General description
A cell-permeable diazepinyl-quinazolinamine, non-SAM (S-adenosylmethionine) analog-based HMTase (histone methyltransferase) inhibitor that selectively interferes with the G9a-catalyzed H3K9me2 (histone H3 Lys9 dimethylation) modification (IC50 = 1.7 µM) in a reversible manner. It inhibits the GLP-catalyzed H3K9me3 only at much higher concentrartions (IC50 = 38 µM) and exhibits little activity against H3 methylations catalyzed by other HMTases (PRMT1, SET7/9, ESET, SUV39H1). Shown to effectively synergize with Oct3/4 and Klf4 in inducing reprogramming of primary murine fetal NPCs (Neural Progenitor Cells) into iPS (induced Pluripotent Stem) cells without additional viral transduction of Sox2 and c-Myc.
Packaging
Packaged under inert gas
Other Notes
Shi, Y., et al. 2008. Cell Stem Cell2, 525.
Kubicek, S., et al. 2007. Mol. Cell25, 473.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | DMSO: 10 mg/mL,ethanol: 10 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | N2(CCC(CC2)Nc3nc(nc5c3cc(c(c5)OC)OC)N4CCN(CCC4)C)Cc1ccccc1 |
| InChI | 1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31) |
| InChI key | OSXFATOLZGZLSK-UHFFFAOYSA-N |
