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Submit ReviewCZC 54252 hydrochloride
Description: Potent LRRK2 inhibitor; neuroprotective
Chemical Name: N-[2-[[5-Chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]methanesulfonamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for CZC 54252 hydrochloride
CZC 54252 hydrochloride is a 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).
Technical Data for CZC 54252 hydrochloride
| M. Wt | 541.45 |
| Formula | C22H25ClN6O4S.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1784253-05-9 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CZC 54252 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.15 | 100 |
Preparing Stock Solutions for CZC 54252 hydrochloride
The following data is based on the product molecular weight 541.45. 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.
| 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 for CZC 54252 hydrochloride
References for CZC 54252 hydrochloride
References are publications that support the biological activity of the product.
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
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Keywords: CZC 54252 hydrochloride, CZC 54252 hydrochloride supplier, CZC54252, leucine-rich, repeat, kinase, 2, LRRK2, inhibitors, inhibits, potent, neuroprotective, neuronal, injury, parkinson's, parkinsons, 4534, Tocris Bioscience
Citations for CZC 54252 hydrochloride
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Literature in this Area
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Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
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- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
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Parkinson's 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.