Chaetocin

Catalog No.S8068

For research use only.

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).

Chaetocin Chemical Structure

CAS No. 28097-03-2

Selleck's Chaetocin has been cited by 8 Publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

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 NXnWSppWS3m2b4TvfIlkcXS7IHHzd4F6 MlrWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{whUUN3MDC9JFAvODJ3IN88UU4> MlW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|MEO3OlcoRjJyM{CzO|Y4RC:jPh?=
Hep3b Ml\xSpVv[3Srb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKEiLRj2xZYxxcGFvbXXkbYF1\WRiVlXHSkBmgHC{ZYPzbY9vKGmwIHj1cYFvKEincEPiJINmdGy|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NEA:KDBwMESg{txONg>? Mn7BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|MEW2NVIoRjJ{M{C1OlEzRC:jPh?=
Hep3b NHy1TllHfW6ldHnvckBie3OjeR?= MYTJcohq[mm2aX;uJI9nKEiLRj2xZYxxcGFvbXXkbYF1\WRiVlXHSkB{\WO{ZYTpc44hcW5iaIXtZY4hUGWyM3KgZ4VtdHNiYomgSWxKW0FuIFnDOVAhRSByLkGg{txONg>? NW\zV4QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzNFU3OTJpPkKyN|A2PjF{PD;hQi=>
Jurkat M3vrbWN6fG:2b4jpZ4l1gSCjc4PhfS=> MVG0NEBpenN? MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDKeZJs[XRiY3XscJMh[W[2ZYKgOFAhcHK|IHLpc4x2dWmwZYPj[Y5k\SCjc4PhfUwhUUN3MDC9JFAvPiEQvF2u M3frWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{CzO|Y4Lz5{MEOwN|c3PzxxYU6=
Drosophila melanogaster SL2 Mke2SpVv[3Srb36gZZN{[Xl? NEWxfIkxNjFidV2= NUHjVYRpPSCmYYnz NEi4SFdKdmirYnn0bY9vKG:oIGPVLHZCWil|LUmgbY4hTHKxc3;wbIlt[SCvZXzhco9o[XO2ZYKgV2wzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDIN2s6dWV{IHH0JFAvOSC3TTDh[pRmeiB3IHThfZMh[nliTVHMSGkuXE:IIF3TJJNm\WSnZDDheEAzNjVibXnscIlwdiClZXzsd{9udCCmZX7zbZR6 MnzqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ2MEiwNVcoRjF4NEC4NFE4RC:jPh?=
Drosophila melanogaster SL2 NXTvNo5mTnWwY4Tpc44h[XO|YYm= M{DX[|AvPSC3TR?= NI\3Vpg2KGSjeYO= NYGwcndYUW6qaXLpeIlwdiCxZjDTWUhXSVJrMz25JIlvKES{b4PvdIhqdGFibXXsZY5w\2G|dHXyJHNNOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gTFNMQW2nMjDheEAxNjVidV2gZYZ1\XJiNTDkZZl{KGK7IF3BUGRKNVSRRjDNV{B{\WWmZXSgZZQhOi53IH3pcIxqd25iY3XscJMwdWxiZHXud4l1gQ>? M2O2UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NEC4NFE4Lz5zNkSwPFAyPzxxYU6=
Drosophila melanogaster SL2 MYXGeY5kfGmxbjDhd5NigQ>? MU[wMlUhfU1? MVrJcohq[mm2aX;uJI9nKFOXKG\BVkk{NTliaX6gSJJwe2:yaHnsZUBu\Wyjbn;nZZN1\XJiU1yyJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCKM1u5cYU{KGG2IECuOUB2VSCkeTDpcY12dm:|dHHpcolv\yCvZYToc4Q> NEXqbXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkSwPFAyPyd-MU[0NFgxOTd:L3G+
HL60 MlryRZBweHSxc3nzJIF{e2G7 NYLjbGRLOzBidV2= M2DGPVQhcHK| NEfLbVBKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhdmWlcn;0bYMh[2WubDDk[YF1cCCjdDCzNEB2VSCjZoTldkA1KGi{czD1d4lv\yCGQWDJM3BKKGK7IHPvcoZw[2GuIHzhd4VzKG2rY4Lvd4NweHliYX7hcJl{cXN? MlHDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4N{WxN|EoRjJyNke1NVMyRC:jPh?=
HL60 NFGw[I1CeG:ydH;zbZMh[XO|YYm= NUHxOZZDOC5|IIXN MnvaOEBpenN? M3e5dmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{BvfWOuZXHyJIZz[WevZX70ZZRqd25iYYSgNE4{KHWPIHHmeIVzKDRiaILzJJV{cW6pIFTBVGkwWEliYomgZ49v\m:lYXygcIF{\XJibXnjdo9{[2:yeTDhcoFtgXOrcx?= NVjuSFdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2O|UyOzFpPkKwOlc2OTNzPD;hQi=>
HL60 M3\PbGFxd3C2b4Ppd{Bie3OjeR?= M{HKR|AvOyC3TR?= MYqyJIhzew>? MY\JcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgZYN1cX[jdHnvckBw\iClYYPwZZNmKDNiYYSgNE4{KHWPIHHmeIVzKDJiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MkPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4N{WxN|EoRjJyNke1NVMyRC:jPh?=
MCF7 MYjGeY5kfGmxbjDhd5NigQ>? M2Tie2lvcGmkaYTpc44hd2ZiaHnzeI9v\S2ueYPpcoUhVi2vZYTofYx1emGwc3\ldoF{\SCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKG2ndHj5cIF1cW:wIH;mJHJCWmKndHGgSG5CKGK7IIHQR3IhdWW2aH;k MnrGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA5QTNzNj:nQmNpTU2ETEyvZV4>
Assay
Methods Test Index PMID
Western blot Procaspase-3 / Cleaved Caspase-3 / PARP 26890137
Growth inhibition assay Cell viability 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 (from reference)

Animal Research:[2]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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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