GSK484 hydrochloride |
| カタログ番号GC19184 |
ペプチジルアルギニンデイミナーゼ4（PAD4）阻害剤
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1652591-81-5
Sample solution is provided at 25 µL, 10mM.
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GSK484 is a selective PAD4 inhibitor, has been used as an anti-ischemic compound and exerts inhibitory activity against PAD4. In the absence of calcium the IC50 value is 50 nM[1-3].
GSK484(25 nM; 1 h before irradiation) facilitated Triple-negative breast cancer (TNBC) cell apoptosis[4]. GSK484(100 nM; 15min) treatment promoted the radiosensitivity of CRC cells and induced cell death by promoting DNA double-strand breaks[5].
GSK484(4 mg/kg; i.p;40days) significantly inhibited tumor size, tumor weight and tumor volume in mice following irradiation in Nasopharyngeal carcinoma (NPC) mice model[6]. GSK484(4 mg/kg; i.p;3days) inhibits PAD4 to reduce distal lung injury by reducing neutrophil infiltration, neutrophil extracellular trap formation, apoptosis, and inflammatory cytokine secretion in mice ischemia reperfusion (IR) model[7].
References:
[1]. Perdomo J, Leung HHL, et,al. Neutrophil activation and NETosis are the major drivers of thrombosis in heparin-induced thrombocytopenia. Nat Commun. 2019 Mar 21;10(1):1322. doi: 10.1038/s41467-019-09160-7. PMID: 30899022; PMCID: PMC6428879.
[2]. Perdomo J, Leung HHL, et,al. Neutrophil activation and NETosis are the major drivers of thrombosis in heparin-induced thrombocytopenia. Nat Commun. 2019 Mar 21;10(1):1322. doi: 10.1038/s41467-019-09160-7. PMID: 30899022; PMCID: PMC6428879.
[3]. Du M, Yang W, et,al. Inhibition of peptidyl arginine deiminase-4 protects against myocardial infarction induced cardiac dysfunction. Int Immunopharmacol. 2020 Jan;78:106055. doi: 10.1016/j.intimp.2019.106055. Epub 2019 Dec 6. PMID: 31816575.
[4]. Wei L, Wang X, et,al. The PAD4 inhibitor GSK484 enhances the radiosensitivity of triple-negative breast cancer. Hum Exp Toxicol. 2021 Jul;40(7):1074-1083. doi: 10.1177/0960327120979028. Epub 2020 Dec 23. Erratum in: Hum Exp Toxicol. 2021 Nov;40(11):2022. PMID: 33355008.
[5]. Wang B, Su X, et,al. GSK484, an inhibitor of peptidyl arginine deiminase 4, increases the radiosensitivity of colorectal cancer and inhibits neutrophil extracellular traps. J Gene Med. 2023 Sep;25(9):e3530. doi: 10.1002/jgm.3530. Epub 2023 May 19. PMID: 37203323.
[6]. Chen H, Luo M, et,al. Inhibition of PAD4 enhances radiosensitivity and inhibits aggressive phenotypes of nasopharyngeal carcinoma cells. Cell Mol Biol Lett. 2021 Mar 16;26(1):9. doi: 10.1186/s11658-021-00251-2. Erratum in: Cell Mol Biol Lett. 2021 Dec 30;26(1):55. Erratum in: Cell Mol Biol Lett. 2023 Apr 4;28(1):29. PMID: 33726680; PMCID: PMC7962337.
[7]. Du M, Yang L, et,al. Inhibition of Peptidyl Arginine Deiminase-4 Prevents Renal Ischemia-Reperfusion-Induced Remote Lung Injury. Mediators Inflamm. 2020 Dec 29;2020:1724206. doi: 10.1155/2020/1724206. PMID: 33456369; PMCID: PMC7787741.
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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