UNC 2400

Short Summary : negative control of UNC1999

Category : Chromatin/Epigenetics|Histone Methyltransferase

Purity : 0.98

CAS Number : 1433200-49-7

Formula : C35H47N7O2

Molecular Weight :

Molecular Weight : 597.79

SMILE : CC(C)N1CCN(C2=NC=C(C3=CC(N(C(C)C)N=C4)=C4C(C(N(C)CC5=C(CCC)C=C(C)N(C)C5=O)=O)=C3)C=C2)CC1

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1 [1].
Histone-lysine N-methyltransferase (EZH1 or EZH2) is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a transcriptionally repressive post-translational modification. Hypertrimethylation of H3K27 and overexpression of EZH2 are involved in cancers [1].
UNC 2400 is a negative control of UNC1999. UNC 2400 inhibited EZH2 with IC50 value of 13 M and exhibited >1,000-fold less potency than UNC1999. Also, UNC 2400 inhibited EZH1 and EZH2 Y641F with IC50 values of 62 and >200 M, respectively. In MCF10A cells, UNC 2400 exhibited little inhibition of H3K27me3 levels and had low cellular toxicity with EC50 value of 27.5 M that was similar to UNC1999. In DB cells, UNC 2400 (3 M) did not significantly inhibit DB cell proliferation and had no influence on H3K27me3 or EZH2 levels [1].
Reference:[1]. Konze KD, Ma A, Li F, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol, 2013, 8(6): 1324-1334.

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