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文件

SML0709

GSK-J1

Name: GSK-J1
Brand: SIGMA

≥98% (HPLC)

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别名:

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

经验公式（希尔记法）:

C₂₂H₂₃N₅O₂

CAS号:

1373422-53-7

分子量:

389.45

MDL编号:

MFCD22683851

PubChem化学物质编号:

329825587

NACRES:

NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 15 mg/mL, clear

储存温度

2-8°C

SMILES字符串

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

应用

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

生化/生理作用

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

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.

特点和优势

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.

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.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

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Small Molecule GSK-J1 Affects Differentiation of Specific Neuronal Subtypes in Developing Rat Retina.

Raeisossadati R, et al.

Molecular Neurobiology, 1-12 (2018)

The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads, 1362-1362 (2017)

Congenital Hyperinsulinism in Infants with Turner Syndrome: Possible Association with Monosomy X and KDM6A Haploinsufficiency.

Christopher E Gibson et al.

Hormone research in paediatrics, 89(6), 413-422 (2018-06-15)

Previous case reports have suggested a possible association of congenital hyperinsulinism with Turner syndrome. We examined the clinical and molecular features in girls with both congenital hyperinsulinism and Turner syndrome seen at The Children's Hospital of Philadelphia (CHOP) between 1974

Characterization of a linked Jumonji domain of the KDM5/JARID1 family of histone H3 lysine 4 demethylases.

Horton JR, et al.

The Journal of Biological Chemistry, 291(6), 2631-2646 (2016)

An epitranscriptomic mechanism underlies selective mRNA translation remodelling in melanoma persister cells.

Shensi Shen et al.

Nature communications, 10(1), 5713-5713 (2019-12-18)

Cancer persister cells tolerate anticancer drugs and serve as the founders of acquired resistance and cancer relapse. Here we show that a subpopulation of BRAFV600 mutant melanoma cells that tolerates exposure to BRAF and MEK inhibitors undergoes a reversible remodelling

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文件

GSK-J1

≥98% (HPLC)

属性

质量水平

检测方案

形式

颜色

溶解性

储存温度

SMILES字符串

InChI

InChI key

相关类别

说明

应用

生化/生理作用

特点和优势

相关产品

相关产品

安全信息

储存分类代码

WGK

闪点(°F)

闪点(°C)

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