Chaetocin

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Cat.No. 4504 - Chaetocin | C30H28N6O6S4 | CAS No. 28097-03-2
Description: SUV39H1 inhibitor
Chemical Name: (3S,3'S,5aR,5aR,10bR,10'bR,11aS,11'aS)-2,2',3,3',5a,5'a,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10b,10'b(11H,11'H)-bi3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole]-1,1',4,4'-tetrone
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Histone methyltransferase SUV39H1 inhibitor (IC50 = 0.8 μM). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo.

Technical Data

M. Wt 696.84
Formula C30H28N6O6S4
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 28097-03-2
PubChem ID 161591
InChI Key PZPPOCZWRGNKIR-UHFFFAOYSA-N
Smiles CN(C([C@]35N1[C@@]2([H])NC4=C(C=CC=C4)[C@]([C@@]68C(C=CC=C9)=C9N[C@@]([H])6N7[C@@](C8)%10C(N(C)[C@@](CO)(SS%10)C7=O)=O)2C3)=O)[C@@](CO)(SS5)C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 6.97 10

Preparing Stock Solutions

The following data is based on the product molecular weight 696.84. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.44 mL 7.18 mL 14.35 mL
5 mM 0.29 mL 1.44 mL 2.87 mL
10 mM 0.14 mL 0.72 mL 1.44 mL
50 mM 0.03 mL 0.14 mL 0.29 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Isham et al (2007) Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 109 2579 PMID: 17090648

Greiner et al (2005) Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat.Chem.Biol. 1 143 PMID: 16408017

Cherblanc et al (2013) Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases. Nat.Chem.Biol. 9 136 PMID: 23416387

Greiner et al (2013) Reply to "Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases". Nat.Chem.Biol. 9 137 PMID: 23416388


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Keywords: Chaetocin, supplier, histone, lysine, methyltransferase, HMTase, SUV39H1, su(var)3-9, epigenetics, inhibits, inhibitors, antiproliferative, myeloma, selective, G9a, Lysine, Methyltransferases, Tocris Bioscience

Citations for Chaetocin

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