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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-SGC0946
SGC0946

Chemical Structure : SGC0946

CAS No.: 1561178-17-3

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SGC0946 (SGC-0946)

货号: PC-49325Not For Human Use, Lab Use Only.

SGC0946 (SGC-0946) is a potent, selective inhibitor of protein methyltransferase DOT1L with KD value of 0.06 nM and IC50 of 0.3 nM, reduces the level of methylation of H3K79 in MCF10A cells with IC50 of 8.8 nM.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2680 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SGC0946 (SGC-0946) is a potent, selective inhibitor of protein methyltransferase DOT1L with KD value of 0.06 nM and IC50 of 0.3 nM, reduces the level of methylation of H3K79 in MCF10A cells with IC50 of 8.8 nM.
SGC0946 is inactive against a panel of 12 protein methyltransferases (PMTs), DNMT1 and PRMT5. SGC0946 is more potent than EPZ004777.
SGC0946 reduced H3K79 methylation and proliferation of MYCN gene-amplified neuroblastoma cells.
SGC0946 displayed selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells transformed with the MLL-AF9 fusion oncogene, without apparent effect on the viability of cells transformed with an MLL-unrelated translocation (TLS-ERG).
SGC0946 (1 μM) effectively lowered the levels of MLL target genes, HOXA9 and Meis1.

物理化学性质&存储条件

分子量 618.577
分子式 C28H40BrN7O4
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-(3-((((2R,3S,4R,5R)-5-(4-amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea

参考文献

1. Yu W, et al. Nat Commun. 2012;3:1288.

2. Wong M, et al. Cancer Res. 2017 May 1;77(9):2522-2533.

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