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PhosphoSitePlus® Resource

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Western blot analysis of extracts from HeLa cells, untreated (-) or treated with UNC1999 (2 hr) at the indicated concentrations, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper), Di-Methyl-Histone H3 (Lys27) (D18C8) XP® Rabbit mAb #9728 (middle), and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower).

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Western blot analysis of extracts from HeLa cells, untreated (-) or treated with UNC1999 (5μM) at the indicated time points, using Tri-Methyl-Histone H3 (Lys27) (C36B11) Rabbit mAb #9733 (upper), Di-Methyl-Histone H3 (Lys27) (D18C8) XP® Rabbit mAb #9728 (middle), and Histone H3 (D1H2) XP® Rabbit mAb #4499 (lower).

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Chemical structure of UNC1999

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Product Usage Information

UNC1999 is supplied as a lyophilized powder. For a 5 mM stock, reconstitute the 1 mg in 350.97 μl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used at 5 nM -5 μM for 2-48 hr.


Storage: Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight:

569.8 g/mol


Purity:

>98%


Molecular Formula:

C33H43N7O2


UNC1999 inhibits EZH2 and EZH1 histone-lysine N-methyltransferase activity through competitive inhibition of the cofactor S-Adenosyl-l-methionine (SAM). The UNC1999 inhibitor displays potent specificity relative to other histone methyltransferases. IC50 values for EZH2 and EZH1 are 2 nM and 45 nM, respectively (1). Research studies demonstrate that UNC1999 effectively blocks histone H3 lysine 27 (H3K27) methylation. UNC1999 induces anti-proliferation, cell differentiation, and apoptosis, while exhibiting low cellular toxicity (1,2).


1.  Konze, K.D. et al. (2013) ACS Chem Biol 8, 1324-34.

2.  Xu, B. et al. (2015) Blood 125, 346-57.



For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.

46080
UNC1999