GSK872
- CAS No.
- 1346546-69-7
- Chemical Name:
- GSK872
- Synonyms
- GSK872;CS-2489;GSK2399872A;GSK'872 (GSK2399872A);GSK-872;GSK 872;GSK872;GSK'872;GSK872;GSK2399872A;N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine;N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine;N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine;4-Quinolinamine, N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-
- CBNumber:
- CB03165850
- Molecular Formula:
- C19H17N3O2S2
- Molecular Weight:
- 383.49
- MDL Number:
- MFCD30481302
- MOL File:
- 1346546-69-7.mol
- MSDS File:
- SDS
| Boiling point | 625.7±55.0 °C(Predicted) |
|---|---|
| Density | 1.395±0.06 g/cm3(Predicted) |
| storage temp. | Keep in dark place,Inert atmosphere,Room temperature |
| solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| pka | 5.53±0.49(Predicted) |
| form | solid |
| color | Off-White or pale yellow |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501 | |||||||||
| NFPA 704 |
|
GSK872 price More Price(21)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 23300 | GSK872 ≥98% | 1346546-69-7 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 23300 | GSK872 ≥98% | 1346546-69-7 | 5mg | $116 | 2024-03-01 | Buy |
| Cayman Chemical | 23300 | GSK872 ≥98% | 1346546-69-7 | 10mg | $214 | 2024-03-01 | Buy |
| Tocris | 6492 | GSK'872 ≥98%(HPLC) | 1346546-69-7 | 10 | $169 | 2021-12-16 | Buy |
| Tocris | 6492 | GSK'872 ≥98%(HPLC) | 1346546-69-7 | 50 | $710 | 2021-12-16 | Buy |
GSK872 Chemical Properties,Uses,Production
Description
GSK 872 (CAS 1346546-69-7) is a potent (IC50 = 1.8nM domain binding; IC50 = 1.3 nM kinase activity) and selective inhibitor of receptor interacting protein 3 (RIP3).1 It is able to prevent necroptosis, virus-induced necrosis, and TLR3-induced necrosis.1,2 GSK872 can induce Caspase8-mediated apoptosis at higher concentrations (e.g.3 μM).2
Uses
GSK''872 is a potent and selective receptor activating protein kinase 3 (RIP3) inhibitor (IC50 = 1.3 nM). Exhibits >1000-fold selectivity for RIP3 over a panel of 300 other kinases including RIP1. Inhibits TNF-induced cell death in 3T3-SA cells and TLR3-induced necrosis in fibroblasts in vitro. Blocks necroptosis of primary human neutrophils from whole blood. Also induces apoptosis at higher concentrations (3 - 10 μM).
Biological Activity
GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
in vitro
When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death.
in vivo
GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo.
storage
-20°C
References
1)?Kaiser et al. (2013) Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL; J. Biol. Chem.?288 31279 2)?Mandal et al. (2014) RIP3 induces apoptosis independent of pro-necrotic kinase activity; Mol. Cell 56 481
GSK872 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| 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 | 10523 | 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 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Suzhou Ran enzyme Biotechnology Co., Ltd. | 0512-0512-62793604 18015430729 | 116667374@qq.com | China | 117 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 |