WB436B | STAT3 inhibitor | Probechem Biochemicals

Chemical Structure : WB436B

CAS No.: 2248552-84-1

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WB436B (STAT3 inhibitor WB436B)

货号: PC-49462Not For Human Use, Lab Use Only.

WB436B is a potent and highly selective small molecule inhibitor of STAT3, specifically targets the STAT3-SH2 domain with KD value of 94.3 nM.

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5 mg	￥2480	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

WB436B is a potent and highly selective small molecule inhibitor of STAT3, specifically targets the STAT3-SH2 domain with KD value of 94.3 nM.
WB436B directly binds STAT3 SH2 and STAT3127-722 with KD of 94.3 nM and 129.0 nM, respectively, in Microscale Thermophoresis (MST) assays.
WB436B showed no appreciable binding to other STAT members including STAT1, STAT2, STAT4, STAT5B and STAT6 (KD>10 uM), also exhibits a weak inhibition of a panel of human kinases in vitro.
WB436B shows highly sensitivity to high p-STAT3Tyr705 pancreatic cancer cell lines (IC50<100 nM).
WB436B specifically inhibited IFN-α induced p-STAT3Tyr705, but had no significant inhibition against STAT1 phosphorylation.
WB436B selectively blocked p-STAT3Tyr705 at lower than 100 nM in PANC-1 cells, with minimal impact on JAK1, STAT1, STAT5, AKT and ERK1/2 phosphorylation.
WB436B inhibited STAT3 nuclear translocation, and then deceased the binding between STAT3 with its target genes in pancreatic cancer cells.
WB436B (2.5 and 5 mg/kg/d) inhibited tumor growth and STAT3 activities in the preclinical pancreatic cancer xenografts, suppressed p-STAT3Tyr705 and Ki67 expression, inhibited STAT3 phosphorylation and downstream gene expression in vivo.

物理化学性质&存储条件

分子量	436.490
分子式	C21H20N6O3S
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	3-cyano-N-(2-methoxyphenyl)-2-(1-methyl-1H-pyrazole-4-carboxamido)-4,7-dihydrothieno[2,3-c]pyridine-6(5H)-carboxamide

参考文献

1. Huang Chen, et al. Clin Cancer Res. 2022 Nov 14;CCR-22-0997.

WB436B (STAT3 inhibitor WB436B)

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物理化学性质&存储条件

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WB436B (STAT3 inhibitor WB436B)

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