Description
Obatoclax (GX15-070) can inhibit bcl-2 with Ki of 220 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C20H19N3O.CH4O3S
Chemical Name
(Z)-2-(5-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-4-methoxy-5H-pyrrol-2-yl)-1H-indole mesylate
Solubility
DMSO 83 mg/mL Water
In vitro
Obatoclax (GX15-070), a small molecule inhibitor, can occupy a hydrophobic pocket within the BH3 binding groove of BCL-2 and induce apoptosis. Obatoclax (GX15-070) potently interfered with the direct interaction between MCL-1 and BAK in intact mitochondrial outer membrane and inhibited the association between MCL-1 and BAK in intact cells. Obatoclax potently induces apoptosis and decreases leukemia cell proliferation. GX15-070 also can inducd autophagy in esophagus cancer cell line EC9706 and osteosarcoma cancer cell line U2OS.
In vivo
Administration of carfilzomib and obatoclax to mice inoculated with SUDHL4 cells substantially suppressed tumor growth, activated JNK, inactivated AKT, and increased survival compared with the effects of single-agent treatment.
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