cells at the level of purine-box/nuclear factor and NF-κB mediated transcription activation. It inhibits the proliferation and colony formation of tumor cells at extremely low concentrations (2–10 ng/mL). This chemical has an inhibitory activity on breast, stomach and leukemia cell line HL-60 cells. It induces apoptosis in tumor cells by blocking NF-κB activation and sensitizing tumor cells for TNF-&alpha induced programmed cell death.
In vivo
Triptolide synergizes with cyclosporin A in promoting graft survival in animal models and in suppression of graft versus host disease in allogeneic bone marrow transplants. In addition, it induces apoptosis in tumor cells and potentiates tumor necrosis factor (TNF-α) induction of apoptosis in part through the suppression of c-IAP2 and c-IAP1 induction. This compound treatment for 2–3 weeks inhibits the growth of xenografts formed by four different tumor cell lines (B16 melanoma, MDA-435 breast cancer, TSU bladder cancer, and MGC80-3 gastric carcinoma), indicating that TPL has a broad spectrum of activity against tumors that contain both wild-type and mutant forms of p53. In addition, it inhibits experimental metastasis of B16F10 cells to the lungs and spleens of mice. It has in vitro and in vivo activities against mouse models of polycystic kidney disease. LD50: Mice 0.83mg/kg (i.v.).
Referenzen
  • [4] https://pubmed.ncbi.nlm.nih.gov/17360534/
  • [5] https://pubmed.ncbi.nlm.nih.gov/23583804/

Anwendungen (Applications)

Methoden Biomarker Bilder PMID
Western blot c-Jun MDM2 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 p-PI3K / PI3K / p85 / p110
S3604-WB1
22666381
Growth inhibition assay Cell viability
S3604-viability1
22666381