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MedKoo product information:
Description of UNC-0638: UNC0638 is an inhibitor of
G9a and GLP with excellent potency and selectivity over a wide range
of epigenetic and non-epigenetic targets. UNC0638 treatment of a
variety of cell lines resulted in lower global H3K9me2 levels,
equivalent to levels observed for small hairpin RNA knockdown of G9a
and GLP with the functional potency of UNC0638 being well separated
from its toxicity. UNC0638 markedly reduced the clonogenicity of
MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of
known G9a-regulated endogenous genes and disproportionately affected
several genomic loci encoding microRNAs. In mouse embryonic stem
cells, UNC0638 reactivated G9a-silenced genes and a retroviral
reporter gene in a concentration-dependent manner without promoting
Nat Chem Biol. ; 7(8): 566–574. doi:10.1038/nchembio.599.).
Current developer: University of North Carolina at
MedKoo Code#: 4
MedKoo Code#: 504910
Chemical Formula: C30H47N5O2
Exact Mass: 509.37
Molecular Weight: 509.72648 Elemental
Analysis: C, 70.69; H, 9.29; N, 13.74; O, 6.28
Availability and price:
(purity >98%) is in stock, price updated: 10/23/2012.
10 mg / $155.00, in stock
20 mg / $195.00, in stock
50 mg / $495.00, in stock
100 mg / $750.00, in stock
200 mg / $1,250.00, in stock
Grams in stock, please ask for price
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Information about this agent
UNC0638 was a potent G9a (IC50 < 15 nM (n = 4)) and
GLP inhibitor (IC50 = 19 ± 1 nM (n = 2)) in these SAHH-coupled assays
(Table 1). An endoproteinase-coupled microfluidic capillary
electrophoresis (MCE) assay, which is orthogonal and complementary to
the SAHH-coupled assay, was also used to evaluate G9a inhibition by
UNC0638, yielding an IC50 < 10 nM (n = 3). In addition, UNC0638
a fluorescein-labeled 15-mer H3 peptide (residues 1–15) with high
efficiency in a G9a fluorescence-polarization assay, suggesting that
UNC0638 binds in the substrate peptidebinding site of G9a. UNC0638 also
stabilized G9a and GLP in differential scanning fluorimetry (DSF)
experiments, with Tm shifts of 4 °C and 8 °C, respectively, consistent
with high-affinity binding.
1: Machleidt T, Robers MB, Hermanson SB, Dudek JM, Bi
K. TR-FRET cellular assays for interrogating posttranslational
modifications of histone H3. J Biomol Screen. 2011 Dec;16(10):1236-46.
Epub 2011 Oct 4. PubMed PMID: 21972037.
2: Hauser AT, Jung M. Chemical probes: sharpen your epigenetic tools.
Nat Chem Biol. 2011 Jul 18;7(8):499-500. doi: 10.1038/nchembio.615.
PubMed PMID: 21769094.
3: Vedadi M, Barsyte-Lovejoy D, Liu F, Rival-Gervier S, Allali-Hassani
A, Labrie V, Wigle TJ, Dimaggio PA, Wasney GA, Siarheyeva A, Dong A,
Tempel W, Wang SC, Chen X, Chau I, Mangano TJ, Huang XP, Simpson CD,
Pattenden SG, Norris JL, Kireev DB, Tripathy A, Edwards A, Roth BL,
Janzen WP, Garcia BA, Petronis A, Ellis J, Brown PJ, Frye SV, Arrowsmith
CH, Jin J. A chemical probe selectively inhibits G9a and GLP
methyltransferase activity in cells. Nat Chem Biol. 2011 Jul
10;7(8):566-74. doi: 10.1038/nchembio.599. Erratum in: Nat Chem Biol.
2011 Sep;7(9):648. Nat Chem Biol. 2011;7(8):following 574. PubMed PMID:
21743462; PubMed Central PMCID: PMC3184254.
(Keyword; CAS#; MedKoo code#)