EB-42486 | G2019S-LRRK2 inhibitor | Probechem Biochemicals

Chemical Structure : EB-42486

CAS No.: 2390475-81-5

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EB-42486 (EB42486)

货号: 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.

规格	价格	库存
1 mg	￥1480	In stock
5 mg	￥2980	In stock
10 mg	￥4880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	414.473
分子式	C22H22N8O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

EB-42486 (EB42486)

生物&药学活性

物理化学性质&存储条件

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EB-42486 (EB42486)

生物&药学活性

物理化学性质&存储条件

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