GNE684

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GNE684 

GNE684 是一种有效的受体相互作用蛋白 1 (RIP1) 抑制剂，作用于人类、小鼠与大鼠 RIP1 的 Kiapp 值分别为 21 nM、189 nM 和 691 nM。

GNE684

GNE684 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively[1].

IC50 & Target

IC50: 21 nM (human RIP1), 189 nM (mouse RIP1), 691 nM (rat RIP1)[1]
体外研究
(In Vitro)

GNE684 (20 μM; 20 hours) inhibits RIP1 kinase driven cell death effectively in several human and mouse cell lines[1].
GNE684 (20 μM; 0-60 minutes) disrupts TBZ (2 μM BV6, 20 ng/ml TNF, 20 μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: L929 cells, Jurkat cells, MEFs
Concentration: 20 μM
Incubation Time: 20 hours
Result: Inhibited RIP1 kinase driven cell death effectively in several human and mouse cell lines.

Western Blot Analysis[1]

Cell Line: HT-29 cells, J774A.1 cells
Concentration: 0 μM, 20 μM
Incubation Time: 0 minute, 15 minutes, 60 minutes
Result: Disrupted TBZ (2 μM BV6, 20 ng/ml TNF, 20μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.

体内研究
(In Vivo)

GNE684 also had no impact on overall survival or tumor growth in the KPP or KPR (LSL-Kras G12D/+; p16/p19 fl/wt ; Trp53 R270H/wt ; Pdx1-cre) PDAC models[1].
GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nemofl/fl Villin.creERT2 mice (NEMO IEC-KO)[1]
Dosage: 50 mg/kg
Administration: Oral administration; twice daily; from days 2–6 treated with tamoxifen
Result: Almost completely protected the NEMO-deficient intestines from colitis and ileitis.

分子量

432.48

Formula

C23H24N6O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Patel S, et al. RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases. Cell Death Differ. 2019 May 17.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务