ARV-825 is a BRD4 Inhibitor based on PROTAC technology.
CAS：1818885-28-7
分子式：C46H47ClN8O9S
分子量：923.43
纯度：98%
存储：Store at -20°C

Background:

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.^[1] ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of BRD4 by the proteasome (50% maximum degradation at < 1 nM).^[1] In Burkitt’s lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis.^[1] The degradation of BRD4 in cells treated with ARV-825 can be blocked with Lenalidomide (CC-5013) (Item No.  ajci14194), a competitor for binding to cereblon.^[2]

参考文献：

[1] Lu, J., Qian, Y., Altieri, M., et al. Hijacking the E3 ubiquitin ligase cereblon to efficiently target BRD4. Chem. Biol. 22(6), 755-763 (2015).

[2]Abruzzese, M.P., Bilotta, M.T., Fionda, C., et al. Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells: role of cMYC-IRF4-miR-125b interplay. J. Hematol. Oncol. 9(1), 134 (2016).