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Submit ReviewCAF 382
Description: Potent and selective CDKL5 inhibitor
Chemical Name: N-[5-[(5-Propan-2-yl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide trifluoroacetate
Purity: ≥98% (HPLC)
Biological Activity for CAF 382
CAF 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).
Licensing Information
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.
Technical Data for CAF 382
| M. Wt | 480.52 |
| Formula | C16H22N4O2S2.CF3CO2H |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CAF 382
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 48.05 | 100 | |
| ethanol | 9.61 | 20 with gentle warming |
Preparing Stock Solutions for CAF 382
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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 |
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Product Datasheets for CAF 382
References for CAF 382
References are publications that support the biological activity of the product.
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.
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Keywords: CAF 382, CAF 382 supplier, CAF382, CDKL5, potent, selective, inhibitors, inhibits, cyclin, dependent, kinases, CDK5, Subfamily, 8105, Tocris Bioscience
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