Catalog No.: PC-49079Not For Human Use, Lab Use Only.
Apabetalone (RVX-208) is a potent, selective inhibitor of second BET bromodomains (BD2) with IC50 of 0.51 uM, 170-fold selectivity over BD1 (IC50=87 uM).
Apabetalone (RVX-208) is a potent, selective inhibitor of second BET bromodomains (BD2) with IC50 of 0.51 uM, 170-fold selectivity over BD1 (IC50=87 uM).
Apabetalone (RVX-208) exhibits a KD of 4.06 ± 0.16 μM for BD1 and more than 20-fold stronger binding to BD2 (0.194 ± 0.013 μM) in the case of BRD3.
Apabetalone (RVX-208) displaces BET proteins from chromatin.
Apabetalone (RVX-208) increases the production of ApoA-I in hepatocytes in vitro, and in vivo in monkeys and humans, which results in increased HDL-C through an epigenetic mechanism.
Apabetalone (RVX-208) downregulates expression of cell surface receptors involved in SARS-CoV-2 entry, including angiotensin-converting enzyme 2 (ACE2) and dipeptidyl-peptidase 4 (DPP4 or CD26) in SARS-CoV-2 permissive cells, inhibits SARS-CoV-2 infection in vitro.
