For research use only. Not for therapeutic Use.
GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members[1][2].
GSK467 (0-100 μM; 6 days) shows antiproliferative effect against human multiple myeloma tumor cells[1].
GSK467 is located in the 2-OG-binding pocket[2].
GSK467 inhibits spheroid formation, colony formation, invasion and migration of HCC cells[3].
GSK-467 can inhibit the proliferation and growth of HCC tumor cells by promoting the expression of miR-448 and inhibiting the YTHDF3/ITGA6 pathway in female BALB/c nude mice[3].
| Catalog Number | I019055 |
| CAS Number | 1628332-52-4 |
| Synonyms | 2-(1-benzylpyrazol-4-yl)oxy-3H-pyrido[3,4-d]pyrimidin-4-one |
| Molecular Formula | C17H13N5O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H13N5O2/c23-16-14-6-7-18-9-15(14)20-17(21-16)24-13-8-19-22(11-13)10-12-4-2-1-3-5-12/h1-9,11H,10H2,(H,20,21,23) |
| InChIKey | ZTYRLXUTLYBVHH-UHFFFAOYSA-N |
| SMILES | C1=CC=C(C=C1)CN2C=C(C=N2)OC3=NC4=C(C=CN=C4)C(=O)N3 |
| Reference | [1]. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45. [2]. Fu YD, et al. Targeting histone demethylase KDM5B for cancer treatment. Eur J Med Chem. 2020 Dec 15;208:112760. [3]. Guo JC, et al. KDM5B promotes self-renewal of hepatocellular carcinoma cells through the microRNA-448-mediated YTHDF3/ITGA6 axis. J Cell Mol Med. 2021 Apr 7;25(13):5949–62. |
