GSK343, 增强子宙斯特 1 多聚核抑制复合体 2 亚基抑制剂;增强子宙斯特 2 多聚核抑制复合体 2 亚基抑制剂

强大的,选择性的,细胞可穿透的\ xa0histone H3-赖氨酸27(H3K27)甲基转移酶EZH2抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
G421313-1ml
1ml 现货 Stock Image
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Compound libraries (12326)

基本描述

别名 1-异丙基-N-[(6-甲基-2-氧代-4-丙基-1,2-二氢-3-吡啶基)甲基]-6-[2-(4-甲基-1-哌嗪基)-4-吡啶基]-1H-吲唑-4-甲酰胺
英文别名 GSK343 | 1346704-33-3 | GSK 343 | GSK-343 | 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide | CHEMBL2204995 | 1-(1-Methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyri
规格或纯度 Moligand™, 2mM in DMSO
英文名称 GSK343
生化机理 它是组蛋白 H3 赖氨酸 27 (H3K27) 甲基转移酶 EZH2 的强效特异性抑制剂。GSK343 抑制 EZH2 酶活性的 IC50 为 4 nM。与 EZH1 相比,该化合物对 EZH2 的选择性为 60 倍,对其他组蛋白甲基转移酶的选择性为 1000 倍或更高。在 HCC1806 细胞中,抑制 H3K27 甲基化的 IC50 小于 200 nM。抑制 EZH2 酶活性(IC 50/xa0= 4 nM)。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 增强子宙斯特 1 多聚核抑制复合体 2 亚基抑制剂;增强子宙斯特 2 多聚核抑制复合体 2 亚基抑制剂
产品介绍

It is an epigenetic chemical probe available through a partnership between Sigma Life Science and the Structural Genomics Consortium (SGC).

It is an epigenetic chemical probe available through a partnership between Sigma Life Science and the Structural Genomics Consortium (SGC).
An inhibitor of the histone lysine methyltransferase ENX-1.

关联靶点(人)

EZH1 Tchem 组蛋白赖氨酸N-甲基转移酶EZH1(Histone-lysine N-methyltransferase EZH1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
EZH2 Tclin 组蛋白赖氨酸N-甲基转移酶EZH2(Histone-lysine N-methyltransferase EZH2) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA1B Tclin Alpha-1b adrenergic receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT1 Tclin DNA (cytosine-5)-methyltransferase 1 (978 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT3A Tclin DNA (cytosine-5)-methyltransferase 3A (310 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SETD7 Tchem Histone-lysine N-methyltransferase SETD7 (390 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT1 Tchem Protein-arginine N-methyltransferase 1 (867 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT3 Tchem Protein arginine N-methyltransferase 3 (219 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DNMT3B Tchem DNA (cytosine-5)-methyltransferase 3B (150 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KMT2A Tchem Histone-lysine N-methyltransferase MLL (17327 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRMT5 Tchem Protein arginine N-methyltransferase 5 (1273 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DOT1L Tchem Histone-lysine N-methyltransferase, H3 lysine-79 specific (648 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SUV39H1 Tchem Histone-lysine N-methyltransferase SUV39H1 (101 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SUV39H2 Tchem Histone-lysine N-methyltransferase SUV39H2 (524 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (2012 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SETMAR Tbio Histone-lysine N-methyltransferase SETMAR (3 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KMT2B Tbio Histone-lysine N-methyltransferase MLL4 (6 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KMT2C Tbio Histone-lysine N-methyltransferase MLL3 (36 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KMT2D Tbio Histone-lysine N-methyltransferase MLL2 (15 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EZH1 Tchem Histone-lysine N-methyltransferase EZH1 (112 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EZH1 Tchem EZH1/SUZ12/EED/AEBP2/RBBP4 complex (29 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EZH2 Tclin EZH2/SUZ12/EED/RBBP7/RBBP4 (11 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点(其它种属)

Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Human immunodeficiency virus 1 (70413 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Carm1 Histone-arginine methyltransferase CARM1 (53 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IUPAC Name N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide
INCHI InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
InChi Key ULNXAWLQFZMIHX-UHFFFAOYSA-N
Canonical SMILES CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C
Isomeric SMILES CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C
WGK Germany 3
PubChem CID 71268957
分子量 541.69

化学和物理性质

分子量 541.700 g/mol
XLogP3 4.000
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 8
精确质量Exact Mass 541.317 Da
单同位素质量Monoisotopic Mass 541.317 Da
拓扑极表面积Topological Polar Surface Area 95.400 Ų
重原子数Heavy Atom Count 40
形式电荷Formal Charge 0
复杂度Complexity 986.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性(GHS)

象形图 GHS07
信号词 Warning
危险声明

H302: 吞食有害

预防措施声明

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P270: 使用本产品时,请勿进食、饮水或吸烟。

P330: 漱口

P301+P317: 如果被吞咽:请寻求医疗帮助。

WGK Germany 3

技术规格说明书

Concentration(Compounding value) 1-3(mmol/L)
Appearance(Colorless Transparent Liquid) Pass
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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