产品名称

英文名称：GSK126

同义词

GSK126、1346574-57-9、GSK-126、GSK 126、(S)-1-(sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide、GSK2816126、GSK-2816126、EZH2 inhibitor、W4OGW9QZ97、CHEMBL3287735、GSK-2816126A、1-

产品性质

CAS编号：1346574-57-9

分子式：C31H38N6O2

分子量：526.67

PubChem编号：68210102

英文别名：GSK126|1346574-57-9|GSK-126|GSK 126|(S)-1-(sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide|GSK2816126|GSK-2816126|EZH2 inhibitor|W4OGW9QZ97|CHEMBL3287735|GSK-2816126A|1-

规格或纯度：≥98%

英文名称：GSK126

生化机理：DescriptionIC50 Value 0.5nM (Ki)GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 may provide a promising treatment for EZH2 mutant lymphoma.in vitro Althoμgh GSK126 induced loss of H3K27me3 independent of EZH2 mutation status, six of seven lymphoma cell lines sensitive to GSK126 treatment were EZH2-mutation(+), while only two of 11 lymphoma cell lines less sensitive to GSK126 were EZH2-mutation(+) [1]. SCLC cell lines were then treated with a selective EZH2 inhibitor, GSK126, at different doses of 0.5, 2, and 8 μM [1].in vivo GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice [2].Clinical trial N/A.Potent inhibitor EZH2 methyltransferase inhibitor (K i = 93 pM). Selective (>150-fold) versus EZH1. Greater than 1000-fold selective against a panel of 20 other human methyltransferases including both SET-domain-containing and non-SET-domain-containing me

储存温度：-20°C储存

运输条件：超低温冰袋运输

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产品介绍：GSK126是高活性，S-腺苷-蛋氨酸竞争性EZH2甲基转移酶抑制剂，Ki为0.5 nM。GSK126 is a potent highly selective S adenosyl methionine competitive small molecule inhibitor of EZH2 methyltransferase with Ki value of 0.5 nM.

ALogP：3.9

IUPAC Name：1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide

INCHI：InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1

InChi Key：FKSFKBQGSFSOSM-QFIPXVFZSA-N

Canonical SMILES：CCC(C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C

Isomeric SMILES：CC[C@H](C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C

PubChem CID：68210102

CAS Registry No.：1346574-57-9

ChEMBL Ligand：CHEMBL3287735

RCSB PDB Ligand：A9G

溶解性：25°C DMSO

产品包装