货号	规格	价格	上海	北京	珠海	重庆	武汉
S88461-5mg买3赠1	98.72%	￥520.00 S88461-5mg ￥520.00 现货（买3赠1）	5 5	-	-	-	-
S88461-10mg买3赠1	98.72%	￥750.00 S88461-10mg ￥750.00 现货（买3赠1）	3 3	-	-	-	-
S88461-25mg买3赠1	98.72%	￥1200.00 S88461-25mg ￥1200.00 现货（买3赠1）	8 0 8	-	-	-	-
S88461-100mg买3赠1	98.72%	￥3000.00 S88461-100mg ￥3000.00 现货（买3赠1）	7 7	-	-	-	-

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产品描述：

GSK484 HCl 是苯并咪唑的衍生物，是一种选择性的、可逆的 peptidylarginine deiminase 4 (PAD4) 的抑制剂，在无钙的情况下IC50值为50 nM

靶点：

PAD4(in the absence of Calcium):50 nM;PAD

体外研究：

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

体内研究：

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

细胞实验：

Cell lines: NB4 cells, HEK293 cells Concentrations: 10 μM, 100 μM Incubation Time: 20 min Method: 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.

动物实验：

Animal Models: MMTV-PyMT mouse model (FVB) and RIP1-Tag2 mouse model (C57BL) Dosages: 4 mg/kg Administration: IP

参考文献：

1. Huw D Lewis, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91. 2. Jessica Cedervall, et al. Pharmacological targeting of peptidylarginine deiminase 4 prevents cancer-associated kidney injury in mice. Oncoimmunology. 2017 Apr 20;6(8):e1320009.

溶解性：

Soluble in DMSO、Ethanol、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.961 ml	9.803 ml	19.607 ml
5 mM	0.392 ml	1.961 ml	3.921 ml
10 mM	0.196 ml	0.98 ml	1.961 ml
50 mM	0.039 ml	0.196 ml	0.392 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

GSK484 hydrochloride

GSK484

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)