010-60605840
结构式搜索
  1. 首页
  2. 产品目录
  3. Signaling Pathways(信号通路)
  4. Epigenetics(表观遗传学)
  5. Protein Arginine Deiminase
中文名称: GSK484 hydrochloride
英文名称: GSK484 hydrochloride
CAS No: 1652591-81-5
分子式: C27H30ClN5O3
分子量: 510.03
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
G10435 GSK484 hydrochloride ≥98% (psaitong)
包装规格：
100mg in glass bottle
溶解性：
溶于DMSO（62.5 mg/mL）
产品描述：

基本信息

产品编号：G10435

产品名称：GSK484 hydrochloride

CAS:

1652591-81-5

 

储存条件

粉末

2-8℃ 充氮保存

四年

分子式：

C27H30ClN5O3

溶于液体

-80℃(氮气保存)

六个月

分子量：

510.03

-20℃(氮气保存)

一个月

化学名： 

 

 

Solubility (25°C)

 

体外

DMSO

100mg/mL (196.06mM)

Ethanol

100mg/mL (196.06mM)

Water

100mg/mL (196.06mM)

体内（现配现用）

 

 

＜1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

1.9607mL

9.8033mL

19.6067mL

5mM

0.3921mL

1.9607mL

3.9213mL

10mM

0.1961mL

0.9803mL

1.9607mL

50mM

0.0392mL

0.1961mL

0.3921mL

 

生物活性

产品描述

一种有效且可逆的肽酰基精氨酸脱亚氨酶 4 (PAD4) 抑制剂。GSK484 hydrochloride 高亲和力与 PAD4 结合，在不存在钙的情况下 IC50 为 50nM。在 2mM 钙的存在下，IC50 为 250nM。

靶点/IC50

PAD4
(in the absence of Calcium)

50nM

 

体外研究

GSK484 demonstrates high affinity binding to the low-calcium form of PAD4 with IC50s of 50nM and 250nM in the absence of Calcium (0mM) and Calcium (2mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2mM Calcium) of benzoylarginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH3 release assay.

体内研究

To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4mg/kg daily for one week. This dose suppress 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, further supporting an improved functional status of the kidneys after GSK484 treatment. Administration of GSK484 at a dose of 4mg/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.

 

推荐实验方法(仅供参考)

激酶实验：

PAD4 is serially diluted in the presence of 10nM GSK215 in assay buffer (100mM HEPES, pH 8,50mM NaCl, 5% glycerol, 1mM CHAPS, 1 mM DTT) at varying concentrations of calcium (0,0.2,2 and 10mM). Following incubation for 50 min, apparent Kds for each calcium concentration are determined using a single site saturation curve. For IC50 determination, test compounds (e.g.,GSK484) are 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 10nM GSK215 in the same assay buffer and volume. Reactions are incubated for 50 min after which IC50 values are calculated using a fourparameter logistic equation.

 

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 15cm diameter plates to subconfluency in DMEM supplemented with 10% Foetal Bovine Serum, harvested by centrifugation and washed once in PBS/2mM EGTA. Cells are lysed in 50mM Tris-Cl, pH 7.4, 1.5mM MgCl2, 5% glycerol,150mM NaCl, 25mM NaF, 1mM Na3VO4, 0.4% NP40, 1mM DTT with protease inhibitors.Lysates are preincubated for 20 min at 4℃ with DMSO alone (2%), 100µM of GSK199,GSK484, GSK106 or 200µM Cl-amidine. Citrullination reactions are performed for 30 min at 37℃ in the presence of 2mM 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 anti-modified citrulline antibody. FLAG-PAD constructs are detected using anti-FLAG antibody.

 

动物实验:

 

Mice

The study includes two transgenic mouse models, 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 (4mg/kg). GSK484 is dissolved in 99.9% ethanol at a concentration of 25mg/mL to generate a stock solution and further diluted 1:50 in 0.9% NaCl shortly before injection of 200μL/mouse.
保存条件：
2-8℃ 充氮保存
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
购物指南
参考资料
支付方式
关于配送
售后服务
微信二维码
首页 |网站使用条款 |隐私政策 |关于我们 |营业执照 |结构式搜索
© 2001-2020 北京普西唐生物科技有限公司  天津普西唐生物医药科技有限公司
版权所有，并保留所有权利 
备案号：京ICP备17064988号-1