![3-[3-[2-(生物素酰胺)乙基]氨基-3-氧代丙基]二硫基]丙酸琥珀酰亚胺酯，100MG，B4531-100MG，Sigma](https://static.bingosci.com/uploadfile/opc/editor/file/202608/05/1785897109578603_M.png)
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General description
A cell-permeable, ATP competitive, potent, and selective LRRK2 inhibitor (IC50 of 13 nM, 6 nM, and 2.45 µM for wild type, G2019S mutant, and drug resistant A2016T mutant LRRK2, respectively, in an in vitro ATP-site competititon binding assay). While it is shown to inhibit DCLK2 (IC50 = 45 nM) and suppress MAPK7 autophosphorylation (EC50 = 160 nM), this compound (<10 µM) demonstrates very good overall selectivity, targeting 12 out of 442 other kinases in a kinase-binding and biochemical assay. At 0.05-3 µM, it induces dose-dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild-type LRRK2 and LRRK2[G2019S] in stably transfected HEK293 cells, but not in the drug-resistant LRRK2[A2016T] and LRRK2[A2016T + G2019S] mutants. Similar effects on endogenous LRRK2 phosphorylation and 14-3-3 binding can be observed in human lympho-blastoid cells and for the LRRK2 G2019S mutant derived from a Parkinson′s disease patient, and in human-derived neuroblastoma SHSY5Y cells, as well as in mouse Swiss 3T3 cells. 100 mg/kg of compound injected into mice elicits complete Ser910 and Ser935 dephosphorylation of LRRK2 in the kidney, but not in the brain which may result from an inability to penetrate the blood-brain barrier. In addition, it promotes relocalization of LRRK2 to more aggregate and fibrillar-like structures.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freexe (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Deng, X., et al. 2011. Nat. Chem. Biol.7, 203.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow-white to pale yellow |
| solubility | DMSO: 50 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | CN1CCN(CC1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)NC4=NC=C5C(=N4)N(C6=CC=CC=C6C(=O)N5C)C)OC |
| InChI key | IWMCPJZTADUIFX-UHFFFAOYSA-N |
| 长度(mm) | |
| 宽度(mm) | |
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