[CAS NO. 173932-75-7] Gambogenic acid
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PRODUCTS SPECIFICATIONS [173932-75-7]
Catalog
SLK-S9031
Brand
Selleck
CAS
173932-75-7
DESCRIPTION [173932-75-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 630.77 |
| Molecular Formula | C38H46O8 |
| SMILES | - |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5854 mL | 7.9268 mL | 15.8536 mL |
| 5 mM | 0.3171 mL | 1.5854 mL | 3.1707 mL |
| 10 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL |
| 50 mM | 0.0317 mL | 0.1585 mL | 0.3171 mL |
Description
Gambogenic Acid, identified from Gamboge, is an inhibitor of the signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
In vitro
Gambogenic acid as a novel agent that specifically and covalently bound to Cys668 within the EZH2‐SET domain, triggers EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination. Gambogenic acid significantly suppresses H3K27Me3 and effectively reactivated polycomb repressor complex 2 (PRC2)‐silenced tumor suppressor genes. Gambogenic acid significantly suppresses tumor growth in an EZH2‐dependent manner.
References
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