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LRRK2-IN-1

Chemical Structure : LRRK2-IN-1

CAS No.: 1234480-84-2

LRRK2-IN-1 (LRRK2 inhibitor)

Catalog No.: PC-42726Not For Human Use, Lab Use Only.

LRRK2-IN-1 is 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).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

LRRK2-IN-1 is 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).
LRRK2-IN-1 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).
LRRK2-IN-1 induces dephosphorylation of Ser910 and Ser935 of LRRK2 and alters the cytoplasmic localisation of LRRK2.

Physicochemical Properties

M.Wt 570.6852
Formula C31H38N8O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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-

References

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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