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Chemical Structure : CAF-382
Catalog No.: PC-20880Not For Human Use, Lab Use Only.
CAF-382 (CDKL5 inhibitor B1) is a potent, specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) with IC50 of 11 nM in NanoBRET assays, shows no activity against GSK3β.
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CAF-382 (CDKL5 inhibitor B1) is a potent, specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) with IC50 of 11 nM in NanoBRET assays, shows no activity against GSK3β.
CAF-382 shows high CDKL5 affinity in CDKL5 split-luciferase assays with IC50 of 6.7 nM, does not inhibit CDKL2 at 10 uM.
CAF-382 has a good selectivity score (S10 (1 µM)=0.017) in the DiscoverX scanMAX panel, several CDKs (CDK9, PCTK1/CDK16, PCTK2/CDK17, PCTK3/CDK18) are potently inhibited (IC50 ≤100 nM).
CAF-382 (5 nM) caused a significant reduction in pSer222 EB2 without a change in total EB2 levels in rat primary cortical neuron cultures.
CAF-382 (100 nM) reduces EB2 phosphorylation in a dose dependent fashion in rat hippocampal slices, selectively reduces AMPA-type glutamate receptor-mediated responses post-synaptically.
CAF-382 reduces hippocampal long-term potentiation (LTP).
| M.Wt | 366.50 | |
| Formula | C16H22N4O2S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Castano A, et al. bioRxiv. 2023 Apr 24:2023.04.24.538049.
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