- HG-10-102-01
| LRRK2-IN-1LRRK2 inhibitor,cell-permeable and ATP competitive |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.78%
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- MS (Mass Spectrometry)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
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Chemical structure
Related Biological Data
| Description | LRRK2-IN-1 is a potent and selective inhibitor ofleucine-rich repeat kinase 2 (LRRK2) with IC50 values of 13 nM and 6 nM for wild-type LRRK2 and G2019S mutant LRRK2, respectively. | |||||
| Targets | wild-type LRRK2 | G2019S mutant LRRK2 | ||||
| IC50 | 13 nM | 6 nM | ||||
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| Cas No. | 1234480-84-2 | SDF | Download SDF |
| Synonyms | LRRK 2-IN-1 | ||
| Chemical Name | 2-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one | ||
| Canonical SMILES | CN1CCN(CC1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)C)OC | ||
| Formula | C31H38N8O3 | M.Wt | 570.7 |
| Solubility | ≥28.55mg/mL in DMSO, ≥57.2mg/mL in EtOH, <2.87mg l="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
LRRK2-IN-1 is a potent and selective inhibitor of LRRK2 with IC50 value of 13 nM. [1]LRRK2 (Leucine-rich repeat kinase 2) is also known dardarin. LRRK2 belongs to the leucine-rich repeat kinase family. LRRK2 mostly located in the cytoplasm, however, it also associates with outer membrane of the mitochondrial. LRRK2 interacts with parkin at the C-terminal R2 RING finger domain. Parkin interacted with LRRK2 at the COR domain. LRRK2 mutation will induce apoptotic cell death of neuroblastoma cells. Expression of LRRK2 mutants has a close relationship with autosomal dominant Parkinson"s disease. The LRRK2 Gly2019Ser mutation is a common cause of familial Parkinson"s disease. The Gly2019Ser mutation has been proved to cause Parkinson"s disease, even though it is a small number of LRRK2 mutations. LRRK2 also has relationship with Crohn"s disease by genomewide association studies.LRRK2-IN-1 dose-dependent inhibit the activity of wild-type and G2019S LRRK2 with IC50 of 0.17 and 0.04μM respectively in HEK293 cells stably expressing GFP tagged wild-type or mutated LRRK2.[2] LRRK2-IN-1 inhibits the activity of both wild-type and G2019S mutant LRRK2 with IC 50 values of 13 nM and 6 nM respectively in vitro enzyme assay with 0.1 mM ATP. LRRK2-IN-1 competed with ATP. LRRK2-IN-1 has a selective profile compared with other 442 diverse kinases and it has no inhibition effect with LRRK1. LRRK2-IN-1 induced endogenous LRRK2 phosphorylation in lymphoblastoid cells. LRRK2-IN-1 also induced Ser910/Ser935 dephosphorylation of LRRK2 in mice kidney at 100 mg/kg.[1]References: [1]. Deng X, Dzamko N, Prescott A, Davies P, Liu Q, Yang Q, Lee JD, Patricelli MP, Nomanbhoy TK, Alessi DR et al: Characterization of a selective inhibitor of the Parkinson"s disease kinase LRRK2. Nat Chem Biol, 7(4):203-205.[2]. Hermanson SB, Carlson CB, Riddle SM, Zhao J, Vogel KW, Nichols RJ, Bi K: Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PLoS One, 7(8):e43580.
