Biological Activity
Potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) (IC50 values are 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively). Attenuates neuronal injury induced by LRRK2-G2019S mutant activity in primary human neurons (EC50 = 1 nM).
Compound Libraries
CZC 54252 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 541.45 |
| Formula | C22H25ClN6O4S.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1191911-27-9 |
| PubChem ID | 90488950 |
| InChI Key | KWCBHUPLQMUKAF-UHFFFAOYSA-N |
| Smiles | ClC1=C(NC3=CC=CC=C3NS(C)(=O)=O)N=C(NC2=C(OC)C=C(N4CCOCC4)C=C2)N=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 541.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.85 mL | 9.23 mL | 18.47 mL |
| 5 mM | 0.37 mL | 1.85 mL | 3.69 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.85 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ramsden et al (2011) Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem.Biol. 6 1021 PMID: 21812418
Kramer et al (2012) Small molecule kinase inhibitors for LRRK2 and their application to Parkinson's disease models. ACS Chem.Neurosci. 3 151 PMID: 22860184
Keywords: CZC 54252 hydrochloride, supplier, CZC54252, leucine-rich, repeat, kinase, 2, LRRK2, inhibitors, inhibits, potent, neuroprotective, neuronal, injury, parkinson's, parkinsons, LRRK2, LRRK2, Tocris Bioscience
