CID 2011756
产品说明书
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同义名 : | - |
| CAS号 : | 638156-11-3 | |
| 货号 : | A576631 | |
| 分子式 : | C22H21ClN2O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 396.867 | |
| MDL号 : | MFCD04094273 | |
| 存储条件： |
Pure form Sealed in dry,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 18 mg/mL(45.36 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Protein kinase D (PKD) is a novel family of serine/threonine kinases regulated by diacylglycerol, which is involved in multiple cellular processes and various pathological conditions[2]. CID 2011756 is an ATP competitive PKD inhibitor, with an IC50 of 3.2 µM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitory activity against PKD2 and PKD3 (IC50, 0.6 and 0.7 µM, respectively)[2]. Confirmed in vitro PKD1 inhibitors are then evaluated for their ability to inhibit the phosphorylation of endogenously expressed PKD1 ser916, an indicator of cellular PKD1 kinase activity. Results shows that CID 2011756 inhibites the phosphorylation of Ser916-PKD1 at levels greater than 50%. CID 2011756 is the most potent of the inhibitors with a cellular EC50 of 10 ± 0.7 µM (n = 3). Moreover, we counter screened 2011756 in IMAP-based CDK7, AKT and PLK1 assays, and find no kinase inhibition at concentrations up to 50 µM[2]. Moreover, preliminary in vitro data suggests that our most potent cell active PKD1 inhibitor, CID 2011756, has pan-PKD inhibitory effects (pKD2 IC50 = 0.6 ± 0.1; pKD3 IC50 = 0.7 ± 0.2 µM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.60mL 2.52mL 1.26mL |
25.20mL 5.04mL 2.52mL |
| 参考文献 |
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