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GSK484 hydrochloride

产品编号 TQ0067 CAS 1652591-81-5

别名: GTPL8577, AOB6992, GSK484盐酸盐

GSK484 hydrochloride (GTPL8577) 是一种可逆的肽酰基精氨酸脱亚氨酶 4 (PAD4) 抑制剂。它高亲和力与 PAD4 结合，在存在 2 mM 钙和不存在钙的情况下，IC50分别为 250 和 50 nM。

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GSK484 hydrochloride, CAS 1652591-81-5

规格	价格/CNY	货期
1 mg	￥ 729	现货
5 mg	￥ 1,770	现货
10 mg	￥ 2,920	现货
25 mg	￥ 4,830	现货
50 mg	￥ 6,890	现货
100 mg	￥ 9,320	现货
500 mg	￥ 18,600	现货
1 mL * 10 mM (in DMSO)	￥ 1,760	现货

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纯度: 99.62%

纯度: 99.51%

纯度: 99.42%

纯度: 99.36%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	GSK484 hydrochloride (GTPL8577) (GTPL8577) is a specifc and reversible peptidyl arginine deiminase 4 (PAD4) inhibitor. It demonstrates high-affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium.
靶点活性	PAD4:50 nM (in 0 mM Calcium), PAD4:50 nM (in 2 mM Calcium)
体外活性	GSK484 demonstrates high-affinity binding to the low-calcium form of PAD4 with IC50s of 50 nM and 250 nM in the absence of Calcium (0 mM) and Calcium (2 mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2 mM Calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner [1].
体内活性	To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4 mg/kg daily for one week. This dose suppresses the elevated number of neutrophils undergoing NETosis in peripheral blood in mice with cancer. In parallel, the total protein level in urine from MMTV-PyMT mice is significantly reduced compared with untreated tumor-bearing mice. Administration of GSK484 at a dose of 4 mg/kg daily during one week reverts signs of kidney dysfunction in tumor-bearing mice to the same extent as DNase I treatment, without any detectable signs of toxicity [2].
激酶实验	PAD4 is serially diluted in the presence of 10 nM GSK215 in assay buffer (100 mM HEPES, pH 8, 50 mM NaCl, 5% glycerol, 1 mM CHAPS, 1 mM DTT) at varying concentrations of calcium (0, 0.2, 2 and 10 mM). Following incubation for 50 min, apparent Kds for each calcium concentration are determined using a single site saturation curve. For IC50 determination, GSK484 is serially diluted in DMSO (1% final assay concentration) and tested at the same range of calcium concentrations in the presence of PAD4 (at the calculated Kd for each calcium condition) and 10 nM GSK215 in the same assay buffer and volume. Reactions are incubated for 50 min after which IC50 values are calculated using a four-parameter logistic equation [1].
细胞实验	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°C with DMSO alone (2%), 100 μM of GSK199, GSK484, GSK106 or 200 μM Cl-amidine. Citrullination reactions are performed for 30 min at 37°C in the presence of 2 mM calcium. Extracts are loaded on to gels, proteins separated by SDS-PAGE and transferred to PVDF membranes. Citrullinated proteins are then chemically modified and detected using an anti-modified citrulline antibody. FLAG-PAD constructs are detected using the anti-FLAG antibody [1].
动物实验	The study includes the MMTV-PyMT mouse model for mammary carcinoma (FVB/n background) and the RIP1-Tag2 mouse model for pancreatic neuroendocrine carcinoma (C57BL/6 background). Mice are treated daily by intra-peritoneal injections of the PAD4 inhibitor GSK484 (4 mg/kg). GSK484 is dissolved in 99.9% ethanol at a concentration of 25 mg/mL to generate a stock solution and further diluted 1:50 in 0.9% NaCl shortly before injection of 200 μL/mouse [2].

别名	GTPL8577, AOB6992, GSK484盐酸盐
分子量	510.03
分子式	C27H32ClN5O3
CAS No.	1652591-81-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (117.64 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9607 mL	9.8033 mL	19.6067 mL	49.0167 mL
	5 mM	0.3921 mL	1.9607 mL	3.9213 mL	9.8033 mL
	10 mM	0.1961 mL	0.9803 mL	1.9607 mL	4.9017 mL
	20 mM	0.098 mL	0.4902 mL	0.9803 mL	2.4508 mL
	50 mM	0.0392 mL	0.1961 mL	0.3921 mL	0.9803 mL
	100 mM	0.0196 mL	0.098 mL	0.1961 mL	0.4902 mL

计算器

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稀释计算器

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分子量计算器

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参考文献

1. Lewis HD, 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. Cedervall J, et al. Pharmacological targeting of peptidylarginine deiminase 4 prevents cancer-associated kidney injury in mice. Oncoimmunology. 2017 Apr 20;6(8):e1320009.

文献引用

1. Chen J, Zhao L, Ding X, et al. Aβ1–40 Oligomers Trigger Neutrophil Extracellular Trap Formation through TLR4- and NADPH Oxidase-Dependent Pathways in Age-Related Macular Degeneration. Oxidative Medicine and Cellular Longevity. 2022

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

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给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

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% ddH₂O

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GSK484 hydrochloride 1652591-81-5 Chromatin/Epigenetic PAD GTPL8577 AOB6992 GSK 484 Protein Arginine Deiminase GTPL-8577 GSK484 Hydrochloride GTPL 8577 GSK-484 AOB-6992 GSK-484 hydrochloride GSK484 inhibit Peptidylarginine Deiminase GSK 484 Hydrochloride AOB 6992 Inhibitor GSK-484 Hydrochloride GSK484盐酸盐 inhibitor

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GSK484 hydrochloride

存储

溶解度

溶液配制表

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参考文献

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剂量换算

体内实验配液计算器

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