Sulfopin 是高选择性共价Pin1抑制剂(Ki:17 nM)，在体内能够阻断 Myc 驱动的肿瘤。其中肽基脯氨酰异构酶 Pin1 在癌症中被用来激活癌基因和灭活肿瘤抑制因子。

Sulfopin is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17nM. Sulfopin blocks Myc-driven tumors in vivo.

Sulfopin (2μM, HEK293 cells, 48 hours) downregulates Myc transcription. Sulfopin (1μM, 2.5μM, PATU-8988T cells, 4 days) shows a significant reduction in the member of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells.[1]

Sulfopin (40mg/kg, p.o., bis in die/qualer in die for 7 days) regresses neuroblastoma in mice. Sulfopin (20-40mg/kg, i.p., daily for days) inhibits pancreatic cancer progression in mice.[1]

2451481-08-4

C11H20ClNO3S

281.8

Acetamide, 2-chloro-N-(2,2-dimethylpropyl)-N-(tetrahydro-1,1-dioxido-3-thienyl)-;sulfopin

DMSO:90 mg/mL (319.38 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years