BRD-K98645985

BRD-K98645985 is a class of 12-membered macrolactam and a BAF (Brg/Brahma-associated factors) transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, and without T cell activation or toxicity[1].

Signaling Pathways >> Anti-infection >> HIV

Research Areas >> Infection

BAF transcriptional repression:2.37 μM (EC50)

HIV-1

BRD-K98645985 (30 µM; 18 hours) treatment shows a 5-fold increase in Bmi1, 2.6-fold increase in Ring1, and 3.3-fold decrease in Fgf4[1]. BRD-K98645985 treatment shows a concentration dependent latency reversal in J-Lat T-cell line models. BRD-K98645985 can be combined with other LRAs to improve reservoir targeting[1].

[1]. Marian CA, et al. Small Molecule Targeting of Specific BAF (mSWI/SNF) Complexes for HIV Latency Reversal. Cell Chem Biol. 2018 Dec 20;25(12):1443-1455.e14.