GSK-J4, JMJ H3K27 Demethylase inhibitor (cell permeable) (TBI1394)

Description

Product Details

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

Molecular Formula: C₂₄H₂₇N₅O₂

Formula Weight: 417.48

CAS Number: 1373423-53-0

Purity: >98%

Formulation: wax

Solubility: Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

JMJ H3K27 Demethylase inhibitor (cell permeable)

Functions

Histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J1. Rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies.

Application Procedures

First dissolved in DMSO (up to 40 mg/ml) or in Ethanol (up to 40 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.