GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC|50|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. The prodrug GSK-J4 inhibited TNF-α production with an IC|50|of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK J4 is an inhibitor of JMJD3 and UTX.GSK J4is A cell permeable inhibitor of the histone demethylase JMJD3/UTX. Specifications and Purity: ≥98%. MDL Number: MFCD22683852. Molecular Formula: C24H27N5O2. Molecular Weight: 417.51. PubChem CID: 71729975. Isomeric SMILES: CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/G382666-SCI_ca4429bef65dc05b1d58a5e1b2bfbfc1.pdf.
- UPC:
- 12352005
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 0.96 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- G382666-50mg
- CAS:
- 1373423-53-0
- Product Size:
- 50mg
- Hazard Statement Codes:
- H319:H335
- Precautionary Statement Codes:
- P261:P264:P271:P280
