Bcl
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.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2141 | ABT 199 | Potent, orally bioavailable BCL-2-selective inhibitor | €70.00 | |
| 3821 | ABT-263 | Potent, selective and orally bioavailable inhibitor of B-cell lymphoma-2 (BCL-2) family proteins | Recently added | Inquire |
| 3814 | AZD4320 | BH3-mimetic inhibitor of BCL-2 protein | Recently added | Inquire |
| 2185 | BAM 7 | Selective small-molecule activator of proapoptotic BAX | €90.00 | |
| 3714 | BCL-201 dihydrochloride | BH3-mimetic inhibitor of BCL-2 protein | Inquire | |
| 1828 | BH3I 1 | Inhibitor of Bcl-2 family protein | €125.00 | |
| 3047 | BI-6C9 | Inhibitor of BID protein | €145.00 | |
| 3295 | BIA | TMBIM6 antagonist | €120.00 | |
| 3431 | BTSA1 | Potent activator of proapoptotic BAX | €110.00 | |
| 3766 | DT-2216 | Selective B-cell lymphoma-extra large (Bcl-XL) targeted protein degrader | Inquire | |
| 2007 | HA 14-1 | Bcl-2 inhibitor and apoptosis inducer of tumor cells | €75.00 | |
| 3079 | NPB | Potent, site-specific Bcl-2-associated death promoter (BAD) inhibitor | €130.00 | |
| 3068 | WEHI-9625 | First-in-class, potent, and selective mBAK-mediated apoptosis inhibitor | €150.00 | |