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Chemical Structure| 28097-03-2 Chemical Structure| 28097-03-2

Structure of Chaetocin
CAS No.: 28097-03-2

Chemical Structure| 28097-03-2

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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. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.

Synonyms: Chaetocin

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Product Details of Chaetocin

CAS No. :28097-03-2
Formula : C30H28N6O6S4
M.W : 696.84
SMILES Code : O=C([C@@](N1C)(SS2)CO)N3[C@](NC4=CC=CC=C54)([H])[C@]5([C@@]6(C7=CC=CC=C7N8)[C@@]8([H])N(C9=O)[C@](C%10=O)(SS[C@]9(CO)N%10C)C6)C[C@]32C1=O
Synonyms :
Chaetocin
MDL No. :MFCD00133163

Safety of Chaetocin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P301+P312+P330

Related Pathways of Chaetocin

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
PC3 human prostate cancer cells 5 nM and 100 nM 18 hours Chaetocin treatment inhibited HIF-1α expression, indicating its suppression of HIF-1α transcriptional activity by disrupting the HIF-1α/p300 complex. PMC4113146
PANC10.05 cells 50 nM 2 days Chaetocin significantly decreased the H3K4me3 level in the CD274 promoter region and remarkably reduced the PD-L1 protein level. PMC5291187
DDLPS cell lines 30-40 nM 24 hours Inhibited DDLPS cell proliferation, decreased H3K9me3 levels, and increased KLF6 expression PMC4563740
DIPG cells 25 nM 24 hours Chaetocin significantly reduced the proliferation of DIPG cells and increased apoptosis. PMC10995509
Normal human astrocytes (NHA) 25 nM 24 hours Chaetocin treatment did not induce apoptosis in NHAs. PMC10995509
E6 cells 10 nM 24 hours Inhibits histone methyltransferases, alleviating shRNA-mediated transcriptional silencing effect PMC5651755
HL-60 cells 20 nM 48 hours Induced differentiation, upregulated CD11b expression, reduced SUV39H1 and G9a expression PMC4476016
KG-1a cells 20 nM 48 hours Induced differentiation, upregulated CD11b expression, reduced SUV39H1 and G9a expression PMC4476016
U937 cells 20 nM 48 hours Upregulated CD11b expression but no significant differentiation observed PMC4476016
Human neural stem cells (hNSC) 25 nM 72 hours Chaetocin treatment did not significantly affect the growth of hNSCs. PMC10995509

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male Fox Chase SCID Beige Mice Prostate cancer xenograft model Intraperitoneal injection 0.25 mg/kg Once daily for 15 days Chaetocin significantly inhibited tumor growth, demonstrating its antitumor activity in vivo. PMC4113146
C57/BL6 mice myocardial infarction model intraperitoneal injection 25 mg/kg 2 days prior to the LAD procedure To investigate the protective effects of Chaetocin on myocardial infarction, results showed that Chaetocin significantly improved the survival rate of mice, reduced infarct size, and improved heart function. PMC5381011
NSG mice DIPG xenograft model Intraperitoneal injection 0.5 mg/kg Every other day, continuous treatment Chaetocin treatment significantly inhibited the growth of DIPG tumor cells and prolonged the survival of mice. PMC10995509

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.44mL

0.29mL

0.14mL

7.18mL

1.44mL

0.72mL

14.35mL

2.87mL

1.44mL

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