HsClpP activator ZK53 | HsClpP activator | Probechem Biochemicals

Chemical Structure : HsClpP activator ZK53

CAS No.: 3031789-26-8

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HsClpP activator ZK53 (ZK53)

货号: PC-21313Not For Human Use, Lab Use Only.

HsClpP activator ZK53 is a potent, selective activator of mitochondrial caseinolytic protease P (HsClpP) with EC50 of 0.22 uM in FI-based protease activity assays, inactive toward bacterial ClpP proteins.

规格	价格	库存
5 mg	￥1180	In stock
10 mg	￥1880	In stock
25 mg	￥2980	In stock
50 mg	￥4880	In stock
100 mg		Get quote

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生物&药学活性

HsClpP activator ZK53 is a potent, selective activator of mitochondrial caseinolytic protease P (HsClpP) with EC50 of 0.22 uM in FI-based protease activity assays, inactive toward bacterial ClpP proteins.
ZK53 selectively binds and stabilizes HsClpP rather than SaClpP in vitro.
ZK53 potently inhibits Lung squamous cell carcinoma (LUSC) cell proliferation with GI50 of 0.5-1 uM, also inhibits cell proliferation in the clonogenic assay and the time-dependent MTT assays, but does not induce cell apoptosis in human lung fibroblast MRC-5 cells.
ZK53 impairs mitochondrial functions and targets HsClpP in LUSC cells, ZK53 triggers a substantial reduction in multiple ETC subunits, including NDUFB8, SDHA, UQCRC2, and COXIV in a dose-dependent manner, also reduces the protein abundances of TFAM, TUFM, and ACO2 in H1703 cells.
ZK53 treatment (1 uM) significantly downregulates the E2F targets in H1703 cells, impairs the essential regulatory pathways for the G1/S transition.
ZK53 activates the ataxia-telangiectasia mutated (ATM)-mediated DNA damage response in H1703 cells.
ZK53 ( 80 mg/kg, dissolved in 40% 2-hydroxypropyl-β-cyclodextrin, i.p. twice a day) exhibits anticancer activity in xenograft and autochthonous mouse models.

物理化学性质&存储条件

分子量	424.29
分子式	C19H20BrF2N3O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(4-bromobenzyl)-4-(3,5-difluorobenzyl)piperazine-1-carboxamide

参考文献

1. Zhou LL, et al. Nat Commun. 2023 Nov 3;14(1):7069.

HsClpP activator ZK53 (ZK53)

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