New Small Molecules from MCE for May 2020

BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC₅₀ of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1latency, without T cell activation or toxicity.

Compound Screening Libraries

32 specific libraries for high throughput screening (HTS) and high content screening (HCS). Optimized for drug screening and new indication research.

GS-443902 (GS-441524 triphosphate) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC₅₀s of 1.1 µM, 5 µM for RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir.

Cell Signaling Pathway

YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.

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2. Nature. 2020 Mar;579(7799):433-437.
3. Science. 2020 Feb 14;367(6479):806-810.
4. Cell. 2020 Apr 6. pii: S0092-8674(20)30268-3.
5. Cell. 2020 Mar 5;180(5):941-955.e20.

Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC₅₀=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.

FPL 62064 is a potent 5-lipoxygenase (5-LOX) and COX dual inhibitor, with IC₅₀ values of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and prostaglandin synthetase (cyclooxygenase), respectively. FPL 62064 has potent anti-inflammatory activity.