INH1

Research use only, not for human use.

INH1 is a cell-permeable Hec1 inhibitor that specifically disrupts the Hec1/Nek2 interaction.

INH1 is a cell-permeable Hec1 inhibitor that specifically disrupts the Hec1/Nek2 interaction.

INH1 (25 μM, 24 h) treatment resulted in reduced association of Hec1 with kinetochore and decrease of global Nek2 protein level.INH1 exhibits GI50 values of 10.5 μM (in MDA-MB-468 cells), 15 μM (in SKBR3 cells), 10.5 μM (in T47D cells), 20.5 μM (in MDA-MB-361 cells), 15 μM (in ZR-75-1 cells), 15 μM (in HBL 100 cells), 15.5 μM (in MDA-MB-435 cells), 11 μM (in HS578T cells) and 41 μM (in MCF10A cells), respectively.INH1 (5k) has an IC50 value of 176 nM in the dose-dependent transwell migration assays in MDA-MB-231 cells. INH1 (5k) substantially reduces cellular f-actin and prevented localization of fascin to actin-rich membrane protrusions.INH1 induces abnormal mitotic processes, as well as cell apoptosis. Cell Cytotoxicity AssayCell Line:MCF10A cells.Concentration:10 μM.Incubation Time:12 days.Result:Effectively inhibits the proliferation of human breast cancer lines.Western Blot AnalysisCell Line:MCF10A cells.Concentration:25 μM.Incubation Time:24 h.Result:Nek2 reduction in INH1-treated cells may be independent of Hec1.

INH1 (50 or 100 mg/kg, i.p., every other day/25 cycles) inhibits tumor outgrowth in a xenografted breast cancer model in nude mice. Animal Model:Xenografted nude mice breast cancer model.Dosage:50 or 100 mg/kg.Administration:I.P., every other day/25 cycles.Result:Inhibited tumor growth.

IBT13131

Apoptosis

TNF

Hec1

Cancer

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313553-47-8

308.4

C18H16N2OS

>98% (HPLC)

DMSO : 100 mg/mL 324.25 mM

Cc1cc(C)c(c2csc(NC(=O)c3ccccc3)n2)cc1

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(-20℃)

With Ice Pack

≥ 2 years