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