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Submit ReviewGSK'872
说明： Potent and selective RIP3 kinase inhibitor
化学名： N-5-Benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-quinolinamine
纯度： ≥98% (HPLC)
生物活性 for GSK'872
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).
化合物库 for GSK'872
GSK'872 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for GSK'872
| 分子量 | 383.49 |
| 公式 | C19H17N3O2S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1346546-69-7 |
| PubChem ID | 54674134 |
| InChI Key | ZCDBTQNFAPKACC-UHFFFAOYSA-N |
| Smiles | CC(S(=O)(C1=CC2=C(N=CC=C2NC3=CC=C4SC=NC4=C3)C=C1)=O)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GSK'872
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 38.35 | 100 | |
| ethanol | 38.35 | 100 |
制备储备液 for GSK'872
以下数据基于产品分子量 383.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.61 mL | 13.04 mL | 26.08 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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产品说明书 for GSK'872
参考文献 for GSK'872
参考文献是支持产品生物活性的出版物。
Kaiser et al (2013) Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL. J.Biol.Chem. 288 31268 PMID: 24019532
Mandal et al (2014) RIP3 induces apoptosis independent of pronecrotic kinase activity. Mol.Cell 56 481 PMID: 25459880
If you know of a relevant reference for GSK'872, please let us know.
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关键词: GSK'872, GSK'872 supplier, GSK872, potent, selective, receptor, activating, protein, kinase, 3, RIP3K, inhibitors, inhibits, necroptosis, necrosis, RIPK3, Necroptosis, RIP, Kinases, 6492, Tocris Bioscience
5 篇 GSK'872 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK'872 的部分引用包括：
Lisa et al (2023) A sense-antisense RNA interaction promotes breast cancer metastasis via regulation of NQO1 expression. Nat Cancer 4 682-698 PMID: 37169843
Timothy et al (2021) RIPK1 activation mediates neuroinflammation and disease progression in multiple sclerosis. Cell Rep 35 109112 PMID: 33979622
Wulf et al (2021) Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells. Cells 10 PMID: 34831323
Tanya A et al (2020) Lytic Cell Death Mechanisms in Human Respiratory Syncytial Virus-Infected Macrophages: Roles of Pyroptosis and Necroptosis. Viruses 12 PMID: 32854254
Kyung-Min et al (2020) Combined the SMAC mimetic and BCL2 inhibitor sensitizes neoadjuvant chemotherapy by targeting necrosome complexes in tyrosine aminoacyl-tRNA synthase-positive breast cancer. Breast Cancer Res 22 130 PMID: 33239070
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GSK'872 的评论
平均评分: 5 (Based on 1 Review.)
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Effective necroptosis inhibitor.
By
JING HE on 06/28/2020
分析类型： In Vitro
种属： Human
细胞系/组织： HT-29
Working concentration using 10 nM for different incubation time in HT-29 cells and the cell death rate was measured.
