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UNC 0638

Cat. No. 4343

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Chemical Name: 2-Cyclohexyl-6-methoxy-N-[1-(1-methylethyl)-4-piperidinyl]-7-[3-(1-pyrrolidinyl)propoxy]-4-quinazolinamine

Biological Activity

Selective inhibitor of G9a and GLP histone lysine methyltransferases (IC₅₀ values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a range of other histone methyltransferases). Potently inhibits dimethylation of H3K9 in MCF-7 cells (IC₅₀ = 70 nM). Cell permeable.

Structural Genomics Consortium (SGC) Collaboration

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the UNC 0638 probe summary on the SGC website.

Technical Data

M.Wt:

509.73

Formula:

C₃₀H₄₇N₅O₂

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol and to 100 mM in 1eq. HCl

Purity:

>99 %

Storage:

Store at +4°C

CAS No:

1255517-77-1

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

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

Liu et al (2011) Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J.Med.Chem. 54 6139. PMID: 21780790.

Vedadi et al (2011) A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat.Chem.Biol. 7 566. PMID: 21743462.

If you know of a relevant citation for this product please let us know.

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Keywords: UNC 0638, supplier, G9a, GLP, histone, lysine, methyltransferases, HMTs, HMTases, epigenetics, histone, modifications, H3K9, H3K9me2, potent, selective, inhibits, inhibitors, UNC0638