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You are here:Home-Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-Kruppel-like Factor (KLF)

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Krüppel-like factor (KLF) family members share a three C2H2 zinc finger DNA binding domain, and are involved in cell proliferation and differentiation control in normal as in pathological situations. KLFs can be deregulated in multiple cancers either by loss of heterozygosity (LOH), somatic mutation or transcriptional silencing by promoter hypermethylation.

KLF family member proteins play a critical role in the growth and metastasis of numerous tumor types, at least in part by regulating the expression of cell cycle genes. Globally, KLF4 and KLF6 are considered as tumor suppressor gene, whereas KLF5 promotes cell proliferation. Family members have different transcriptional properties and can modulate each other's activity by a variety of mechanisms. Since cells can express multiple KLFs, KLF transcription factors build likely a transcriptional network to control cell proliferation. Effects of changes in KLF factors are context-dependent and can appear contradictory, considering differences in the expression profile of family members in various cells. Last, KLF variants may antagonize the function of wild type proteins.

Cat. No. Product Name CAS No. Information
H5853

YD-277

 		2468202-78-8

A novel small molecule KLF5 inhibitor derived from ML264, demonstrates >10-fold enhanced efficacy in multiple cancer cell lines with IC50 of 1.5-10 uM; decreases cancer cell viability in a KLF5-independent manner, induces G1 cell cycle arrest and promotes apoptosis through activating IRE1α in MDA-MB-231 and MDA-MB-468 cells; significantly inhibits the growth of MDA-MB-231 tumor xenografts in nude mice.
H5852

ML-264

 		1550008-55-3

ML-264 (ML 264) is a potent, selective of KLF5 expression inhibtor, withour effect on kinases associated with the KLF5 pathway; inhibits the proliferation of DLD-1 cells with IC50 of 29 nM, and several other KLF5-expressing cell types as well HCT116, IC50 560 nM; HT29, IC50=130 nM; SW620, IC50=430 nM); potently inhibits proliferation of colorectal cancer cells in vitro through modifications of the cell-cycle profile; efficiently inhibits growth of the tumo in an established xenograft mouse model of colon cancer.

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