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Chaetocin

Catalog No. T6803   CAS 28097-03-2

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.

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Chaetocin Chemical Structure
Chaetocin, CAS 28097-03-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 133.00
5 mg In stock $ 398.00
10 mg In stock $ 592.00
25 mg In stock $ 947.00
50 mg In stock $ 1,280.00
1 mL * 10 mM (in DMSO) In stock $ 529.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.
Targets&IC50 DIM5 (neurospora crassa):3 μM, G9a (mouse):2.5 μM, dSU(VAR)3-9:0.8 μM
In vitro In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. [1] In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. [2] Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM. [3]
In vivo In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. [2] In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities. [3]
Cell Research HeLa cells are transfected with 1 μg pcDNA or pcDNA-Trx. Twenty four h after transfection the cells are treated with either DMSO, 100 nM chaetocin or 100 nM doxorubicin for 24 h. The cells are then trypsinized and manually counted in trypan blue to exclude dead cells. For immunoblotting (24 h after transfections), cells are trypsinized, ished in cold PBS, and lysed in CelLytic lysis buffer containing protease inhibitors. Protein is analyzed by BCA assay and lysates are electrophoresed on 15% SDS-PAGE gels and transferred to nitrocellulose. Immunoblotting for thioredoxin and actin is then performed[2].
Molecular Weight 696.84
Formula C30H28N6O6S4
CAS No. 28097-03-2

Storage

store at low temperature

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 7 mg/mL (10 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Greiner D, et al. Nat Chem Biol. 2005, 1(3), 143-145. 2. Lee YM, et al. Hepatology. 2011, 53(1), 171-180. 3. Isham CR, et al. Br J Cancer. 2012, 106(2), 314-323.

Related compound libraries

This product is contained In the following compound libraries:
Microbial Natural Product Library Epigenetics Compound Library Natural Product Library for HTS

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CPI-360 BML-278 WDR5-47 MS0124 Cyproheptadine hydrochloride sesquihydrate BRD9539 SGC-iMLLT CARM1 degrader-2

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Keywords

Chaetocin 28097-03-2 Chromatin/Epigenetic Microbiology/Virology Antibiotic Antibacterial Histone Methyltransferase Inhibitor inhibit Bacterial inhibitor

 

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