Cas No.: | 1357647-78-9 |
Chemical Name: | BRD-K98645985 |
Synonyms: | BRDK98645985; BRD K98645985; BRD-K98645985 |
SMILES: | O=C(NC1=CC=C(OC[C@H](C)N(CC2=CC=C(C3=NC=CC=C3)C=C2)C[C@H](C)[C@@H](OC)CN(C)C4=O)C4=C1)NC(C)C |
Formula: | C33H43N5O4 |
M.Wt: | 573.73 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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]. |
Target: | BAF transcriptional repression:2.37 μM (EC50) HIV-1 |
In Vitro: | 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]. |
References: | [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. |