BCL-2 family proteins have been studied intensively for their importance in the regulation of apoptosis, tumorigenesis and cellular responses to anti-cancer therapy. BCL-2 family members have classically been grouped into three classes. One class inhibits apoptosis (BCL-2, BCL-XL, BCL-W, MCL1, BCL-B (also known as BCL-2L10) and A1 (also known as BCL-2A1), whereas a second class promotes apoptosis (BAX, BAK and BOK (also known as MTD)). A third divergent class of BH3-only proteins (BAD, BIK (also known as BLK or NBK), BID, HRK (also known as death protein-5 (DP5)), BIM (also known as BOD), BMF, NOXA and PUMA (also known as BBC3)) has a conserved BH3 domain that can bind and regulate the anti-apoptotic BCL-2 proteins to promote apoptosis. Simultaneous over-expression of the anti-apoptotic Bcl-2 and the proto-oncogene myc may produce aggressive B-cell malignancies including lymphoma[1]. ABT-199 (Axon 2141), is a so-called BH3-mimetic drug designed to block the function of the Bcl-2 protein, on patients with chronic lymphocytic leukemia[2].

[1] J.E. Chipuk et al. TheBCL-2 family reunion. Mol Cell. 2010, 37, 299-310.
[2] R.J. Youle, A. Strasser. TheBCL-2 protein family: opposing activities that mediate cell death. Nat. Rev. Mol. Cell Biol. 2008, 9, 47-59.

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Axon ID Name Description From price
2141 ABT 199 Potent, orally bioavailable BCL-2-selective inhibitor €135.00
2185 BAM 7 Selective small-molecule activator of proapoptotic BAX €105.00
1828 BH3I 1 Inhibitor of Bcl-2 family protein €125.00
2007 HA 14-1 Bcl-2 inhibitor and apoptosis inducer of tumor cells €75.00

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