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Merck

SML4002

SGC-CAF382-1

≥98% (HPLC)

Synonym(s):

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

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

O=C(NC1=NC=C(S1)SCC2=NC=C(O2)C(C)C)C3CCNCC3.[xTFA]

Related Categories

Biochem/physiol Actions

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).

Disclaimer

Hygroscopic

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

SML4002-5MG:
SML4002-VAR:
SML4002-BULK:
SML4002-25MG:

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Certificates of Analysis (COA)

Lot/Batch Number
0000390763
0000390764
0000373723
0000390764
0000390763

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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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