GSK481
- CAS No.
- 1622849-58-4
- Chemical Name:
- GSK481
- Synonyms
- GSK481;CS-2186;GSK481 - GSK'481;GSK481,inhibit,Inhibitor,RIPK,GSK-481,RIP kinase,GSK 481,Receptor-interacting protein kinases;(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide;3-Isoxazolecarboxamide, 5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-
- CBNumber:
- CB03122822
- Molecular Formula:
- C21H19N3O4
- Molecular Weight:
- 377.39
- MDL Number:
- MOL File:
- 1622849-58-4.mol
- MSDS File:
- SDS
GSK481 price More Price(20)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | SML2745 | GSK′481 ≥98% (HPLC) | 1622849-58-4 | 5MG | $150 | 2024-03-01 | Buy |
Sigma-Aldrich | SML2745 | GSK′481 ≥98% (HPLC) | 1622849-58-4 | 25MG | $593 | 2024-03-01 | Buy |
Cayman Chemical | 20308 | GSK481 ≥98% | 1622849-58-4 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 20308 | GSK481 ≥98% | 1622849-58-4 | 5mg | $139 | 2024-03-01 | Buy |
Cayman Chemical | 20308 | GSK481 ≥98% | 1622849-58-4 | 10mg | $243 | 2024-03-01 | Buy |
GSK481 Chemical Properties,Uses,Production
Biological Activity
gsk481 is a receptor interacting protein kinase 1 (rip1) inhibitor.the role of rip1 kinase in tumor necrosis factor mediated inflammation has resulted in its emergence as a promising target for the treatment of multiple inflammatory diseases.
in vitro
previous study showed that gsk481 could not only trigger an increase in biochemical activity but also exhibit great translation in the u937 cellular assay with ic50 of 10 nm. moreover, gsk481 also showed complete specificity for rip1 kinase against all other tested kinases when profiled over both a p33 radiolabeled assay screen. in tight-binding adp-glo ic50 evaluation with increasing atp concentration, gsk481 exhibited a shift to lower potency, which was corresponding to a competitive model. in addition, gsk481 was also found to be a potent inhibitor of s166 phosphorylation in wild-type human rip1 but was ineffective at reducing s166 phosphorylation for wild-type mouse rip1. gsk481 was also able to more potently inhibit ser166 phosphorylation in all three tested mouse rip1 mutants than in wild-type mouse [1].
target
Target | Value |
RIP1 |
IC 50
1.3 nm for rip1
References
[1] harris pa et al. dna-encoded library screening identifies benzo[b][1,4]oxazepin-4-ones as highly potent and monoselective receptor interacting protein 1 kinase inhibitors. j med chem, 2016 mar 10, 59(5):2163-78.
GSK481 Preparation Products And Raw materials
Raw materials
Preparation Products
GSK481 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
Chemtour Biotech Co., Ltd | +8617327281506 | market@chemtour.com | China | 1460 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
HangZhou YuHao Chemical Technology Co., Ltd. | 0571-82693216 | info@yuhaochemical.com | China | 2029 | 58 |