197333

Bcl-2 Inhibitor VI, ABT-737

The Bcl-2 Inhibitor VI, ABT-737, also referenced under CAS 852808-04-9, controls the biological activity of Bcl-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• Synonym(s): Bcl-2 Inhibitor VI, ABT-737, 4-{4-[(4ʹ-Chlorobiphenyl-2-yl)methyl]piperazin-1-yl}-N-{[4-({(1R)-3-(dimethylamino)-1-[(phenylsulfanyl)methyl]propyl}amino)-3-nitrophenyl]sulfonyl}benzamide
• Empirical Formula (Hill Notation): C₄₂H₄₅ClN₆O₅S₂
• CAS Number: 852808-04-9
• Molecular Weight: 813.43
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C42H45ClN6O5S2/c1-46(2)23-22-35(30-55-37-9-4-3-5-10-37)44-40-21-20-38(28-41(40)49(51)52)56(53,54)45-42(50)32-14-18-36(19-15-32)48-26-24-47(25-27-48)29-33-8-6-7-11-39(33)31-12-16-34(43)17-13-31/h3-21,28,35,44H,22-27,29-30H2,1-2H3,(H,45,50)/t35-/m1/s1
• InChI key: HPLNQCPCUACXLM-PGUFJCEWSA-N

Description

General description

A cell-permeable nitrophenylsulfonylbenzamide compound that is shown to bind anti-apoptotic Bcl-2 family members Bcl-2, Bcl-X_L, and Bcl-w with high affinity (K_i ≤ 1 nM) and serves as a nonpeptidyl alternative to Bad-derived BH3 peptide (Cat. No. 197220) in preventing the binding and inhibition of the pro-apoptotic by the anti-apoptotic Bcl-2 family proteins. ABT-737 is demonstrated to fully reverse the blockage of Myr-Bid-induced cytochrome c release by Bcl-2 in mitochondria preparations from Bcl-2 overexpressing FL5.12 cells and effectively inhibit the growth of numerous cancer cells both in cultures in vitro (IC₅₀ ≤100 nM against H146 and H1963) and in vivo (complete regression of H146 and H1963 in xenograft mice at 100 mg/kg/day, i.p.). Application of ABT-737 is also demonstrated to significantly reduce the disease severity in several murine models of autoimmunity. Also available as a 25 mM solution in DMSO (Cat. No. 197334).

A cell-permeable nitrophenylsulfonylbenzamide compound that is shown to bind anti-apoptotic Bcl-2 family members Bcl-2, Bcl-X_L, and Bcl-w with high affinity (K_i ≤1 nM) and serves as a nonpeptidyl alternative to Bad-derived BH3 peptide (Cat. No. 197220) in preventing the binding and inhibition of the pro-apoptotic by the anti-apoptotic Bcl-2 family proteins. ABT-737 is demonstrated to fully reverse the blockage of Myr-Bid-induced cytochrome c release by Bcl-2 in mitochondria preparations from Bcl-2 overexpressing FL5.12 cells and effectively inhibit the growth of numerous cancer cells both in cultures in vitro (IC₅₀ ≤100 nM against H146 and H1963) and in vivo (complete regression of H146 and H1963 in xenograft mice at 100 mg/kg/day, i.p.). Application of ABT-737 is also demonstrated to significantly reduce the disease severity in several murine models of autoimmunity.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Bardwell, P.D., et al. 2009. J. Immunol.182, 7482.
Oltersdorf, T., et al. 2005. Nature435, 677.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable