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), also induces cell cycle arrest and cancer cell death by specifically binding to human proliferating cell nuclear antigen (PCNA) in cancer cells.
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), also induces cell cycle arrest and cancer cell death by specifically binding to human proliferating cell nuclear antigen (PCNA) in cancer cells.
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.
LRRK2-IN-1 demonstrated antiproliferative activity by inhibiting DNA replication processes and inducing cell cycle arrest.
