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CLK1 inhibitor 25

Chemical Structure : CLK1 inhibitor 25

CAS No.: 2123491-32-5

CLK1 inhibitor 25

Catalog No.: PC-21433Not For Human Use, Lab Use Only.

CLK1 inhibitor 25 is a potent and selective inhibitor of cdc2-like kinase 1 (CLK1) with IC50 of 2 nM, 69-fold selective over DYRK1A.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CLK1 inhibitor 25 is a potent and selective inhibitor of cdc2-like kinase 1 (CLK1) with IC50 of 2 nM, 69-fold selective over DYRK1A.
CLK1 inhibitor 25 also potently inhibits CLK2 (IC50: 31 nM) and CLK4 (IC50: 8 nM).
CLK1 inhibitor 25 displays at least 110-fold selectivity toward CLK1 over 351 of the 357 kinases tested (98.32%), does not show obvious activity against 292 kinases (IC50>10 μM).
CLK1 inhibitor 25 (10 uM) alters the location and redistribution of SR proteins in BNL CL.2 cells.
CLK1 inhibitor 25 induces autophagy in in vitro assays and displays significant hepatoprotective effects in the acetaminophen (APAP)-induced liver injury mouse model.

Physicochemical Properties

M.Wt 409.42
Formula C24H16FN5O
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

(S)-5-(1-(1-(4-fluorophenyl)ethyl)-1H-[1,2,3]triazolo[4,5-c]quinolin-8-yl)benzo[d]oxazole

References

1. Sun QZ, et al. J Med Chem. 2017 Jul 27;60(14):6337-6352.

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