Bcl Family Set I

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Background

A DMSO solution containing 25 μl (10 mM) each of the following inhibitors: A8193 ABT-737, A3935 WEHI-539, A4234 TW-37, and A3007 ABT-263 (Navitoclax) ABT-737 is a BH3 mimetic inhibitor of Bcl-xL (EC50=78.7 nM), Bcl-2 (EC50=30.3 nM) and Bcl-w (EC50=197.8 nM), respectively. There is no inhibition observed against Mcl-1, Bcl-B and Bfl-1. WEHI-539, has high affinity (subnanomolar) and selectivity for and potently kills cells by selectively antagonizing the prosurvival activity of BCL-XL (IC50 = 1.1 nM). TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2 (ki=0.29 μM), Bcl-xL (ki=1.11 μM) and Mcl-1 (ki=0.26 μM), respectively. ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM.

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[2] Lessene G, Czabotar P E, Sleebs B E, et al. Structure-guided design of a selective BCL-XL inhibitor. Nature chemical biology, 2013, 9(6): 390-397.
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[4] Mérino D1, Khaw SL, Glaser SP et al. Bcl-2, Bcl-x(L), and Bcl-w are not equivalent targets of ABT-737 and navitoclax (ABT-263) in lymphoid and leukemic cells.Blood. 2012 Jun 14;119(24):5807-16.