2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. KLF

KLF

Krüppel-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 Effect Purity Chemical Structure
  • HY-16291
    APTO-253
    		Activator 99.74%
    APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity.
    APTO-253
  • HY-19994
    ML264
    		Inhibitor 98.32%
    ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.
    ML264
  • HY-136530
    SR18662
    		Inhibitor 99.61%
    SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer.
    SR18662
  • HY-N1570
    Pterosin B
    		Inhibitor 99.98%
    Pterosin B is an orally active indanone. Pterosin B can be obtained from Pteridium aquilinum. Pterosin B is a Sik3 signaling inhibitor. Pterosin B inhibits Klf5 expression and reduces β-amyloid deposition. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice. Pterosin B inhibits cardiomyocyte hypertrophy, improves cognitive impairment, and lowers blood glucose. Pterosin B can be used in research on arthritis, Alzheimer's disease, pathological cardiac hypertrophy and diabetes.
    Pterosin B
  • HY-139691
    SR15006
    		Inhibitor 99.90%
    SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells).
    SR15006
  • HY-182820
    YZ-836P
    		Inhibitor
    YZ-836P is a Protein arginine methyltransferase 5 (PRMT5) targeting agent. YZ-836P promotes ubiquitination and proteasomal degradation of PRMT5 in a cereblon (CRBN)-dependent manner, which in turn reduces levels of its downstream target KLF5. YZ-836P induces G1 phase cell cycle arrest in triple-negative breast cancer cells. YZ-836P induces Apoptosis in triple-negative breast cancer cells. YZ-836P exerts cytotoxic effects on triple-negative breast cancer cells. YZ-836P inhibits the growth of triple-negative breast cancer patient-derived organoids. YZ-836P inhibits the growth of triple-negative breast cancer xenografts in nude mice. YZ-836P can be used for the research of triple-negative breast cancer.
    YZ-836P
  • HY-W072962
    WX2-43
    		Inhibitor 98.74%
    WX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer.
    WX2-43
  • HY-N18377
    Moldapyranone A
    		Activator
    Moldapyranone A (formula I) is a pyrone compound with a significant effect on up-regulating the expression of KLF2. Moldapyranone A can be used for the study of cardiovascular disease or anti-inflammatory.
    Moldapyranone A
  • HY-W011044
    CID 5951923
    		Inhibitor 98.87%
    CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
    CID 5951923
  • HY-178143
    Sp1-IN-1
    		Inhibitor
    Sp1-IN-1 is a selective specificity protein 1 (Sp1) inhibitor. Sp1-IN-1 inhibits the proliferation of Hela cells and MCF-7 cells. Sp1-IN-1 can be used to the studies of cervical cancer and breast cancer.
    Sp1-IN-1
  • HY-169213
    LN-439A
    		Inhibitor
    LN-439A (compound LN-439A) is a BAP1 inhibitor that inhibits the growth of basal-like breast cancer by degrading KLF5..
    LN-439A
  • HY-N1570R
    Pterosin B (Standard)
    		Inhibitor
    Pterosin B (Standard) is the analytical standard of Pterosin B (HY-N1570). This product is intended for research and analytical applications. Pterosin B is an indanone. Pterosin B can be obtained from Pteridium aquilinum. Pterosin B is a Sik3 signaling inhibitor. Pterosin B inhibits Klf5 expression and reduces β-amyloid deposition. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice. Pterosin B inhibits cardiomyocyte hypertrophy, improves cognitive impairment, and lowers blood glucose. Pterosin B can be used in research on arthritis, Alzheimer's disease, pathological cardiac hypertrophy and diabetes.
    Pterosin B (Standard)
Cat. No. Product Name / Synonyms Application Reactivity