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Submit ReviewGSK 583 is a potent RIPK2 inhibitor (IC50 values are 2 and 5 nM at rat and human kinases, respectively). Displays selectivity for RIP2K over p38α, VEGFR2 and a panel of 300 kinases. Exhibits some inhibition at BRK and Aurora A. Also displays similar binding affinity, but no detectable functional activity at RIP3. Active in vivo. Moderately orally bioavailable and cell permeable.
分子量 | 398.45 |
公式 | C20H19FN4O2S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1346547-00-9 |
PubChem ID | 67469084 |
InChI Key | XLOGLWKOHPIJLV-UHFFFAOYSA-N |
Smiles | CC(C)(S(=O)(C1=CC2=C(N=CC=C2NC3=NNC4=CC=C(C=C34)F)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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.84 | 100 | |
ethanol | 7.97 | 20 |
以下数据基于产品分子量 398.45。 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 | 2.51 mL | 12.55 mL | 25.1 mL |
5 mM | 0.5 mL | 2.51 mL | 5.02 mL |
10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
参考文献是支持产品生物活性的出版物。
Haile et al (2016) The identification and pharmacological characterization of 6-(tert-butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a highly potent and selective inhibitor of RIP2 kinase. J.Med.Chem. 59 4867 PMID: 27109867
If you know of a relevant reference for GSK 583, please let us know.
关键词: GSK 583, GSK 583 supplier, GSK583, Potent, RIP2, kinase, inhibitors, inhibits, oral, bioavailability, cell, permeable, receptor-interacting, protein, 1, RIP, Kinases, 6480, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GSK 583 的部分引用包括:
Rui et al (2021) Integrated transcriptomic analysis of human tuberculosis granulomas and a biomimetic model identifies therapeutic targets. J Clin Invest 131 PMID: 34128839
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