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CZC 54252 hydrochloride

Potent LRRK2 inhibitor; neuroprotective CAS# 1191911-27-9

CZC 54252 hydrochloride

Catalog No. BCC6218----Order now to get a substantial discount!

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Chemical structure

CZC 54252 hydrochloride

3D structure

Chemical Properties of CZC 54252 hydrochloride

Cas No. 1191911-27-9 SDF Download SDF
PubChem ID 44252734 Appearance Powder
Formula C22H25ClN6O4S M.Wt 505.0
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (198.02 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N-[2-[[5-chloro-2-(2-methoxy-4-morpholin-4-ylanilino)pyrimidin-4-yl]amino]phenyl]methanesulfonamide
SMILES COC1=C(C=CC(=C1)N2CCOCC2)NC3=NC=C(C(=N3)NC4=CC=CC=C4NS(=O)(=O)C)Cl
Standard InChIKey CLGWUCNXOBLWFM-UHFFFAOYSA-N
Standard InChI InChI=1S/C22H25ClN6O4S/c1-32-20-13-15(29-9-11-33-12-10-29)7-8-19(20)26-22-24-14-16(23)21(27-22)25-17-5-3-4-6-18(17)28-34(2,30)31/h3-8,13-14,28H,9-12H2,1-2H3,(H2,24,25,26,27)
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CZC 54252 hydrochloride

DescriptionPotent 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).

CZC 54252 hydrochloride Dilution Calculator

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CZC 54252 hydrochloride Molarity Calculator

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Preparing Stock Solutions of CZC 54252 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9802 mL 9.901 mL 19.802 mL 39.604 mL 49.505 mL
5 mM 0.396 mL 1.9802 mL 3.9604 mL 7.9208 mL 9.901 mL
10 mM 0.198 mL 0.9901 mL 1.9802 mL 3.9604 mL 4.9505 mL
50 mM 0.0396 mL 0.198 mL 0.396 mL 0.7921 mL 0.9901 mL
100 mM 0.0198 mL 0.099 mL 0.198 mL 0.396 mL 0.495 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CZC 54252 hydrochloride

CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively. IC50 value: 1.28 nM/1.85 nM(LRRK2/G2019S LRRK2) [1] Target: LRRK2 inhibitor in vitro: CZC-54252 inhibited the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ~1 to ~5 nM. The G2019S mutant was inhibited with an IC50 ranging from ~2 to ~7 nM in a TF-FRET assay. In addition, they were screened against a kinase panel of 185 kinases and exhibited good selectivity. CZC-25146 (19) inhibited five other kinases, PLK4, GAK, TNK1, CAMKK2, and PIP4K2C, with high potency only, but none of them have been classified as predictors of genotoxicity or hematopoietic toxicity [1]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-25146 with an EC50 of ~4 nM (EC50 CZC-54252 ~1 nM) and fully reversed to wild-type levels by both compounds at concentrations as low as 8 nM (1.6 nM for CZC-54252) [2]. in vivo: In vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146 (19). Unfortunately, it exhibited a poor brain penetration of just 4%.

References:
[1]. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8. [2]. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.

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References on CZC 54252 hydrochloride

Small molecule kinase inhibitors for LRRK2 and their application to Parkinson's disease models.[Pubmed:22860184]

ACS Chem Neurosci. 2012 Mar 21;3(3):151-60.

Parkinson's disease (PD) is the second most common neurodegenerative disorder. Several single gene mutations have been linked to this disease. Mutations in the gene encoding leucine-rich repeat kinase 2 (LRRK2) indicate LRRK2 as promising therapeutic target for the treatment of PD. LRRK2 mutations were observed in sporadic as well as familial PD patients and have been investigated intensively. LRRK2 is a large and complex protein, with multiple enzymatic and protein-interaction domains, each of which is effected by mutations. The most common mutation in PD patients is G2019S. Several LRRK2 inhibitors have been reported already, although the crystal structure of LRRK2 has not yet been determined. This review provides a summary of known LRRK2 inhibitors and will discuss recent in vitro and in vivo results of these inhibitors.

Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons.[Pubmed:21812418]

ACS Chem Biol. 2011 Oct 21;6(10):1021-8.

Leucine-rich repeat kinase-2 (LRRK2) mutations are the most important cause of familial Parkinson's disease, and non-selective inhibitors are protective in rodent disease models. Because of their poor potency and selectivity, the neuroprotective mechanism of these tool compounds has remained elusive so far, and it is still unknown whether selective LRRK2 inhibition can attenuate mutant LRRK2-dependent toxicity in human neurons. Here, we employ a chemoproteomics strategy to identify potent, selective, and metabolically stable LRRK2 inhibitors. We demonstrate that CZC-25146 prevents mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency. These precise chemical probes further validate this emerging therapeutic strategy. They will enable more detailed studies of LRRK2-dependent signaling and pathogenesis and accelerate drug discovery.

Description

CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.

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