Free shipping on all orders over $ 500

GSK-J4

Cat. No. M5149
GSK-J4 Structure
Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 120 In stock
25mg USD 250 In stock
Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GSK-J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 417.5
Formula C24H27N5O2
CAS Number 1373423-53-0
Purity >99%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8. PMID: 22842901.

Related Histone demethylases Products
SP2509

SP2509 is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase.

Mebhydrolin napadisylate

Mebhydrolin (napadisylate) is an antihistamine, used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.

EPZ020411

EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has >10 fold selectivity for PRMT6 over PRMT1 and PRMT8. IC50 value: 10 nM

ORY-1001

ORY-1001 (RG-6016) is the only dual KDM1A/LSD1 inhibitor, and it is also the only KDM1A inhibitor in development for the treatment of neurodegenerative disease.

GSK2879552

GSK2879552 is a potent, selective, orally bioavailable, mechanism-based irreversible inactivator of LSD1.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK-J4 supplier, Histone demethylases, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.