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Chemical Structure : SGC-CDKL5/GSK3-1
Catalog No.: PC-49792Not For Human Use, Lab Use Only.
CDKL5/GSK3 inhibitor 2 is a highly potent and cell-active chemical probe inhibitor of cyclindependent kinase-like 5 (CDKL5)/GSK3 (glycogen synthase kinase 3) with IC50 of 4.6/9.5/24 nM for CDKL5/GSK3⍺/GSK3β, respectively.
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SGC-CDKL5/GSK3-1 is a highly potent and cell-active chemical probe inhibitor of cyclindependent kinase-like 5 (CDKL5)/GSK3 (glycogen synthase kinase 3) with IC50 of 4.6/9.5/24 nM for CDKL5/GSK3⍺/GSK3β, respectively.
SGC-CDKL5/GSK3-1 displays exquisitely selectivity against CDKL family (CDKL1/2/3) and the Eurofins DiscoverX scanMAX panel including 403 wild-type (WT) human as well as several mutant and non-human kinases.
SGC-CDKL5/GSK3-1 potently inhibits CDKL5 kinase activity and downstream signaling, demonstrates canonical ATP-competitive binding to CDKL5.
SGC-CDKL5/GSK3-1 (5 nM) inhibits phosphorylation of EB2 and phospho-β-catenin in DIV15-16 cortical primary rat neurons.
SGC-CDKL5/GSK3-1 promotes survival of motor neurons in response to ER stress, which is a hallmark of neurodegenerative diseases like ALS.
| M.Wt | 349.34 | |
| Formula | C16H17F2N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ong HW, et al. bioRxiv. 2023 Feb 10:2023.02.09.527935.
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