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 .
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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 | ✔ | Nrf2,HDAC | 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。 |
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]. |
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 |
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 |
动物实验配方 |