A potent LRRK2 inhibitor
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CZC-25146

Item No. 22931

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[[5-fluoro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-methanesulfonamide
CAS Number
1191911-26-8
Molecular Formula
C22H25FN6O4S
Formula Weight
488.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 10 mg/ml
λmax
281 nm
SMILES
COC1=CC(N2CCOCC2)=CC=C1NC3=NC=C(F)C(NC4=CC=CC=C4NS(C)(=O)=O)=N3
InChi Code
InChI=1S/C22H25FN6O4S/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)
InChi Key
XXHHOTZUJIXPJX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $219

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    25 mg

    $502

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    Product Description

    CZC-25146 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 4.76 nM for the human recombinant kinase).1 It also inhibits LRRK2G2019S, a mutant linked to neurotoxicity and Parkinson’s disease, with an IC50 value of 6.87 nM. CZC-25146 is selective for LRRK2 over a panel of kinases in HeLa cell lysates, Jurkat/Ramos mixed cell lysates, as well as whole mouse brain extracts (IC50s = >2 μM). It reduces LRRK2G2019S-induced cell injury in rat primary cortical neurons.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ramsden, N.G., Perrin, J., Ren, Z., et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson’s disease-related toxicity in human neurons. ACS Chem Biol. 6(10), 1021-1028 (2011).