GSK-J1, JMJ H3K27 Demethylase inhibitor (cell impermeable) (TBI1393)

Description

Product Details

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

Molecular Formula: C₂₂H₂₃N₅O₂

Formula Weight: 389.46

CAS Number: 1373422-53-7

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 20 mg/ml).

Storage: RT

Stability: ≥ 2 years.

Applications

JMJ H3K27 Demethylase inhibitor (cell impermeable)

Functions

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.

Application Procedures

First dissolved in DMSO (up to 20 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 3 months.