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IACS-52825

Chemical Structure : IACS-52825

CAS No.: 2640376-72-1

IACS-52825 (IACS52825, IACS 52825)

Catalog No.: PC-20983Not For Human Use, Lab Use Only.

IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.
IACS-52825 shows no significant inhibition of the hERG channel or CYP P450 enzymes and no significant activities against an 80-member Eurofins CEREP panel of various ion channels and receptors or a 403-member Eurofins DiscoverX kinase panel.
IACS-52825 (orally once daily at 3, 10, or 30 mg/kg) dose-dependently reverses cisplatin-induced mechanical allodynia.

Physicochemical Properties

M.Wt 426.29
Formula C16H13F7N4O2
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

(R)-1-(4-(6-Amino-5-(trifluoromethoxy)pyridin-3-yl)-1-(3-fluorobicyclo[1.1.1]pentan-1-yl)-1H-imidazol-2-yl)-2,2,2-trifluoroethanol

References

1. Kang Le, et al. J Med Chem. 2023 Jul 12. doi: 10.1021/acs.jmedchem.3c00788.

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