A selective inhibitor of KLF5 (IC50 = 29 nM in a cell-based assay for proliferation of KLF5-expressing DLD-1 cells); induces death in most colon cancer cell lines (HCT116

ML-264 – 10 mg

Brand:
Cayman
CAS:
1550008-55-3
Storage:
-20
UN-No:
Non-Hazardous - /

ML-264 is a selective inhibitor of Krüppel-like factor 5 (KLF5), a zinc finger-containing transcription factor that is highly expressed in rapidly dividing intestinal epithelial cells. It displays an IC50 value of 29 nM in a cell-based assay for proliferation of KLF5-expressing DLD-1 cells and an IC50 value of 81 nM in a cell-based luciferase assay but does not inhibit kinases associated with the KLF5 pathway, as determined using a panel of 47 selected kinases.{32740} ML-264 induces death in most colon cancer cell lines (HCT116, IC50 = 560 nM; HT-29, IC50 = 130 nM; SW620, IC50 = 430 nM), with cytotoxicity toward an established xenograft mouse model of colon cancer as well.{32740,32741}  

 

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Description

A selective inhibitor of KLF5 (IC50 = 29 nM in a cell-based assay for proliferation of KLF5-expressing DLD-1 cells); induces death in most colon cancer cell lines (HCT116, IC50 = 560 nM; HT-29, IC50 = 130 nM; SW620, IC50 = 430 nM)

Formal name: (2E)-3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-2-propenamide

Synonyms: 

Molecular weight: 384.9

CAS: 1550008-55-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death||Research Area|Cancer|Transcription Factors||Research Area|Cell Biology|Cell Cycle||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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