Obatoclax Inhibitor CAS No. 803712-79-0

Cat. No.	Name	Size	Price
KI0216	Obatoclax	5 mg	$217.6
	Obatoclax	10 mg	$409.6
	Obatoclax	50 mg	$1113.6

Chemical Characteristic

Product Name	Obatoclax
Synonyms	GX15- 7
CAS No.	803712-79-0
Molecular Weight	413.49
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
Smiles	[nH]1c(cc2ccccc12)C1=N/C(=C\c2[nH]c(cc2C)C)/C(=C1)OC CS(=O)(=O)O
Chemical Structure

Biological activities

Obatoclax is an inhibitor of Bcl-2 with a K_{i of 220 nM. Obatoclax occupies a hydrophobic pocket within the BH3 binding groove of BCL-2 and antagonizes members of the BCL-2 pro-survival family of proteins. Obatoclax induces apoptosis dependent on BCL2-associated X protein (BAX) and BCL-2 homologous antagonist/killer (BAK). Pretreatment of the mitochondria with 10 nM obatoclax before the addition of cross-linking agent strongly inhibits the formation of MCL-1/BAK dimmers. In SK-Mel5 cells, obatoclax at 1 µM causes a significant reduction in the amount of BAK interacting with MCL-1, with near complete inhibition at 5 µM obatoclax. In a KB oral carcinoma cell line, 0.1 µM obatoclax overcomes MCL-1-mediated resistance to ABT-737, leading to cell death in combination. In the melanoma cell line B16-F1, 50 nM obatoclax overcomes MCL-1-mediated resistance to the proteasome inhibitor bortezomib (either 50 or 500 nM).^[1] Obatoclax markedly reduces the cell viability of esophageal carcinoma cell line EC9706 in a dose-dependent manner with an IC50 value of 3.06 µM. Obatoclax potently inhibits the number of surviving clonogenic EC9706 cells in a dose-dependent manner, with an IC50 value of 1 µM. Obatoclax also significantly inhibits the protein biomass of U2OS cells, with an IC50 value about 146.6 nM. Obatoclax (6 µM) induces the formation of autophagosomes in the cytoplasm when compared to control EC9706 cells. Furthermore, obatoclax increases the mRNA level of Beclin-1 in U2OS cells in a time- and dose-dependent manner.^[2] Obatoclax potently inhibits the viability of 15 of 16 human myeloma cell lines (HMCLs) with mean IC50 value of 246 nM, including those resistant to melphalan and dexamethasone. Five primary multiple myeloma (MM) samples of 14 patient are highly sensitive to obatoclax at doses of 250 and 500 nM with residual plasma cell viability from 5% to 40% of DMSO-treated controls. A further 3 primary MM samples of 14 demonstrates minor cytotoxic responses with a viable cell population of 80% of controls at the 500-nM concentration of obatoclax. Obatoclax has minimal effect on peripheral blood lymphocytes (PBLs) viability at concentrations up to 4 µM. However, continuous exposure to obatoclax significantly suppresses colony formation, affecting erythroid??urst-forming unit (BFU-E), granulocyte macrophage??olony-forming unit (CFU-GM), and granulocyte-erythrocyte-macrophage-megakaryocyte??olony-forming unit (CFU-GEMM) lineages. In a subcutaneous plasmacytoma xenograft mouse model, no significant difference in tumor progression is observed between vehicle or obatoclax-treated (4 mg/kg) mice.^[3] However, in SCID mice bearing human C33A cerivical carcinoma tumors, obatoclax exhibits high antitumor activity at a dose of 0.5 mg/kg. ^[1]}

Protocols

Obatoclax (tartrate or mesylate salts) is prepared as a stock solution in dimethyl sulfoxide (DMSO) .^[1]

References

[1] Nguyen M, et al. Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007, 104(49): 19512-19517. [2] Pan J, et al. The BH3-mimetic GX15-070 induces autophagy, potentiates the cytotoxicity of carboplatin and 5-fluorouracil in esophageal carcinoma cells. Cancer Lett. 2010, 293(2): 167-174. [3] Trudel S, et al. Preclinical studies of the pan-Bcl inhibitor obatoclax (GX015-070) in multiple myeloma. Blood. 2007, 109(12): 5430-5438.

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