Catalog No.S7939 Synonyms: NSC289491, BRN0077366
Molecular Weight(MW): 710.87
Chetomin is an inhibitor of HIF-1 by weaken transcription of HIF-1,disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.
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|Description||Chetomin is an inhibitor of HIF-1 by weaken transcription of HIF-1,disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.|
HIF-1 (hypoxia-inducible factors 1) is transcription factor which respond to changes of cellular environment oxygen. Chetomin selectively inhibits HIF-1 activities through disruption of the interaction of HIF-1 with its transcriptional coactivator p300. HIF-1 inhibition by chetomin effectively reduces hypoxia-dependent transcription and radiosensitizes hypoxic HT 1080 human fibrosarcoma cells in vitro. Chetomin attenuates the hypoxia-induced radioresistance of malignant glioma cell lines U251MG (DMF10: 1.35 and 1.18) and U343MG (DMF10: 1.78 and 1.48). Targeting of HIF-1 using chetomin abolishes the differentiation-inhibitory effect of hypoxia-inducible factor-1α.
|In vivo||Administration of chetomin in combination with forskolin significantly suppresses malignant glioma growth in an in vivo xenograft model . Che-M(chetomin loaded micelles) dramatically inhibits embryonic angiogenesis, tumor-induced angiogenesis and tumor growth in zebrafish. In mouse model, Che-M suppresses tumor growth and prolongs the survival in the subcutaneous CT26 tumor model .|
|In vitro||DMSO||100 mg/mL (140.67 mM)|
|Ethanol||10 mg/mL (14.06 mM)|
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