Gsk484 Hydrochloride

製品コードS7803 バッチS780302

印刷

化学情報

Chemical Structure Synonyms GSK484 hydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C27H32ClN5O3
分子量 510.03 CAS No. 1652591-81-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (196.06 mM)
Water 100 mg/mL (196.06 mM)
Ethanol 100 mg/mL (196.06 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GSK484 HCl, a benzoimidazole derivative, is a selective and reversible inhibitor of peptidylarginine deiminase 4 (PAD4) with IC50 of 50 nM in the absence of Calcium.
in vitro

GSK484 also inhibits PAD4 citrullination (at 0.2 mM calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH3 release assay. GSK484 causes a clear, statistically-significant reduction in diffused NETs.[1]
in vivo

GSK484 prevents tumor-induced NETosis in vivo and can antagonize kidney injury in mice with mammary carcinoma or pancreatic neuroendocrine tumors.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NB4 cells, HEK293 cells
濃度 10 μM, 100 μM
反応時間 20 min
実験の流れ

HEK293 cells stably expressing N-terminal FLAG-tagged PAD1, PAD2, PAD3 or PAD4 are engineered by retroviral transduction. Cells are grown in 15 cm diameter plates to subconfluency in DMEM supplemented with 10% Foetal Bovine Serum, harvested by centrifugation and washed once in PBS/2 mM EGTA. Cells are lysed in 50 mM Tris-Cl, pH 7.4, 1.5 mM MgCl2, 5% glycerol, 150 mM NaCl, 25 mM NaF, 1 mM Na3VO4, 0.4% NP40, 1 mM DTT with protease inhibitors. Lysates are pre-incubated for 20 min at 4℃ with DMSO alone (2%) or 100 μM of GSK484. Citrullination reactions are performed for 30 min at 37℃ in the presence of 2 mM calcium.
動物実験 動物モデル MMTV-PyMT mouse model (FVB) and RIP1-Tag2 mouse model (C57BL)
投薬量 4 mg/kg
投与方法 IP

参考

  • https://pubmed.ncbi.nlm.nih.gov/25622091/
  • https://pubmed.ncbi.nlm.nih.gov/28919990/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Neutrophil extracellular traps promote pre-metastatic niche formation in the omentum by expanding innate-like B cells that express IL-10 [ Cancer Cell, 2025, 43(1):69-85.e11] PubMed: 39753138
Metabolic Implications of Elevated Neutrophil Extracellular Traps in Polycystic Ovary Syndrome: A Focus on Hepatic Glycolysis [ Biomolecules, 2025, 15(4)572] PubMed: 40305335
Cryoablation-induced neutrophil Ca2+ elevation and NET formation exacerbate immune escape in colorectal cancer liver metastasis [ J Exp Clin Cancer Res, 2024, 43(1):319] PubMed: 39648199
Berbamine ameliorates DSS-induced colitis by inhibiting peptidyl-arginine deiminase 4-dependent neutrophil extracellular traps formation [ Eur J Pharmacol, 2024, S0014-2999(24)00322-4] PubMed: 38710356
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Re-Du-Ning injection ameliorates LPS-induced lung injury through inhibiting neutrophil extracellular traps formation [ Phytomedicine, 2021, 90:153635] PubMed: 34229173
The PAD4 inhibitor GSK484 enhances the radiosensitivity of triple-negative breast cancer [ Hum Exp Toxicol, 2020, 960327120979028] PubMed: 33355008

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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