Stat3 inhibitor H182

Chemical Structure : Stat3 inhibitor H182

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货号: PC-72002Not For Human Use, Lab Use Only.

Stat3 inhibitor H182 is a potent, selective STAT3 inhibitor, inhibits Stat3 DNA-binding activity with IC50 of 0.66 uM.

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生物&药学活性

Stat3 inhibitor H182 is a potent, selective STAT3 inhibitor, inhibits Stat3 DNA-binding activity with IC50 of 0.66 uM.
Stat3 inhibitor H182 shows selective inhibition of Stat3:Stat3 DNA-binding activity, over the inhibition of Stat1:Stat3 (IC50 of 3.4-8.3 μM), with far lower potencies against Stat1:Stat1 (IC50 > 15.8 uM) and Stat5:Stat5 activities (IC50 >19.1 uM).
Stat3 inhibitor H182 irreversibly and covalently binds (KD=1.97 uM, ITC) to Stat3 key residues Cys426 and Cys468.
Stat3 inhibitor H182 inhibits constitutive and ligand-induced Stat3 activation (pY705Stat3) and blocks Stat3 nuclear accumulation with no change in Stat3 protein levels in breast cancer cells, with little or no effects on pS727Stat3, Stat1, JAK2, EGFR, Shc, Erk1/2, Src, or Akt induction.
Stat3 inhibitor H182 inhibited anchorage-dependent and independent growth (MDA-MB-231, IC50=1 uM), induced apoptosis, and suppressed Stat3 target gene expression in TNBC cells harboring constitutively-active Stat3.
Stat3 inhibitor H182 inhibited growth of breast tumors in mice, enhanced response to radiation and prolonged survival.

物理化学性质&存储条件

分子量	647.621
分子式	C30H26F5N5O4S
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	2-Azetidinecarboxamide, N-[(5-cyclohexyl-2-pyridinyl)methyl]-N-(1,2-dihydro-1-oxo-6-phthalazinyl)-1-[(2,3,4,5,6-pentafluorophenyl)sulfonyl]-, (2R)-

参考文献

1. Peibin Yue, et al. Cancer Lett. 2022 Mar 9;534:215613.