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Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon. Obatoclax prevents the interaction of these pro-survival proteins with Bax or Bak, thereby inducing apoptosis with up-regulation of Bim, induced cytochrome c release, and activation of caspase-3. Obstoclax also induces autophagy in mouse embryo fibroblasts and in HeLa cells.This compound inhibits the growth of cancer cell lines and primary cancer isolates. Obatoclax enhances cytarabine-induced apoptosis by enhancing DNA DSBs. This novel mechanism provides compelling evidence for the clinical use of BH3 mimetics in combination with DNA-damaging agents in AML and possibly a broader range of malignancies.
| Molecular Weight | 413.49 |
| Formula | C20H19N3O.CH4O3S |
| CAS Number | 803712-79-0 |
| Solubility (25°C) | DMSO ≥80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Bcl-2 Products |
|---|
| ABT-263
ABT-263 (Navitoclax) is a potent, orally bioavailable inhibitor of the antiapoptotic Bcl-2 family members Bcl-2, Bcl-x (L), and Bcl-w. |
| ABT-737
ABT-737 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, in small cell lung cancer. |
| AT-101
AT-101 (R-(-)-gossypol acetic acid) is a pan small molecule inhibitor of Bcl-2, Bcl-xL, and Mcl-1. |
| ABT-199
ABT-199 (Venetoclax) is a highly potent, orally bioavailable and BCL-2 inhibitor. ABT-199 is the first inhibitor targeting Bcl-2 and PPI. |
| TW-37
TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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