
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)






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10MG | 77 | In Stock |
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25MG | 159 | In Stock |
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50MG | 289 | In Stock |
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100MG | 507 | In Stock |
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Biological Information
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Product NameLRRK2-IN-1
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NoteResearch use only, not for human use.
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Brief DescriptionA potent LRRK2 inhibitor with IC50s of 13 nM/6 nM for wild-type/G2019S mutant LRRK2 repectively (0.1 mM ATP in the assay).
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DescriptionA 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.
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In VitroWild-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.
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In VivoLRRK2-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.
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SynonymsLRRK 2-IN-1
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PathwayAutophagy
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TargetLRRK2
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RecptorDCLK1|DCLK2|LRRK2(A2016T)|LRRK2(G2019S)|LRRK2(WT)
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number1234480-84-2
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Formula Weight570.6852
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Molecular FormulaC31H38N8O3
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C1N(C)C2=CN=C(NC3=CC=C(C(N4CCC(N5CCN(C)CC5)CC4)=O)C=C3OC)N=C2N(C)C6=CC=CC=C16
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Chemical Name6H-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
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Storage(-20℃)
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ShippingWith Ice Pack
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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.
molnova catalog



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