Chaetocin

For research use only.

Catalog No.S8068

6 publications

Chaetocin Chemical Structure

CAS No. 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. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).

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Selleck's Chaetocin has been cited by 6 publications

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Biological Activity

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. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).
Targets
dSU(VAR)3-9 [1]
()
mouse G9a [1]
()
Neurospora crassa DIM5 [1]
()
0.8 μM 2.5 μM 3 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 MXPDfZRwfG:6aXPpeJkh[XO|YYm= M3zBdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMtKEmFNUCgQUAxNjB{NTFOwG0v NGXuW|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEOwN|c3Pyd-MkCzNFM4Pjd:L3G+
Hep3b MVHGeY5kfGmxbjDhd5NigQ>? MkftTY5pcWKrdHnvckBw\iCKSV[tNYFteGijLX3l[IlifGWmIG\FS2Yh\XiycnXzd4lwdiCrbjDoeY1idiCKZYCzZkBk\WyuczDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVAhRSByLkC0JO69VS5? MlLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MEW2NVIoRjJ{M{C1OlEzRC:jPh?=
Hep3b NYjU[JR{TnWwY4Tpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKEiLRj2xZYxxcGFvbXXkbYF1\WRiVlXHSkB{\WO{ZYTpc44hcW5iaIXtZY4hUGWyM3KgZ4VtdHNiYomgSWxKW0FuIFnDOVAhRSByLkGg{txONg>? NVzydoVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNFU3OTJpPkKyN|A2PjF{PD;hQi=>
Jurkat MoraR5l1d3SxeHnjbZR6KGG|c3H5 MYO0NEBpenN? NGD6fVJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBLfXKtYYSgZ4VtdHNiYX\0[ZIhPDBiaILzJIJqd2y3bXnu[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwNjFOwG0v NGXub2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEOwN|c3Pyd-MkCzNFM4Pjd:L3G+
Drosophila melanogaster SL2 NVLmelBMTnWwY4Tpc44h[XO|YYm= MX:wMlEhfU1? MoruOUBl[Xm| M2H1S2lvcGmkaYTpc44hd2ZiU2WoWmFTMTNvOTDpckBFem:|b4DobYxiKG2nbHHuc4die3SncjDTUFIh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFizT|lu\TJiYYSgNE4yKHWPIHHmeIVzKDViZHH5d{BjgSCPQVzETU1VV0ZiTWOgd4Vm\GWmIHH0JFIvPSCvaXzsbY9vKGOnbHzzM41tKGSnboPpeJk> NF\XS3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkSwPFAyPyd-MU[0NFgxOTd:L3G+
Drosophila melanogaster SL2 MWfGeY5kfGmxbjDhd5NigQ>? NFv6bHYxNjVidV2= M174XFUh\GG7cx?= Mo\pTY5pcWKrdHnvckBw\iCVVTjWRXIqOy17IHnuJGRzd3OxcHjpcIEhdWWuYX7v[4F{fGW{IGPMNkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiSEPLPY1mOiCjdDCwMlUhfU1iYX\0[ZIhPSCmYYnzJIJ6KE2DTFTJMXRQTiCPUzDz[YVl\WRiYYSgNk42KG2rbHzpc44h[2WubIOvcYwh\GWwc3n0fS=> NV3TcHdYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[0NFgxOTdpPkG2OFA5ODF5PD;hQi=>
Drosophila melanogaster SL2 Mo\vSpVv[3Srb36gZZN{[Xl? NHT5TZoxNjVidV2= MWfJcohq[mm2aX;uJI9nKFOXKG\BVkk{NTliaX6gSJJwe2:yaHnsZUBu\Wyjbn;nZZN1\XJiU1yyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCKM1u5cYU{KGG2IECuOUB2VSCkeTDpcY12dm:|dHHpcolv\yCvZYToc4Q> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjRyOECxO{c,OTZ2MEiwNVc9N2F-
HL60 MVjBdI9xfG:|aYOgZZN{[Xl? M4\JZlMxKHWP MlfVOEBpenN? NYrDXYh{UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KG6nY4LveIlkKGOnbHyg[IVifGhiYYSgN|AhfU1iYX\0[ZIhPCCqcoOgeZNqdmdiRFHQTU9RUSCkeTDjc45nd2OjbDDsZZNmeiCvaXPyc5Nkd3C7IHHuZYx6e2m| NFLpUGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[3OVE{OSd-MkC2O|UyOzF:L3G+
HL60 MljoRZBweHSxc3nzJIF{e2G7 NEHHfVkxNjNidV2= Mn;0OEBpenN? MVTJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgcpVkdGWjcjDmdoFodWWwdHH0bY9vKGG2IECuN{B2VSCjZoTldkA1KGi{czD1d4lv\yCGQWDJM3BKKGK7IHPvcoZw[2GuIHzhd4VzKG2rY4Lvd4NweHliYX7hcJl{cXN? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ5NUGzNUc,OjB4N{WxN|E9N2F-
HL60 MoLhRZBweHSxc3nzJIF{e2G7 M{fGd|AvOyC3TR?= MkGzNkBpenN? NGT4WVRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMh[WO2aY\heIlwdiCxZjDjZZNx[XOnIEOgZZQhOC5|IIXNJIFnfGW{IEKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NH;RZnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[3OVE{OSd-MkC2O|UyOzF:L3G+
MCF7 NYPFOGs6TnWwY4Tpc44h[XO|YYm= M3\k[WlvcGmkaYTpc44hd2ZiaHnzeI9v\S2ueYPpcoUhVi2vZYTofYx1emGwc3\ldoF{\SCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKG2ndHj5cIF1cW:wIH;mJHJCWmKndHGgSG5CKGK7IIHQR3IhdWW2aH;k NHnMbpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODh7M{G2M{c,S2iHTVLMQE9iRg>?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Procaspase-3 / Cleaved Caspase-3 / PARP ; 

PubMed: 26890137     


Immunoblotting of procaspase-3, cleaved caspase-3 and PARP from three hepatoma cell lines following different treatment times (a) of chaetocin as indicated. Immunoblotting for β-actin was used as loading control.

26890137
Growth inhibition assay
Cell viability; 

PubMed: 18176557     


Cytotoxicity of mirin in HEK293 cells. HEK293 cells were treated with the indicated concentrations of mirin, then fixed and stained 10 d later (see Methods). Stained plates were counted for colonies. Percentage survival is expressed as the average number of colonies on treated plates divided by the average number of colonies on control plates (0 μM mirin). Each bar represents an average of three independent experiments with s.d. shown.

18176557
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]

Protocol

Animal Research:[2]
- Collapse
  • Animal Models: Hur7 tumor-bearing mice, Hepa 1c1c-7 tumor-bearing mice
  • Dosages: 0.25 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (143.5 mM)
Water Insoluble
Ethanol 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 696.84
Formula

C30H28N6O6S4

CAS No. 28097-03-2
Storage powder
in solvent
Synonyms N/A
Smiles CN1C(=O)C23CC4(C(N2C(=O)C1(SS3)CO)NC5=CC=CC=C54)C67CC89C(=O)N(C(C(=O)N8C6NC1=CC=CC=C71)(SS9)CO)C

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID