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Submit ReviewGSK 626616
说明： Potent and selective DYRK inhibitor; orally bioavailable.
化学名： (5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone
纯度： ≥95% (HPLC)
生物活性 for GSK 626616
GSK 626616 is a potent and selective DYRK inhibitor (IC50 = 0.7 nM for DYRK3, similar potency for DYRK1 and 2). Exhibits ~20-fold selectivity over casein kinase 2 and negligible activity against a panel of 451 kinases screened. Enhances number of CFU-E stimulated by Epo from human marrow. Increases hemoglobin levels in anemic mice. Orally bioavailable.
技术数据 for GSK 626616
| 分子量 | 401.27 |
| 公式 | C18H10Cl2N4OS |
| 储存 | Store at +4°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 1025821-33-3 |
| PubChem ID | 135416229 |
| InChI Key | RJPNRXFBYZVRIB-DHDCSXOGSA-N |
| Smiles | O=C(N=C(NC1=C(Cl)C=CC=C1Cl)S/2)C2=C\C3=CC=C(N=CC=N4)C4=C3 |
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 626616
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 40.13 | 100 |
制备储备液 for GSK 626616
以下数据基于产品分子量 401.27。 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 | 2.49 mL | 12.46 mL | 24.92 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.98 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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产品说明书 for GSK 626616
参考文献 for GSK 626616
参考文献是支持产品生物活性的出版物。
Erickson-Miller et al (2007) GSK626616: A DYRK3 inhibitor as a potential new therapy for the treatment of anemia. Blood 110 510
Wippich et al (2013) Dual specificity kinase DYRK3 couples stress granule condensation/dissolution to mTORC1 signaling. Cell 152 791 PMID: 23415227
Rai et al (2018) Kinase-controlled phase transition of membraneless organelles in mitosis. Nature 559 211 PMID: 29973724
If you know of a relevant reference for GSK 626616, please let us know.
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关键词: GSK 626616, GSK 626616 supplier, GSK626616, potent, dyrk1, dyrk2, dyrk3, dual, specificity, tyrosine, phosphorylation, regulated, kinases, inhibitors, inhibits, selective, DYRK, 6638, Tocris Bioscience
1 篇 GSK 626616 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK 626616 的部分引用包括：
Scott R et al (2019) Mammalian cell growth dynamics in mitosis. Elife 8 PMID: 31063131
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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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