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Submit ReviewAZ Dyrk1B 33 is a potent and selective ATP-competitive Dyrk1B kinase inhibitor (IC50 = 7 nM); displays distinct cellular effects when compared to DYRK1B knockdown through siRNA. Demonstrates cellular in vitro activity (IC50 = 194 nM). Exhibits better selectivity than AZ 191 (Cat. No 5232); displays no off-target effects against a panel of 124 kinases tested (no kinase was inhibited above 50% at 1 μM).
AZ Dyrk1B 33 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。
分子量 | 300.36 |
公式 | C19H16N4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1679330-37-0 |
PubChem ID | 118735338 |
InChI Key | CZCUSHJQJWKYTD-UHFFFAOYSA-N |
Smiles | CC1=NC=CC(C2=CN(CC3=CC=CC=C3)C4=CN=CC=C42)=N1 |
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 | |||
1eq. HCl | 30.04 | 100 | |
DMSO | 30.04 | 100 |
以下数据基于产品分子量 300.36。 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 | 3.33 mL | 16.65 mL | 33.29 mL |
5 mM | 0.67 mL | 3.33 mL | 6.66 mL |
10 mM | 0.33 mL | 1.66 mL | 3.33 mL |
50 mM | 0.07 mL | 0.33 mL | 0.67 mL |
参考文献是支持产品生物活性的出版物。
Kettle et al (2015) Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. J.Med.Chem. 58 2834 PMID: 25738750
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关键词: AZ Dyrk1B 33, AZ Dyrk1B 33 supplier, AZDyrk1B33, Dyrk1B, kinase, inhibitors, inhibits, dual, specificity, tyrosine, phosphorylation, regulated, kinases, potent, DYRK, 5632, Tocris Bioscience
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.