LRRK2-IN-1

CAS No. 1234480-84-2

LRRK2-IN-1( LRRK 2-IN-1 )

Catalog No. M10936 CAS No. 1234480-84-2

A potent LRRK2 inhibitor with IC50s of 13 nM/6 nM for wild-type/G2019S mutant LRRK2 repectively (0.1 mM ATP in the assay).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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5MG 54 In Stock
10MG 77 In Stock
25MG 159 In Stock
50MG 289 In Stock
100MG 507 In Stock
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Biological Information

  • Product Name
    LRRK2-IN-1
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent LRRK2 inhibitor with IC50s of 13 nM/6 nM for wild-type/G2019S mutant LRRK2 repectively (0.1 mM ATP in the assay).
  • Description
    A potent LRRK2 inhibitor with IC50s of 13 nM/6 nM for wild-type/G2019S mutant LRRK2 repectively (0.1 mM ATP in the assay); shows modest activity against LRRK2 A2016T (IC50=2.45 uM) and LRRK2 A2016T+G2019S mutant (IC50=3.08 uM); also inhibits DCLK1 (IC50=2.61 nM) and 2 (IC50=45 nM); induces dephosphorylation of Ser910 and Ser935 of LRRK2 and alters the cytoplasmic localisation of LRRK2.
  • In Vitro
    Wild-type and G2019S transduction results in 2.5 fold higher TR-FRET signal which can be inhibited by LRRK2-IN-1 in a dose-dependent manner with IC50 values of 0.08 μM and 0.03 μM, respectively. LRRK2-IN-1 possessed an IC50 of 45 nM for inhibition of DCLK2 and exhibits an IC50 of greater than 1 μM when evaluated in biochemical assays for AURKB, CHEK2, MKNK2, MYLK, NUAK1, and PLK1. LRRK2-IN-1 is confirmed to inhibit MAPK7 with an EC50 of 160 nM. LRRK2-IN-1 induces a dose dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. LRRK2-IN-1 is moderately cytotoxic with IC50 of 49.3 μM in HepG2 cells. LRRK2-IN-1 exhibits genotoxicity in the presence and absence of S9 at 15.6 and 3.9 μM, respectively. LRRK2-IN-1 inhibits proliferation, migration, and induces cell death with hallmarks of apoptosis of HCT116 and AsPC-1 cells.
  • In Vivo
    LRRK2-IN-1 (100 mg/kg, i.p.) induces dephosphorylation of LRRK2 in the kidney of the mice. Peritumoral injection of LRRK2-IN-1 (100 mg/kg) results in a significant decrease in tumor volume and weight of AsPC-1 tumor xenografts.
  • Synonyms
    LRRK 2-IN-1
  • Pathway
    Autophagy
  • Target
    LRRK2
  • Recptor
    DCLK1|DCLK2|LRRK2(A2016T)|LRRK2(G2019S)|LRRK2(WT)
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    1234480-84-2
  • Formula Weight
    570.6852
  • Molecular Formula
    C31H38N8O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C1N(C)C2=CN=C(NC3=CC=C(C(N4CCC(N5CCN(C)CC5)CC4)=O)C=C3OC)N=C2N(C)C6=CC=CC=C16
  • Chemical Name
    6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one, 5,11-dihydro-2-[[2-methoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dimethyl-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Deng X, et al. Nat Chem Biol. 2011 Apr;7(4):203-5. 2. Weygant N, et al. Mol Cancer. 2014 May 6;13:103. 3. Luerman GC, et al. J Neurochem. 2014 Feb;128(4):561-76.
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