GSK-J1 --- H3K27 Histone Demethylases UTX and JMJD3 Inhibitor


Catalog No. size PriceQuantity
M60062-2D 2 mg in DMSO (0.513 mL) $109
M60062-2S 2mg solid $109
M60062-10S 10mg solid $431

Description

GSK-J1 is the first selective and potent inhibitor of the H3K27 histone demethylases UTX and JMJD3. H3K27 methylations play important roles in regulating gene expression through the polycomb-repressive complex (PRC1 or PRC2). This epigenetic mark can be demethylated by lysine demethylase (KDM) UTX and JMJD3, which play important roles in cellular differentiation, development and cancer. In relevant biological assays, GSK-J1 was shown to reduce lipopolysaccharide-induced pro-inflammatory cytokine production by human primary macrophages, a process that depends on both UTX and JMJD3. GSK-J1 represents a unique small molecule tool to allow selective pharmacological intervention across the JMJ family. Although critical for in vitro binding, the highly polar carboxylate group of GSK-J1 restricts its cellular permeability. Therefore another compound, GSK-J4, was developed as a pro-drug, masking the polarity of the acid group of the GSK-J1, for cellular assays.

Product information

CAS Number: 1373422-53-7

Molecular Weight: 389.45

Formula: C22H23N5O2

Related CAS Number:

2309668-29-7 (Lithium)

Chemical Name: 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid

Smiles: OC(=O)CCNC1=CC(=NC(=N1)C1=CC=CC=N1)N1CCC2=CC=CC=C2CC1

InChiKey: AVZCPICCWKMZDT-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GSK-J1 was used at 30-100 µM final concentration in vitro.

References:

  1. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response (2012) Nature. 488(7411):404-8.
  2. SGC website: http://www.thesgc.org/scientists/chemical_probes/GSKJ1

Products are for research use only. Not for human use.


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