Chetomin

Catalog No.S7939 Synonyms: NSC289491, BRN0077366

Chetomin Chemical Structure

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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Biological Activity

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.
Targets
HIF-1 [1]
In vitro

HIF-1 (hypoxia-inducible factors 1) is transcription factor which respond to changes of cellular environment oxygen[2]. 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[1]. 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)[3]. Targeting of HIF-1 using chetomin abolishes the differentiation-inhibitory effect of hypoxia-inducible factor-1α[4].

In vivo Administration of chetomin in combination with forskolin significantly suppresses malignant glioma growth in an in vivo xenograft model [4]. 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 [5].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Early-passage HT 1080 human fibrosarcoma cells
  • Concentrations: 150 nM
  • Incubation Time: 16 h
  • Method:

    In RT-PCR and clonogenic survival experiments, chetomin is added in a concentration of 150 nM to fully supplemented medium four hours before treatment with hypoxia. HT 1080 cells are then transferred to the hypoxic workstation (0.1% O2, 12 h) or to the well-humidified incubator (12 hours) without changing medium. HT1080 cells are thus treated for 16 hours with chetomin (150 nM) prior to radiation treatment.


    (Only for Reference)
Animal Research:

[5]

+ Expand
  • Animal Models: Transgenic fish Tg(flk1:EGFP); Mouse model(BALB/c mice)
  • Formulation: Free/ Chetomin loaded micelles
  • Dosages: 1 mg/mL(for zebrafish); 2 mg/kg(for mouse)
  • Administration: s.c.(Mouse Models)
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (140.67 mM)
Ethanol 10 mg/mL (14.06 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 710.87
Formula

C31H30N6O6S4

CAS No. 1403-36-7
Storage powder
Synonyms NSC289491, BRN0077366

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID