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Submit ReviewCAF 382 is potent and selective CDKL5 (cyclin-dependent kinase-like 5) inhibitor (IC50 = 10 nM). Exhibits nearly 100-fold selectivity for CDKL5 over CDKL2, low inhibition for CDKL3 and CDKL4 (IC50 = 2.1-2.7 µM), and no inhibition for CDKL1. CAF 382 lacks GSK3β activity. It causes a significant reduction in pSer222 EB2 at 5 nM without a change in total EB2 levels in rat primary cortical neuron cultures. CAF 382 is an analog of SNS 032 (Cat. No. 4075).
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC-CAF382-1 probe summary on the SGC website.
分子量 | 480.52 |
公式 | C16H22N4O2S2.CF3CO2H |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
InChI Key | CZYALDCQIWYWJJ-UHFFFAOYSA-N |
Smiles | O=C(C1CCNCC1)NC2=NC=C(SCC3=NC=C(C(C)C)O3)S2.O=C(O)C(F)(F)F |
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 | 48.05 | 100 | |
ethanol | 9.61 | 20 温和加热 |
以下数据基于产品分子量 480.52。 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 | 2.08 mL | 10.41 mL | 20.81 mL |
5 mM | 0.42 mL | 2.08 mL | 4.16 mL |
10 mM | 0.21 mL | 1.04 mL | 2.08 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Castano et al (2023) Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology. Elife 12 e88206 PMID: 37490324
If you know of a relevant reference for CAF 382, please let us know.
关键词: CAF 382, CAF 382 supplier, CAF382, CDKL5, potent, selective, inhibitors, inhibits, cyclin, dependent, kinases, CDK5, Subfamily, 8105, Tocris Bioscience
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