化合物 SGC0946|T3082|TargetMol

SGC0946
1561178-17-3

￥432 2mg 起订

￥778 5mg 起订

￥1258 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 SGC0946

英文名称：: SGC0946

CAS号：: 1561178-17-3

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.82%

产品类别：: 抑制剂

货号：: T3082

Product Introduction

Bioactivity

Name	SGC0946
Description	SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
Kinase Assay	Determination of Inhibitor IC50 Values: EPZ004777 is serially diluted 3-fold in DMSO for a total of ten concentrations, beginning at 1 mM. A 1 μL aliquot of each inhibitor dilution is plated in a 384-well microtiter plate. The 100% inhibition control consisted of 2.5 mM ?nal concentration of the product inhibitor S-adenosyl-L-homocysteine, (SAH). Compound is incubated for 30 min with 40 ml per well of 0.25 nM DOT1L(1-416) in assay buffer (20 mM TRIS [pH 8.0] 10 mM NaCl, 0.002% Tween 20, 0.005% Bovine Skin Gelatin, 100 mM KCl, and 0.5 mM DTT). 10 ml per well of substrate mix comprising assay buffer with 200 nM 3H-SAM (American Radiolabeled Chemicals: 80 Ci/mmol), 600 nM unlabeled SAM, and 20 nM nucleosomes are added to initiate the reaction (both substrates are present in the ?nal reaction mixture at their respective KM values). Reactions are incubated for 120 min and quenched with 10 ml per well of 800 mM SAM. Incorporation of radioactivity into nucleosome substrate is measured in a ?ashplate. IC50 values for enzymes in the histone methyltransferase panel are determined under similar balanced assay conditions with both SAM and protein/peptide substrate present at concentrations equal to their respective KM values.
In vivo	SGC 0946可使A431细胞（IC50：2.6 nM）和MCF10A细胞（IC50：8.8 nM）中H3K79二甲基化显著降低,并可有效并选择性地杀死含MLL易位的细胞。与其类似物EPZ004777相比,SGC 0946对DOT1L更有效,从而用于癌症治疗的研究中。SGC 0946比其他组蛋白甲基转移酶/HMTs选择性高100倍。
Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 93 mg/mL (150.3 mM) Ethanol : 93 mg/mL (150.3 mM)
Keywords	Inhibitor \| inhibit \| Histone Methyltransferase \| Molm13 MLL \| MLL-rearrange \| leukemia \| cord blood cells \| SGC-0946 \| SGC 0946 \| ovarian cancer \| TOV21G \| SGC0946
Inhibitors Related	Tazemetostat hydrobromide \| XY1 \| BML-278 \| MRTX-1719 \| MAK683 \| GSK126 \| Tazemetostat \| EPZ015666 \| UNC 0631 \| AMI-1 free acid \| MS37452 \| Piribedil
Related Compound Libraries	Inhibitor Library \| Nucleotide Compound Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Chromatin Modification Compound Library \| Highly Selective Inhibitor Library \| NO PAINS Compound Library \| Epigenetics Compound Library \| Anti-COVID-19 Compound Library \| Target-Focused Phenotypic Screening Library

SGC0946|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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