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GSK2983559 free acid {[allProObj[0].p_purity_real_show]}

货号:A939659 同义名: GSK2983559;compound 3

GSK2983559 free acid is a small-molecule inhibitor of RIP2 kinase. GSK2983559 free acid potently binds to RIP2 kinase with good kinase specificity and has excellent activity in blocking many proinflammatory cytokine responses in vivo .

GSK2983559 free acid 化学结构 CAS号:1579965-12-0
GSK2983559 free acid 化学结构
CAS号:1579965-12-0
GSK2983559 free acid 3D分子结构
CAS号:1579965-12-0
GSK2983559 free acid 化学结构 CAS号:1579965-12-0
GSK2983559 free acid 3D分子结构 CAS号:1579965-12-0
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GSK2983559 free acid 纯度/质量文件 产品仅供科研

货号:A939659 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 NF-κB 其他靶点 纯度
PDTC ammonium 98%
QNZ ++++

NF-κB, IC50: 11 nM

99%+
Sodium 4-Aminosalicylate Dihydrate 98%
Sodium Salicylate 95%
Parthenolide p53 97% HPLC
JSH-23 +

NF-κB, IC50: 7.1 μM

98%
Phenethyl caffeate 98%
Andrographolide 98+%
Curcumin HDAC,Nrf2 98%
SC75741 +++

NF-κB, EC50: 200 nM

99%+
CBL0137 HCl ++

NF-κB, EC50: 0.47 μM

p53 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

GSK2983559 free acid 生物活性

描述 Receptor-interacting-protein kinase 2 (RIP2) has been identified as a key signal transduction partner in the nucleotide oligomerization domain 2 (NOD2) pathway contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. GSK2983559 is the first RIP2 kinase inhibitor to enter clinical trials, currently under phase 1 evaluation. VEGFR3 was the only kinase inhibited by more than 90% by GSK2983559. An additional 11 kinases were inhibited in the range of 70−89%. In a screen against non-kinase targets (Eurofins, 104 receptor and ion channel binding assays and 35 enzyme and cell-based assays), GSK2983559 was highly selective, inhibiting only melatonin receptor MT3 at a concentration under 10 μM. The in vivo efficacy of GSK2983559 was evaluated in a murine 2,4,6-trinitrobenzenesulfonic acid (TNBS) induced colitis model. Mice were dosed orally from days −2 to 5 at 0.25, 7.5, and 145 mg/kg b.i.d. which corresponds to predicted 10%, 50%, and 90% inhibition at 24 h, respectively. Further, administration of GSK2983559 at the 7.5 and 145 mg/kg b.i.d. doses exhibited efficacy similar to that of prednisolone as measured by summed colon scores[1].

GSK2983559 free acid 参考文献

[1]Haile PA, Casillas LN, Votta BJ, et al. Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases. J Med Chem. 2019;62(14):6482-6494

GSK2983559 free acid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.28mL

1.86mL

0.93mL

18.57mL

3.71mL

1.86mL

GSK2983559 free acid 技术信息

CAS号1579965-12-0
分子式C21H23N4O7PS2
分子量 538.534
别名 GSK2983559;compound 3;RIPK2-IN-1;RIP2 kinase inhibitor 1
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 4 mg/mL(7.43 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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