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

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 .

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