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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-UNC1999
UNC1999

Chemical Structure : UNC1999

CAS No.: 1431612-23-5

UNC1999 (UNC 1999)

货号: PC-21940Not For Human Use, Lab Use Only.

UNC1999 is a potent, selectice SAM-competitive and orally bioavailable inhibitor of EZH2/EZH1 with IC50 of <10 nM/45 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

UNC1999 is a potent, selectice SAM-competitive and orally bioavailable inhibitor of EZH2/EZH1 with IC50 of <10 nM/45 nM, respectively.
UNC1999 is highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets.
UNC1999 potently reduces H3K27me3 levels in cells and selectively killed diffused large B cell lymphoma cell lines harboring the EZH2(Y641N) mutant.
UNC1999 prolongs survival of a well-defined murine leukemia model bearing MLL-AF9.

物理化学性质&存储条件

分子量 569.75
分子式 C33H43N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide

参考文献

1. Grinshtein N, et al. Oncotarget. 2016 Sep 13;7(37):59360-59376.

2. Xu B, et al. Blood. 2015 Jan 8;125(2):346-57.

3. Konze KD, et al. ACS Chem Biol. 2013;8(6):1324-34.

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