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Obatoclax Catalog No : 17022707

Chemical Information

Product NameObatoclax
Iupac Chemical NameObatoclax 
SynonymsObatoclax Mesylate; GX15-070 
Molecular FormulaC₂₁H₂₃N₃O₄S 
Molecular Weight413.49 
SmileCc1cc([nH]c1/C=C\2/C(=CC(=N2)c3cc4ccccc4[nH]3)OC)C.CS(=O)(=O)O
InChiKeyZFKXDVMHNXPEIY-PEZBNFGJSA-N
InChiInChI=1S/C20H19N3O.CH4O3S/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17;1-5(2,3)4/h4-11,21-22H,1-3H3;1H3,(H,2,3,4)/b19-10-;
Cas803712-79-0
MDLMFCD18074508

Technical Data

Appearanceoff-white solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
Quality control

Description

Obatoclax  (GX15-070) is Bcl-2 homology domain-3 (BH3) mimetic, antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L)

Obatoclax is a BH3 mimetic which binds to a broad spectrum of Bcl-2 family members, including Bcl-2, Bcl-xL, and Mcl-1. Obatoclax uniquely displaces BH3 domains by activation of the pocket of Mcl-1 followed by a triggering of apoptosis mediated by oligomerization of Bak and release of cytochrome c. Obatoclax is sensitive to Bcl-xL in cell lines lacking it or showing low expression. It shows low cytotoxicity to Mcl-1, Bcl-2, and Bcl-xL in all the strongly-expressed cell lines. Obatoclax inhibits multiple myeloma (MM) cell lines (KMS12PE, KMS18, MY5, etc.) with IC50 values ranging from 52 to 1100 nM and the inhibition is umimpaired even in the presence of IL-6 or IGF-1, which are resistance to cytotoxic agents, at a concentration of 150 nM. Obatoclax enhances the antimyeloma activity induced by melphalan, dexamethasone, or bortezomib. Obatoclax potentiates TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-mediated apoptosis by unsequestering Bak and Bim from Bcl-2/Bcl-xL or Mcl-1 proteins in PANC-1 and BxPC-3 cells.

 

Chemical Structure

17022707 - Obatoclax | CAS 803712-79-0

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