GSK-J1 (Free acid) | 2761

GSK-J1 is a potent and selective inhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC₅₀ = 60 nM, human JMJD3). This is the first known inhibitor selective for the H3K27me3-specific JMJ subfamily which binds to the active catalytic site of the enzyme. The COOH group confers cell impermeability and as such is useful as a standard in in vitro assays. A cell permeable ethyl ester analog is also available (Cat. Nos. 2259 & 2762).

GSK-J1 is a potent and selective inhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC₅₀ = 60 nM, human JMJD3). This is the first known inhibitor selective for the H3K27me3-specific JMJ subfamily which binds to the active catalytic site of the enzyme. The COOH group confers cell impermeability and as such is useful as a standard in in vitro assays. A cell permeable ethyl ester analog is also available (Cat. Nos. 2259 & 2762).

2761 | GSK-J1 (Free acid) DataSheet

Alternate Name/Synonyms: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine

Appearance: Pale yellow solid

Formulation: N/A

CAS Number: 1373422-53-7

Structure Available?: Y

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₂H₂₃N₅O₂

Molecular Weight: 398.45

Cell-Permeable?: Y

Purity: ≥98% by TLC

Solubilities: DMSO (~ 20 mg/ml)

Handling: Protect from light and moisture

Country of Origin: USA

Tag Line: A potent histone demethylase JMJD3/UTX inhibitor

MDL Number: MFCD22683851

PubChem CID: 56963315

SMILES: C1CN(CCC2=CC=CC=C21)C3=CC(=NC(=N3)C4=CC=CC=N4)NCCC(=O)O

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)

InChi Key: AVZCPICCWKMZDT-UHFFFAOYSA-N