Sulfopin_product_DataBase

Bioactivity

Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors[1].

Invitro

MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days)[1].Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription[1].Sulfopin (1, 2.5 μM; PATU-8988T cells; 4 days) shows a small but significant reduction in the number of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells[1]. Cell Proliferation Assay[1] Cell Line:

In Vivo

Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice[1].Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice[1].Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish[1]. Animal Model:

Name

Sulfopin

CAS

2451481-08-4

Formula

C11H20ClNO3S

Molar Mass

281.80

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Dubiella C, et al. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021;17(9):954-963.

PeptideDB

Sulfopin

CAS: 2451481-08-4 F: C11H20ClNO3S W: 281.80