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| | GSK-467 Basic information |
| Product Name: | GSK-467 | | Synonyms: | cGAS inhibitor 467;GSK-467;2-((1-Benzyl-1H-pyrazol-4-yl)oxy)pyrido[3,4-d]pyrimidin-4(3H)-one;HCC,inhibit,GSK 467,GSK467,Histone Demethylase,GSK-467,human multiple myeloma tumor,anticancer,PLU1,Inhibitor,JARID1B;Pyrido[3,4-d]pyrimidin-4(3H)-one, 2-[[1-(phenylmethyl)-1H-pyrazol-4-yl]oxy]-;GSK467, 10 mM in DMSO | | CAS: | 1628332-52-4 | | MF: | C17H13N5O2 | | MW: | 319.32 | | EINECS: | | | Product Categories: | | | Mol File: | 1628332-52-4.mol |  |
| | GSK-467 Chemical Properties |
| Boiling point | 560.6±60.0 °C(Predicted) | | density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO : 20.83 mg/mL (65.23 mM);Water : < 0.1 mg/mL (insoluble) | | pka | 2.27±0.20(Predicted) | | form | Solid | | color | White to off-white |
| | GSK-467 Usage And Synthesis |
| 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 |
| | GSK-467 Preparation Products And Raw materials |
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