EB-42486 | G2019S-LRRK2 inhibitor | Probechem Biochemicals

Chemical Structure : EB-42486

CAS No.: 2390475-81-5

EB-42486 (EB42486)

Catalog No.: PC-72160Not 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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1 mg	$148	In stock
5 mg	$298	In stock
10 mg	$488	In stock
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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	414.473
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.

EB-42486 (EB42486)

Biological Activity

Physicochemical Properties

References

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