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GSK-J1 (Free acid)

A potent histone demethylase JMJD3/UTX inhibitor
Catalog #: 2761
SKU-Size Size Price Qty
2761-1 1 mg
$65.00
2761-5 5 mg
$195.00
More Sizes Get Quote

Product Details

Alternate Name N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Appearance Pale yellow solid
CAS # 1373422-53-7
Molecular Formula C₂₂H₂₃N₅O₂
Molecular Weight 398.45
Purity ≥98% by TLC
Solubility DMSO (~ 20 mg/ml)
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
PubChem CID 56963315
MDL Number MFCD22683851
Handling Protect from light and moisture
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

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).


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