ZH97 | BFL-1 inhibitor | Probechem Biochemicals

Chemical Structure : ZH97

ZH97 (BFL-1 selective inhibitor)

Catalog No.: PC-73235Not For Human Use, Lab Use Only.

ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.

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Biological Activity

ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.
ZH97 does not bind to BCL-xL, BCL-2, TEAD2, TEAD4, MDM2, MDMX, BRD2 BD1, BRD2 BD2, BRD3 BD1, BRD3 BD2, BCL9, PD1/PD-L1 (Ki>400 uM).
ZH97 modifies BFL-1 at the C55 residue, blocks BFL-1/BID interaction in vitro.
ZH97 dose-dependently increased cytoplasmic cytochrome c level in U937 cells, has cell growth inhibition with IC50 of 2.8 uM, 5.5 uM, 7.7 uM, 6.8 uM, and 3.9 uM in U937, Kasumi-1, K562, MM.1S, and MV4-11 cell lines, respectively.
ZH97 inhibits BFL-1/PUMA interaction in cell lysate and is effective in cancer cells that harboring high
expression level of BFL-1.

Physicochemical Properties

M.Wt	440.522
Formula	C27H25FN4O
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
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(4-(2-benzyl-6-(3-fluorophenyl)-2H-indazol-3-yl)piperazin-1-yl)prop-2-en-1-one

References

1. Xuexin Feng, et al. European Journal of Medicinal Chemistry 236 (2022) 114327

2. Karson J Kump, et al. J Med Chem. 2020 Mar 12;63(5):2489-2510.

ZH97 (BFL-1 selective inhibitor)

Biological Activity

Physicochemical Properties

References

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