Compound 182 | PTP1B/PTPN2 inhibitor | Probechem Biochemicals

Chemical Structure : Compound 182

CAS No.: 2407611-02-1

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Compound 182 (PTP1B/PTPN2 inhibitor XI)

货号: PC-20969Not For Human Use, Lab Use Only.

Compound 182 is a highly potent and selective active site competitive inhibitor of PTP1B and PTPN2, inhibits the catalytic activities of PTP1B and PTPN2 with IC50 of 0.63 and 0.58 nM, respectively.

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5 mg	￥3580	In stock
10 mg	￥5580	In stock
25 mg	￥8980	In stock
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100 mg		Get quote

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生物&药学活性

Compound 182 is a highly potent and selective active site competitive inhibitor of PTP1B and PTPN2, inhibits the catalytic activities of PTP1B and PTPN2 with IC50 of 0.63 and 0.58 nM, respectively.
Compound 182 is a classic competitive inhibitor of PTP1B and PTPN2, with Ki values of 0.34 and 0.26 nM respectively.
Compound 182 inhibits PTP1B and PTPN2 in a reversible manner.
Compound 182 exhibits >15,00-fold selectivity for PTP1B and PTPN2 over other PTP family members with the exception of PTPe, CDC14B and CDC14A for which it is >1,300-, >8,000- and >10,000-fold respectively more selective for PTP1B and PTPN2.
Compound 182 promotes TCR and cytokine signaling in T cells, significantly enhances T cell responses ex vivo.
Compound 182 (10 mg/kg every 2 days or 3 days, i.v.) effectively represses the growth of AT3-OVA syngeneic tumors in C57BL/6 mice without promoting overt immune-related toxicities.
Compound 182 increases both the infiltration and activation of T cells, as well as the recruitment of NK cells and B cells that promote anti-tumor immunity.

物理化学性质&存储条件

分子量	398.41
分子式	C17H19FN2O6S
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	5-(1-fluoro-3-hydroxy-7-(3-hydroxy-3-methylbutoxy)naphthalen-2-yl)-1,2,5-thiadiazolidin-3-one 1,1-dioxide

参考文献

1. Patent WO2019/246513A1

2. Liang S, et al. Nat Commun. 2023 Jul 27;14(1):4524.

Compound 182 (PTP1B/PTPN2 inhibitor XI)

生物&药学活性

物理化学性质&存储条件

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Compound 182 (PTP1B/PTPN2 inhibitor XI)

生物&药学活性

物理化学性质&存储条件

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