[CAS NO. 1234480-84-2] LRRK2-IN-1

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PRODUCTS SPECIFICATIONS [1234480-84-2]

Catalog

SLK-S7584

Brand

Selleck

CAS

1234480-84-2

DESCRIPTION [1234480-84-2]

Overview

MDL	MFCD22683805
Molecular Weight	570.69
Molecular Formula	C31H38N8O3
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

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7523 mL	8.7613 mL	17.5226 mL
5 mM	0.3505 mL	1.7523 mL	3.5045 mL
10 mM	0.1752 mL	0.8761 mL	1.7523 mL
50 mM	0.0350 mL	0.1752 mL	0.3505 mL

Description

LRRK2-IN-1 is a potent and selective inhibitor with of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

Targets

LRRK2 (G2019S) ^[1] (Cell-free assay)	LRRK2 (WT) ^[1] (Cell-free assay)	DCLK2 ^[1] (Cell-free assay)
6 nM	13 nM	45 nM

In vitro

In HEK 293 cells stably expressing GFP-LRRK2[G2019S], LRRK2-IN-1 alters the cytoplasmic localization of LRRK2. In human-derived neuroblastoma SHSY5Y cells and mouse Swiss 3T3 cells, LRRK2-IN-1 induces a similar dose-dependent Ser910 and Ser935 dephosphorylation and loss of 14-3-3 binding to endogenous LRRK2. In transgenic C. elegans expressing human R1441C- and G2019S-LRRK2, LRRK2-IN1 rescues the behavioral deficit characteristic of dopaminergic impairment. In mouse fibroblasts, LRRK2-IN1 reduces cell motility. In AsPC-1 and HCT116 cell lines, LRRK2-IN-1 shows anti-proliferative and pro-apoptotic properties, induces G1 and G2/M cell cycle arrest and inhibits DCLK1 mRNA and protein expression.

In vivo

In wild type male C57BL/6 mice, LRRK2-IN-1 (100 mg/kg, i.p.) inhibits Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, while no effects in the brain.

References

[1] Deng X, et al. Nat Chem Biol. 2011, 7(4), 203-205.
[2] Yao C, et al. Hum Mol Genet. 2013, 22(2), 328-344.
[3] Caesar M, et al. Neurobiol Dis. 2013, 54, 280-288.
[4] Weygant N, et al. Mol Cancer. 2014, 13, 103.