1. Autophagy
  2. LRRK2
  3. CZC-54252

CZC-54252 

Cat. No.: HY-B0792 Purity: 99.18%
Handling Instructions

CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity.

For research use only. We do not sell to patients.

CZC-54252 Chemical Structure

CZC-54252 Chemical Structure

CAS No. : 1191911-27-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 176 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 560 In-stock
Estimated Time of Arrival: December 31
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Description

CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity[1].

IC50 & Target

IC50: 1.28 nM (Wild-type LRRK2) and 1.85 nM (G2019S LRRK2)[1]

In Vitro

CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ~1 to ~5 nM. The G2019S mutant is inhibited with an IC50 ranging from ~2 to ~7 nM in a TF-FRET assay. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity[1].
G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC50 of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

504.99

Formula

C₂₂H₂₅ClN₆O₄S

CAS No.
SMILES

CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (198.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9802 mL 9.9012 mL 19.8024 mL
5 mM 0.3960 mL 1.9802 mL 3.9605 mL
10 mM 0.1980 mL 0.9901 mL 1.9802 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

CZC-54252CZC54252CZC 54252LRRK2Leucine-rich repeat kinase 2neuroprotectiveneuronalinjuryLRRK2-G2019SInhibitorinhibitorinhibit

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Product Name:
CZC-54252
Cat. No.:
HY-B0792
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