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AB144396

GSK-J1, H3K27 histone demethylase inhibitor

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MW 389.4 Da, Purity >99%. Potent and selective H3K27 histone demethylase inhibitor (IC50 = 60 nM, JMJD3). Inhibits UTX. Some activity for the H3K4me3/2/1 demethylases Jarid1b and Jarid1c (IC50 values are 950 nM and 1.76 μM, respectively). No significant inhibitory activity against 100 protein kinases at a concentration of 30 μM. Anti-inflammatory effects.

View Alternative Names

CT31, Cancer/testis antigen 31, DKFZp686A03225, DKFZp686A24246, DKFZp686P07111, DXS1272E, Histone demethylase JARID1A, Histone demethylase JARID1B, Histone demethylase JARID1C, Histone demethylase JMJD3, Histone demethylase UTX, JARID1A, JARID1B, JARID1C, JHDM2A, JHMD2A, JMJD1, JMJD1A, JMJD2E, JmjC domain containing protein SMCX, JmjC domain-containing histone demethylation protein 2A, JmjC domain-containing protein 3, Jumonji AT rich interactive domain 1B, Jumonji AT rich interactive domain 1C, Jumonji C domain containing histone demethylase 2A, Jumonji D3, Jumonji domain containing 1, Jumonji domain containing 1A, Jumonji domain containing 3, Jumonji domain containing 3 histone lysine demethylase, Jumonji domain-containing protein 1A, Jumonji domain-containing protein 3, Jumonji, AT rich interactive domain 1C (RBP2 like), Jumonji/ARID domain-containing protein 1A, Jumonji/ARID domain-containing protein 1B, Jumonji/ARID domain-containing protein 1C, KABUK2, KDM3A_HUMAN, KDM4D-like protein, KDM4DL, KDM5A_HUMAN, KDM5B_HUMAN, KDM5C_HUMAN, KDM6A_HUMAN, KDM6B_HUMAN, KIAA0346, KIAA0742, Lysine (K) specific demethylase 3A, Lysine (K) specific demethylase 5B, Lysine (K) specific demethylase 5C, Lysine (K) specific demethylase 6A, Lysine K specific demethylase 6A, Lysine K specific demethylase 6B, Lysine demethylase 5B, Lysine demethylase 6B, Lysine specific demethylase 4E, Lysine specific demethylase 6A ubiquitously transcribed tetratricopeptide repeat gene X chromosome, Lysine-specific demethylase 3A, Lysine-specific demethylase 5A, Lysine-specific demethylase 5B, Lysine-specific demethylase 5C, Lysine-specific demethylase 6A, Lysine-specific demethylase 6B, MGC141941, MRX13, MRXJ, MRXSCJ, MRXSJ, PLU-1, PPP1R98, PUT1, Protein SmcX, Protein Xe169, Protein phosphatase 1 regulatory subunit 98, RBBP-2, RBBP2H1A, RBP2 like, RBP2-H1, Retinoblastoma-binding protein 2, Retinoblastoma-binding protein 2 homolog 1, Retinoblastoma-binding protein 2 homolog 1A, SMCX, Selected cDNA on X, SmcX protein, Smcx homolog X chromosome, Smcy homolog X linked, TSGA, Testis specific protein A, UTX, Ubiquitously transcribed TPR gene on the X chromosome, Ubiquitously transcribed tetratricopeptide repeat X chromosome, Ubiquitously transcribed tetratricopeptide repeat protein X linked, Ubiquitously-transcribed TPR protein on the X chromosome, Ubiquitously-transcribed X chromosome tetratricopeptide repeat protein, XE169, Xe169 protein, bA386N14.2, bA386N14.2 (ubiquitously transcribed X chromosome tetratricopeptide repeat protein (UTX), bA386N14.2 ubiquitously transcribed X chromosome tetratricopeptide repeat protein UTX, lysine (K)-specific demethylase 4E, putative DNA/chromatin binding motif, rbp2 like protein

1 Images
Chemical Structure - GSK-J1, H3K27 histone demethylase inhibitor (AB144396)
  • Chemical Structure

Lab

Chemical Structure - GSK-J1, H3K27 histone demethylase inhibitor (AB144396)

2D chemical structure image of ab144396, GSK-J1, H3K27 histone demethylase inhibitor

Key facts

CAS number

1373422-53-7

Purity

>99%

Form

Solid

form

Molecular weight

389.4 Da

Molecular formula

C<sub>2</sub><sub>2</sub>H<sub>2</sub><sub>3</sub>N<sub>5</sub>O<sub>2</sub>

PubChem

56963315

Nature

Synthetic

Biochemical name

3-[[2-Pyridin-2-Yl-6-(1,2,4,5-Tetrahydro-3-Benzazepin-3-Yl)pyrimidin-4-Yl]amino]propanoic Acid

Biological description

Potent and selective H3K27 histone demethylase inhibitor (IC50 = 60 nM, JMJD3). Inhibits UTX. Some activity for the H3K4me3/2/1 demethylases Jarid1b and Jarid1c (IC50 values are 950 nM and 1.76 μM, respectively). No significant inhibitory activity against 100 protein kinases at a concentration of 30 μM. Anti-inflammatory effects.

Canonical smiles

C1CN(CCC2=CC=CC=C21)C3=NC(=NC(=C3)NCCC(=O)O)C4=CC=CC=N4

InChi

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)

InChiKey

AVZCPICCWKMZDT-UHFFFAOYSA-N

IUPAC Name

3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoic acid

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Product protocols

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