SML4002
SGC-CAF382-1
≥98% (HPLC)
别名:
CAF 382, CAF 382 (B1), CAF-382, CAF-382 (B1), CAF382, CAF382 (B1), N-(5-(((5-Isopropyloxazol-2-yl)methyl)thio)thiazol-2-yl)piperidine-4-carboxamide 2,2,2-trifluoroacetate
质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(NC1=NC=C(S1)SCC2=NC=C(O2)C(C)C)C3CCNCC3.[xTFA]
相关类别
生化/生理作用
Potent cyclin-dependent kinase-like 5 inhibitor with additional potency against CDK9/16/17/18 and good kinome-wide selectivity.
SGC-CAF382-1 is a potent cyclin-dependent kinase-like 5 inhibitor (CDKL5 IC50 = 6.7 nM by binding assay & 10 nM by cellular NanoBRET) with additional potency against CDK9/16/17/18 (IC50 = 20/62/89/100 nM by cell-free enzymatic assay, 280/390/240/260 nM by cellular NanoBRET) and good kinome-wide selectivity. SGC-CAF382-1 downregulates EB2 Ser222 phosphorylation in DIV14-16 rat primary neurons (IC50 <5 nM) and in hippocampal slices from P20–30 rats ex vivo (IC50 <45 nM).
SGC-CAF382-1 is a potent cyclin-dependent kinase-like 5 inhibitor (CDKL5 IC50 = 6.7 nM by binding assay & 10 nM by cellular NanoBRET) with additional potency against CDK9/16/17/18 (IC50 = 20/62/89/100 nM by cell-free enzymatic assay, 280/390/240/260 nM by cellular NanoBRET) and good kinome-wide selectivity. SGC-CAF382-1 downregulates EB2 Ser222 phosphorylation in DIV14-16 rat primary neurons (IC50 <5 nM) and in hippocampal slices from P20–30 rats ex vivo (IC50 <45 nM).
免责声明
Hygroscopic
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
Anna Castano et al.
eLife, 12 (2023-07-25)
Pathological loss-of-function mutations in cyclin-dependent kinase-like 5 (CDKL5) cause CDKL5 deficiency disorder (CDD), a rare and severe neurodevelopmental disorder associated with severe and medically refractory early-life epilepsy, motor, cognitive, visual, and autonomic disturbances in the absence of any structural brain
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