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CDKL2 inhibitor 9

Chemical Structure : CDKL2 inhibitor 9

CAS No.: 2471972-15-1

CDKL2 inhibitor 9

Catalog No.: PC-22396Not For Human Use, Lab Use Only.

CDKL2 inhibitor 9 is a selective cyclin-dependent kinase-like 2 (CDKL2, KKIAMRE, P56) chemical probe inhibitor with enzyme IC50 of 230 nM in radiometric enzymatic assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CDKL2 inhibitor 9 is a selective cyclin-dependent kinase-like 2 (CDKL2, KKIAMRE, P56) chemical probe inhibitor with enzyme IC50 of 230 nM in radiometric enzymatic assays.
CDKL2 inhibitor 9 exhibits IC50 of 460 nM in the CDKL2 NanoBRET assay to gauge their ability to engage CDKL2 in cells.
CDKL2 inhibitor 9 displays excellent kinome-wide selectivity against 403 wild-type human kinases with selectivity score (S10(1 µM) = 0.002), as well as high selectivity over CDKL1, CDKL3, CDKL4, or CDKL5.
CDKL2 inhibitor 9 suppressed the CDKL2-mediated EB2 phosphorylation in a dose-dependent manner in rat primary neurons.

Physicochemical Properties

M.Wt 426.54
Formula C22H26N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(6-(3-(((2-methylpropyl)sulfonamido)methyl)phenyl)-1H-indazol-3-yl)cyclopropanecarboxamide

References

1. Bashore FM, et al. bioRxiv [Preprint]. 2024 May 14:2024.05.12.593776.

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