Gsk484 Hydrochloride

製品コードS7803 バッチS780301

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)
Ethanol 100 mg/mL (196.06 mM)
Water 8 mg/mL (15.68 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 ベンゾイミダゾール誘導体であるGSK484 HClは、カルシウム非存在下でIC50が50 nMのペプチジルアルギニンデイミナーゼ4 (PAD4)の選択的かつ可逆的阻害剤です。
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.
in vivo

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

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
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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