CAS 1373422-53-7; 3-((6-(4,5-dihydro-1h-benzo[d]azepin-3(2h)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid; n-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3h-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine; gsk-j1

CAS:

1373422-53-7

分子式:

C₂₂H₂₃N₅O₂

分子量:

389.45

中文名称:

3-((6-(4,5-dihydro-1h-benzo[d]azepin-3(2h)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid; n-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3h-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine

英文名称:

gsk-j1

用途:

GSK-J1是一种高效的 H3K27 histone demethylase 抑制剂，无细胞试验中对JMJD3 (KDM6B) 和 UTX (KDM6A)的 IC50 分别为 28 nM 和 53 nM，比作用于其他测试的脱甲基酶选择性高10倍多。

推荐供应商

货号

品牌

产品名称

规格

包装、参考价格

G792308

MACKLIN

GSK J1

10mM in DMSO

539元/1ml;

咨询

储存：-20°C

G872492

MACKLIN

GSK J1

99%

409元/5mg; 696元/25mg; 2009元/100mg; 3417元/250mg;

咨询

储存：-20℃
状态：白色到米黄色粉末

SML0709

Sigma-Aldrich

GSK-J1

≥98% (HPLC)

1412.42元/5 MG; 4556.8元/25 MG;

咨询

产品说明

应用

GSK-J1 has been used in formaldehyde dehydrogenase (FDH)-coupled demethylase assay.

包装

5, 25 mg in glass bottle

生化/生理作用

GSK-J1 is also termed as 3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate. It may disturb the differentiation of specific neuronal subtypes in growing rat retina.
GSK-J1 is a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC₅₀ of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. For full characterization details, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

特点和优势

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
GSK-J1 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.

基本信息

经验(实验)分子式	C₂₂H₂₃N₅O₂
分子量	389.45
MDL编号	MFCD22683851
PubChem化学物质编号	329825587
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 15 mg/mL, clear
储存温度	2-8℃
SMILES string	OC(CCNC1=CC(N2CCC(C=CC=C3)=C3CC2)=NC(C4=CC=CC=N4)=N1)=O
InChI	1S/C22H23N5O2/c28-21(29)8-12-24-19-15-20(26-22(25-19)18-7-3-4-11-23-18)27-13-9-16-5-1-2-6-17(16)10-14-27/h1-7,11,15H,8-10,12-14H2,(H,28,29)(H,24,25,26)
InChI key	AVZCPICCWKMZDT-UHFFFAOYSA-N

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

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