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UNC 2400
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
UNC 2400图片
CAS NO:1433200-49-7
包装:10mg
市场价:3014元

UNC 2400 与 UNC1999 非常相似，作为细胞研究的阴性对照，其效力比 UNC1999 低 1,000 倍以上。
Cas No.1433200-49-7
化学名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 SMILESCC(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
分子式C35H47N7O2
分子量597.79
溶解度Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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