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Chetomin

Catalog No. T6804   CAS 1403-36-7
Synonyms: Chaetomin, NSC289491, BRN0077366

Chetomin (BRN0077366) 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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Chetomin Chemical Structure
Chetomin, CAS 1403-36-7
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Chetomin (BRN0077366) 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.
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 U251 mg (DMF10: 1.35 and 1.18) and U343 mg (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].
Cell Research 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)
Synonyms Chaetomin, NSC289491, BRN0077366
Molecular Weight 710.87
Formula C31H30N6O6S4
CAS No. 1403-36-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 10 mg/mL (14.06 mM)

H2O: <1 mg/mL

DMSO: 93 mg/mL (130.8 mM)

TargetMolReferences and Literature

1. Staab A,et al. BMC Cancer. 2007, 7:231. 2. Thomas G Smith, et al. Br J Haematol. 2008, 141(3):325–334. 3. Thomas G Smith, et al. BMC Cancer. 2010, 10:605. 4. Lu H, et al. FEBS J. 2009, 276(24):7291-7304. 5. Wu Q, et al. Nanoscale. 2014, 6(20):11940-11952.

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Keywords

Chetomin 1403-36-7 Angiogenesis Apoptosis Chromatin/Epigenetic Cytoskeletal Signaling Metabolism HSP HIF Heat shock proteins targeting nontoxic Chaetomium NSCLC NSC-289491 Chaetomin hypoxia-inducible potent BRN 0077366 non-small BRN-0077366 inhibit globosum NSC 289491 Inhibitor NSC289491 BRN0077366 inhibitor

 

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