HG-10-102-01

HG-10-102-01

Catalog Number:
L002369891APE
Mfr. No.:
APE-B1262
Price:
$276
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      • Overview
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          Background

          HG-10-102-01 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with the IC50 values of 20.3nM and 3.2nM for wild type LRRK2 and LRRK2 [G1019S], respectively [1].
          HG-10-102-01 has shown the potent and selective inhibitor of LRRK2 with the IC50 values of 20.3nM, 153.7nM, 95.9nM and 3.2nM for wild type LRRK2, LRRK2 [A2016T], LRRK2 [G2019S+A1016T] and LRRK2 [G1019S], respectively. In addition, HG-10-102-01 has been reported to induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 [G2019S] stably transfected into HEK 293 cells. Moreover, it has been demonstrated that increasing doses of HG-10-102-01 led to similar dephosphorylation of endogenous LRRK2 at Ser910 and Ser935 in HEK293 cells, mouse Swiss 3T3 cells and mouse embryonic fibroblast cells [1].

          [1] Choi HG1, Zhang J, Deng X, Hatcher JM, Patricelli MP, Zhao Z, Alessi DR, Gray NS. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662. Epub 2012 Jun 18.

      • Properties
        • Alternative Name
          (E)-(4-((5-chloro-6-(methylimino)-1,6-dihydropyrimidin-2-yl)amino)-2-methoxyphenyl)(morpholino)methanone
          CAS Number
          1351758-81-0
          Molecular Formula
          C17H20ClN5O3
          Molecular Weight
          377.83
          Appearance
          A solid
          Purity
          98.59%
          Solubility
          insoluble in H2O; ≥18.9 mg/mL in DMSO; ≥7.64 mg/mL in EtOH with ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Chen ZC, Zhang W, et al. "Phosphorylation of amyloid precursor protein by mutant LRRK2 promotes AICD activity and neurotoxicity in Parkinson's disease." Sci Signal. 2017 Jul 18;10(488). pii: eaam6790. PMID:28720718

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