438195 | LRRK2 Inhibitor III, HG-10-102-01 - Calbiochem

438195
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      Overview

      Replacement Information

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      438195-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA 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] = 100 µM), displaying much reduced potency against MNK2 and MLK1 (IC50 = 0.6 and 2.1 µM, respectively; [ATP] = 100 µM) and little activity toward a panel of 136 other kinases. Although both HG-10-102-01 and LRRK2-In-1 (Cat. No. 438193) inhibit cellular wt and G20195 LRRK2 phosphorylation (Optimal conc. 1 to 3 µM), only HG-10-102-01 is effective against cellular A2016T and G2019S/A2016T LRRK2 phosphorylations (IC50 <3 µM). 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 (30 mg/kg to 50 mg/kg i.p.) in vivo.
          Catalogue Number438195
          Brand Family Calbiochem®
          SynonymsLeucine-Rich Repeat Kinase 2 Inhibitor III, Mixed-Lineage Kinase 1 Inhibitor I, MLK1 Inhibitor I, MNK Inhibitor III, (4-(5-Chloro-4-(methylamino)pyrimidin-2-ylamino)-3-methoxyphenyl)(morpholino)methanone
          References
          ReferencesChoi, H.G., et al. 2012. ACS Med. Chem. Lett. 3, 658.
          Product Information
          FormOff-white powder
          Hill FormulaC₁₇H₂₀ClN₅O₃
          Chemical formulaC₁₇H₂₀ClN₅O₃
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetLRRK2
          Primary Target IC<sub>50</sub>20.3, 3.2, 153.7 and 95.9 nM, respectively, against Nictide phosphorylation by recombinant human wt LRRK2 and G2019S, A2016T, G2019S/A2016T LRRK2 mutant constructs
          Purity≥99% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          References

          Reference overview
          Choi, H.G., et al. 2012. ACS Med. Chem. Lett. 3, 658.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision28-March-2013 JSW
          SynonymsLeucine-Rich Repeat Kinase 2 Inhibitor III, Mixed-Lineage Kinase 1 Inhibitor I, MLK1 Inhibitor I, MNK Inhibitor III, (4-(5-Chloro-4-(methylamino)pyrimidin-2-ylamino)-3-methoxyphenyl)(morpholino)methanone
          DescriptionA cell-permeable 2,4-diaminopyrimidinyl compound that acts as a potent, ATP-competitive LRRK2-selective inhibitor (IC50 = 20.3, 3.2, 153.7 and 95.9 nM, respectively, against Nictide phosphorylation by recombinant human wt LRRK2 and G2019S, A2016T, G2019S/A2016T LRRK2 mutant constructs; [ATP] = 100 µM), displaying much reduced potency against MNK2 and MLK1 (IC50 = 0.6 and 2.1 µM, respectively; [ATP] = 100 µM) and little or no activity toward a panel of 136 other kinases. While both HG-10-102-01 and LRRK2-IN-1 (Cat. No. 438193) inhibit Ser910/Ser395 phosphorylation of wt and G20195 LRRK2 in human and murine cultures with similar potency (Optimal conc. 1 to 3 µM), only HG-10-102-01 is effective toward cellular phosphorylation of A2016T and G2019S/A2016T LRRK2 mutants (IC50 <3 µM). And only HG-10-102-01, but not LRRK2-IN-1 or CZC-25146 (Cat. No. 438194), can cross blood-brain-barrier and effectively inhibit brain LRRK2 phosphorylation in mice (by 40% and 70%, respectively, 1 h after i.p. dose of 30 mg/kg and ≥50 mg/kg) in vivo despite its low metabolic stability both in vitro (T1/2 = 13 min in mouse liver microsome) and in vivo (Plasma T1/2 = 0.13 h and AUClast = 74.85 h·ng/mL; 1 mg/kg via i.v.).
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₂₀ClN₅O₃
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesChoi, H.G., et al. 2012. ACS Med. Chem. Lett. 3, 658.