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EB‐42486

Chemical Structure : EB‐42486

CAS No.: 2390475-81-5

EB‐42486 (EB42486)

Catalog No.: PC-21887Not For Human Use, Lab Use Only.

EB‐42486 is a potent, selective G2019S-LRRK2 kinase inhibitor with IC50 of 3.1 nM (pS935-LRRK2) in FRET-based assay, >300-fold selective over WT-LRRR2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EB‐42486 is a potent, selective G2019S-LRRK2 kinase inhibitor with IC50 of 3.1 nM (pS935-LRRK2) in FRET-based assay, >300-fold selective over WT-LRRR2.
EB‐42486 potently inhibits pS1292-LRRK2 G2019S in Meso Scale Discovery (MSD) electrochemiluminescence assay with IC50 of 1.7 nM, 70-fold selective over WT LRRK2.
EB‐42486 exhibits impressive kinome selectivity against a panel of 409 kinases at 100 nM.
EB‐42486 inhibits phosphorylation of the LRRK2 substrate, Rab10, 344-fold more potently in the G2019S-LRRK2 overexpression line with IC50 of 11.4 nM, compared to that in the WT-LRRK2 overexpression line.
EB‐42486 inhibits pS935-LRRK2 837-fold more potently in the G2019S-LRRK2 line (IC50 = 2.5 nM) compared to that in the WT-LRRK2 line.

Physicochemical Properties

M.Wt 414.47
Formula C22H22N8O
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

4,5,7,7-Tetramethyl-N-(3-phenyl-1H-indazol-5-yl)-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxamide

References

1. Albert W Garofalo, et al. J Med Chem. 2020 Dec 10;63(23):14821-14839.

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