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说明： Potent and selective LRRK2 inhibitor
化学名： rel-3-[6-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-pyrimidyl]-5-[(1-methylcyclopropyl)oxy]-1H-indazole
纯度： ≥98% (HPLC)
生物活性 for MLi-2
MLi-2 is a potent and selective LRRK2 inhibitor (IC50 = 0.76-3.4 nM depending on assay), which exhibits >295-fold selectivity for over 300 kinases and a diverse panel of receptors and ion channels. MLi-2 is centrally bioavailable and active in vivo.
External Portal Information for MLi-2
Chemicalprobes.org and the Chemical Probes webpages of the Structural Genomics Consortium are portals that offer independent guidance on the selection and/or application of small molecules for research. The use of MLi-2 is reviewed on chemicalprobes.org and the SGC website.
化合物库 for MLi-2
MLi-2 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for MLi-2
| 分子量 | 379.46 |
| 公式 | C21H25N5O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1627091-47-7 |
| PubChem ID | 78319901 |
| InChI Key | ATUUNJCZCOMUKD-OKILXGFUSA-N |
| Smiles | CC1(CC1)OC2=CC=C3C(C(C4=NC=NC(N5C[C@@H](C)O[C@@H](C)C5)=C4)=NN3)=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for MLi-2
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 18.97 | 50 |
制备储备液 for MLi-2
以下数据基于产品分子量 379.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.27 mL | 26.35 mL | 52.71 mL |
| 2.5 mM | 1.05 mL | 5.27 mL | 10.54 mL |
| 5 mM | 0.53 mL | 2.64 mL | 5.27 mL |
| 25 mM | 0.11 mL | 0.53 mL | 1.05 mL |
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产品说明书 for MLi-2
参考文献 for MLi-2
参考文献是支持产品生物活性的出版物。
Fell et al (2015) MLi-2, a potent, selective, and centrally active compound for exploring the therapeutic potential and safety of LRRK2 kinase inhibition. J.Pharmacol.Exp.Ther. 355 397 PMID: 26407721
If you know of a relevant reference for MLi-2, please let us know.
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关键词: MLi-2, MLi-2 supplier, leucine-rich, repeat, kinase, 2, LRRK2, inhibitors, inhibits, potent, neuroprotective, neuronal, injury, parkinson's, parkinsons, 5756, Tocris Bioscience
22 篇 MLi-2 的引用文献
引用文献是使用了 Tocris 产品的出版物。 MLi-2 的部分引用包括：
Henderson et al (2018) LRRK2 activity does not dramatically alter α-synuclein pathology in primary neurons. Acta Neuropathol Commun 6 45 PMID: 29855356
Henderikus et al (2023) Characterization of Lipopolysaccharide Effects on LRRK2 Signaling in RAW Macrophages. Int J Mol Sci 24 PMID: 36675159
Mark R et al (2022) Lysosomal positioning regulates Rab10 phosphorylation at LRRK2+ lysosomes. Proc Natl Acad Sci U S A 119 e2205492119 PMID: 36256825
Vincent et al (2022) A cell-based GEF assay reveals new substrates for DENN domains and a role for DENND2B in primary ciliogenesis. Sci Adv 8 eabk3088 PMID: 35196081
Sven H et al (2022) Nanobodies as allosteric modulators of Parkinson's disease-associated LRRK2. Proc Natl Acad Sci U S A 119 PMID: 35217606
Sung-Woo et al (2022) LRRK2 Inhibition Mitigates the Neuroinflammation Caused by TLR2-Specific α-Synuclein and Alleviates Neuroinflammation-Derived Dopaminergic Neuronal Loss. Cells 11 PMID: 35269482
Elisa et al (2022) Trafficking of the glutamate transporter is impaired in LRRK2-related Parkinson's disease. Acta Neuropathol 144 81-106 PMID: 35596783
Mark R et al (2022) Directing LRRK2 to membranes of the endolysosomal pathway triggers RAB phosphorylation and JIP4 recruitment. Neurobiol Dis 170 105769 PMID: 35580815
Nicolas et al (2022) WHOPPA Enables Parallel Assessment of Leucine-Rich Repeat Kinase 2 and Glucocerebrosidase Enzymatic Activity in Parkinson's Disease Monocytes. Front Cell Neurosci 16 892899 PMID: 35755775
Catherine et al (2022) DJ-1 is an essential downstream mediator in PINK1/parkin-dependent mitophagy. Brain 145 4368-4384 PMID: 36039535
Ole et al (2019) Mitochondrial clearance and maturation of autophagosomes are compromised in LRRK2 G2019S familial Parkinson's disease patient fibroblasts. Hum Mol Genet 28 3232-3243 PMID: 31261377
Yuriko et al (2021) Pathogenic LRRK2 regulates ciliation probability upstream of tau tubulin kinase 2 via Rab10 and RILPL1 proteins. Proc Natl Acad Sci U S A 118 PMID: 33653948
John Q et al (2021) LRRK2 Kinase Activity Does Not Alter Cell-Autonomous Tau Pathology Development in Primary Neurons. J Parkinsons Dis 11 1187-1196 PMID: 33720852
Dan et al (2021) Increased LRRK2 kinase activity alters neuronal autophagy by disrupting the axonal transport of autophagosomes. Curr Biol 31 2140-2154.e6 PMID: 33765413
Chelsie A et al (2021) Endosomal traffic and glutamate synapse activity are increased in VPS35 D620N mutant knock-in mouse neurons, and resistant to LRRK2 kinase inhibition. Mol Brain 14 143 PMID: 34530877
Matthias et al (2020) Accurate MS-based Rab10 Phosphorylation Stoichiometry Determination as Readout for LRRK2 Activity in Parkinson's Disease. Mol Cell Proteomics 19 1546-1560 PMID: 33451735
Weidong et al (2020) Parkinson's disease-related Leucine-rich repeat kinase 2 modulates nuclear morphology and genomic stability in striatal projection neurons during aging. Mol Neurodegener 15 12 PMID: 32075681
Shaun et al (2020) LRRK2 mutations impair depolarization-induced mitophagy through inhibition of mitochondrial accumulation of RAB10. Autophagy 16 203-222 PMID: 30945962
Ravindran et al (2020) LRRK2 mediates tubulation and vesicle sorting from lysosomes. Sci Adv 6 PMID: 33177079
Huw R et al (2020) LRRK2 activation controls the repair of damaged endomembranes in macrophages. EMBO J 39 e104494 PMID: 32643832
Matthias et al (2020) Accurate MS-based Rab10 Phosphorylation Stoichiometry Determination as Readout for LRRK2 Activity in Parkinson's Disease. Mol Cell Proteomics 19 1546-1560 PMID: 32601174
Eleanor T et al (2020) Protein synthesis is suppressed in sporadic and familial Parkinson's disease by LRRK2. FASEB J 34 14217-14233 PMID: 32926469
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MLi-2 的评论
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Good LRRK2 inhibitor.
By
Anonymous on 01/27/2023
分析类型： In Vitro
种属： Rat
细胞系/组织： Primary hippocampal neurons
The drug was incubated at 500 nM to inhibit LRRK2.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.