GSK840
- CAS No.
- 2361146-30-5
- Chemical Name:
- GSK840
- Synonyms
- GSK840;tert-butyl2-(4-(5-(methylcarbamoyl)-1H-benzo[d]im;tert-butyl 2-(4-(5-(methylcarbamoyl)-1H-benzo[d]imidazol-1-yl)phenyl)acetate;Inhibitor,RIP kinase,GSK 840,Receptor-interacting protein kinases,GSK840,inhibit,GSK-840,RIPK;Benzeneacetic acid, 4-[5-[(methylamino)carbonyl]-1H-benzimidazol-1-yl]-, 1,1-dimethylethyl ester
- CBNumber:
- CB95419747
- Molecular Formula:
- C21H23N3O3
- Molecular Weight:
- 365.43
- MDL Number:
- MOL File:
- 2361146-30-5.mol
GSK840 Chemical Properties,Uses,Production
Uses
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM[1].
Biological Activity
GSK840 is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, binds with high affinity to the RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
in vitro
GSK840 (GSK'840) (0.01-3 μM; 24 hours) blocks TNF-induced necroptosis in a concentration-dependent manner.
GSK840 binds the kinase domain and inhibits kinase activity with high specificity, targeting a broader range of pro-necrotic stimuli than can be achieved with RIP1 kinase inhibitors.
Cell Viability Assay
| Cell Line: | Human HT-29 cells (TNF 10 ng/ml + zVAD-fmk 20 μM + SMAC007 100 nM) |
| Concentration: | 0.01-3 μM |
| Incubation Time: | 24 hours |
| Result: | Blocked TNF-induced necroptosis in a concentration-dependent manner. |
target
IC50: 0.3 nM (RIP3)
References
[1] Mandal P, et al. RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol Cell. 2014 Nov 20;56(4):481-95. DOI:10.1016/j.molcel.2014.10.021
GSK840 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK840 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49732 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Jilin Chinese Academy of Sciences-yanshen Technology | +undefined18143011203 | info@chemextension.com | China | 42056 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8011 | 62 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 18892239720 | psaitong@jm-bio.com | China | 12306 | 58 |
| Yujinpharma(Tianjin) Technology Co.,Ltd. | 13370351217 kungfu1217@1 | kungfu1217@163.com | China | 8976 | 58 |