| Chemical Properties | Back Directory | [Boiling point ]
560.6±60.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO : 20.83 mg/mL (65.23 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
2.27±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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]. | [IC 50]
KDM5: 10 nM (Ki); KDM5: 26 nM (IC50) | [References]
[1] Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45. DOI:10.1038/nchembio.2087
[2] Fu YD, et al. Targeting histone demethylase KDM5B for cancer treatment. Eur J Med Chem. 2020 Dec 15;208:112760. DOI:10.1016/j.ejmech.2020.112760
[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. DOI:10.1111/jcmm.16342 |
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