GSK-J4 1μM R07 exp362
Mechanism of Action
JMJD3/KDM6B, UTX/KDM6A histone demethylase inhibitor (H3K27me2/me3)
- Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor
Technical Notes
Compound References
- PubChem Name: GSK J4 HCl
- Synonyms: N/A
- CAS #: 1797983-09-5
- PubChem CID: 71729974
- IUPAC: ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate;hydrochloride
- INCHI Name: InChI=1S/C24H27N5O2.ClH/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29;/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28);1H
- INCHI Key: TYXWLTBYINKVNT-UHFFFAOYSA-N
- Molecular Weight: 454
- Canonical SMILES: CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3.Cl
- Isomeric SMILES: N/A
- Molecular Formula: C24H28ClN5O2
Compound Supplier
- Supplier Name: Sigma-Aldrich
- Catalog #: SML0701
- Lot #: 053M4601V
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C24H27N5O2 418.22375; found 418.22478
Dose Response Curve
- Platform ID: GSK-J4
- Min: -0.8548; Max: 90.3053
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | 0.5053 |
| IC30 | 0.6250 |
| IC40 | 0.7484 |
| IC50 | 0.8887 |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 07
- Dose: 1µM
- Days of incubation: 8
- Doublings: 6.3
- Numbers of reads: 19363826
Screen Results
| Sensitive/Resistant hits (FDR<0.05) | CRANKS | Score Plot | Top 30 Genes | Screen Similarity | Top 30 Sensitive GO terms | Top 30 Resistant GO terms |
|---|---|---|---|---|---|---|
| 7/0 | Scores |
GSK-J4 1μM R07 exp362
GSK-J4 1μM R07 exp362 vs UM0131023 0.05μM R05 exp248
GSK-J4 1μM R07 exp362 vs VHL-ligand-1 20μM R07 exp421
GSK-J4 1-1.25μM to day4 R07 exp363 vs GSK-J4 1μM R07 exp362
