SML4091
SGC-CDKL5/GSK3-1
≥98% (HPLC)
Synonym(s):
4-(3,5-Difluorobenzamido)-N-(piperidin-4-yl)-1H-pyrazole-3-carboxamide, 4-[(3,5-Difluorobenzoyl)amino]-N-4-piperidinyl-1H-pyrazole-3-carboxamide
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C(NC1CCNCC1)C2=NNC=C2NC(C3=CC(F)=CC(F)=C3)=O
Biochem/physiol Actions
Potent cyclin-dependent kinase-like 5 (CDKL5) and glycogen synthase kinase-3 (GSK3⍺/β) inhibitor with good kinome-wide selectivity.
SGC-CDKL5/GSK3-1 is a potent cyclin-dependent kinase-like 5 and glycogen synthase kinase-3 inhibitor (CDKL5/GSK3⍺/GSK3β IC50 = 6.5/4/9 nM by cell-free enzymatic assay, 3.5/10/35 nM by cellular NanoBRET) with good kinome-wide selectivity. SGC-CDKL5/GSK3-1 protects iPSC-derived motor neurons from ER stress-induced death.
SGC-CDKL5/GSK3-1 is a potent cyclin-dependent kinase-like 5 and glycogen synthase kinase-3 inhibitor (CDKL5/GSK3⍺/GSK3β IC50 = 6.5/4/9 nM by cell-free enzymatic assay, 3.5/10/35 nM by cellular NanoBRET) with good kinome-wide selectivity. SGC-CDKL5/GSK3-1 protects iPSC-derived motor neurons from ER stress-induced death.
Regulatory Information
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