Bfl-1 inhibitor (R,R,S)-26

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Chemical Structure : Bfl-1 inhibitor (R,R,S)-26

Catalog No.: PC-23065Not For Human Use, Lab Use Only.

Bfl-1 inhibitor (R,R,S)-26 is a potent, selective, covalent, cell active Bfl-1 inhibitor with IC50 of 22 nM, shows no activity against Bcl-xl, Bcl-2 and Mcl-1 (IC50>30 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Bfl-1 inhibitor (R,R,S)-26 is a potent, selective, covalent, cell active Bfl-1 inhibitor with IC50 of 22 nM, shows no activity against Bcl-xl, Bcl-2 and Mcl-1 (IC50>30 uM).
(R,R,S)-26 covalently binds to Cys55 of Bfl-1.
(R,R,S)-26 shows EC50 of 0.37 uM for caspase activation in SU-DHL-1 cellular assay monitoring caspase-3/7 activity, and cell viability EC50 of 1.3 uM.
(R,R,S)-26 is a suitable chemical tool that can be used to probe the biology of Bfl-1 with the potential to deliver a more optimal in vivo profile.

Physicochemical Properties

M.Wt	443.47
Formula	C24H24F3N3O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-(((1R,3R)-3-Aminocyclopentyl)oxy)phenyl)-N-((S)-1-(3-cyano-4-(trifluoromethyl)phenyl)ethyl)acrylamide

References

1. Lucas SCC, et al. J Med Chem. 2024 Sep 18. doi: 10.1021/acs.jmedchem.4c01288.

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