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UNC 2400 negative control of UNC1999

Catalog No.B4948
Size Price Stock Qty
10mg
$250.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

UNC 2400

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Chemical Properties

Cas No. 1433200-49-7 SDF Download SDF
Chemical Name N-((1,6-dimethyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-methyl-1H-indazole-4-carboxamide
Canonical SMILES 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
Formula C35H47N7O2 M.Wt 597.79
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance Off White solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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 µM and exhibited >1,000-fold less potency than UNC1999. Also, UNC 2400 inhibited EZH1 and EZH2 Y641F with IC50 values of 62 and >200 µM, respectively. In MCF10A cells, UNC 2400 exhibited little inhibition of H3K27me3 levels and had low cellular toxicity with EC50 value of 27.5 µM that was similar to UNC1999. In DB cells, UNC 2400 (3 µM) 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.