Sulfopin

Chemical Structure : Sulfopin

CAS No.: 2451481-08-4

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货号: PC-22076Not For Human Use, Lab Use Only.

Sulfopin is a potent, selective and covalent inhibitor of Pin1 with Ki of 17 nM in FP assay, targets Pin1's active site Cys113, blocks Myc-driven tumors.

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5 mg	￥980	In stock
10 mg	￥1380	In stock
25 mg	￥2480	In stock
50 mg	￥3980	In stock
100 mg		Get quote

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生物&药学活性

Sulfopin is a potent, selective and covalent inhibitor of Pin1 with Ki of 17 nM in FP assay, targets Pin1's active site Cys113, blocks Myc-driven tumors.
Sulfopin inhibits the catalytic activity of Pin1 with an apparent Ki of 211 nM in chymotrypsin-coupled peptidyl-prolyl isomerization assay.
Sulfopin is highly selective for Pin1 Cys113 over other 161 cysteine residues.
Sulfopin could phenocopy Pin1 knockout.
Sulfopin significantly resensitized HeLa cells to irradiation in a dose-dependent manner, and decreases IRAK1 Thr209 phosphorylation at concentrations as low as 100 nM.
Sulfopin (1 μM) shows a Pin1-dependent viability effect following long-term exposure.
Sulfopin downregulates Myc transcriptional activity and increases c-Myc protein levels in Mino B cells, blocks neuroblastoma in zebrafish.
Sulfopin (20 or 40 mg/kg) inhibits pancreatic cancer progression in mice, significantly extends survival.

物理化学性质&存储条件

分子量	281.80
分子式	C11H20ClNO3S
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-chloro-N-(1,1-dioxidotetrahydrothiophen-3-yl)-N-neopentylacetamide

参考文献

1. Dubiella C, et al. Nat Chem Biol. 2021 Sep;17(9):954-963.

Sulfopin

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