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MilliporeSigma™ Calbiochem™ LRRK2 Inhibitor III, HG-10-102-01

Catalog No. 43819510MG Shop All MilliporeSigma Products
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43-819-510MG 10 mg
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Catalog No. 43-819-510MG Supplier MilliporeSigma™ Supplier No. 43819510MG
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Description

A cell-permeable 2,4-diaminopyrimidinyl compound that acts as a potent, ATP-competitive LRRK2-selective inhibitor (IC5050 =

A cell-permeable 2,4-diaminopyrimidinyl compound that acts as a potent, ATP-competitive LRRK2-selective inhibitor (IC5050 = 20.3, 3.2, 153.7 and 95.9 nM, respectively,against human wt LRRK2 and G2019S, A2016T, G2019S/A2016T LRRK2 mutant; [ATP] = 100μM), displaying much reduced potency against MNK2 and MLK1 (IC50 = 0.6 and 2.1μM, respectively; [ATP] = 100μM) and little activity toward a panel of 136 other kinases. Although both HG-10-102-01 and LRRK2-In-1 438193) inhibit cellular wt and G20195 LRRK2 phosphorylation (Optimal conc. 1 to 3μM), only HG-10-102-01 is effective against cellular A2016T and G2019S/A2016T LRRK2 phosphorylations (IC50 <3μM). And only HG-10-102-01, but not LRRK2-In-1 or CZC-25146 (Cat. No. 438194), can cross blood-brain-barrier for LRRK2 phosphorylation inhibition in mice (30mg/kg to 50mg/kg i.p.) in vivo .
TRUSTED_SUSTAINABILITY

Specifications

Color Off-white
Description 99% by HPLC
Target Proteins LRRK2
Molecular Formula C17H20ClN5O3
Formula Weight 377.8g/mol
Solubility DMSO
Content And Storage Protect from light
Form Powder
Quantity 10 mg
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