Chemical Structure : EB‐42486
CAS No.: 2390475-81-5
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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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.
M.Wt | 414.47 | |
Formula | C22H22N8O | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4,5,7,7-Tetramethyl-N-(3-phenyl-1H-indazol-5-yl)-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxamide |
1. Albert W Garofalo, et al. J Med Chem. 2020 Dec 10;63(23):14821-14839.
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