LRRK2-IN-1 | LRRK2 inhibitor, PCNA inhibitor | Probechem Biochemicals

Chemical Structure : LRRK2-IN-1

CAS No.: 1234480-84-2

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LRRK2-IN-1 (LRRK2 inhibitor)

货号: 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.

规格	价格	库存
10 mg	￥880	In stock
25 mg	￥1580	In stock
50 mg	￥2580	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	570.6852
分子式	C31H38N8O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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-

参考文献

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.

LRRK2-IN-1 (LRRK2 inhibitor)

生物&药学活性

物理化学性质&存储条件

参考文献

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LRRK2-IN-1 (LRRK2 inhibitor)

生物&药学活性

物理化学性质&存储条件

参考文献

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