LRRK2/JNK3-IN-1
LRRK2/JNK3-IN-1 is a brain-penetrant multi-target inhibitor of LRRK2 (including G2019S mutant and wild-type) and JNK3, with enzymatic IC50 values of 3.90 nM against LRRK2G2019S, 3.24 nM against wild-type LRRK2, and 22.1 nM against JNK3. LRRK2/JNK3-IN-1 displays favorable selectivity in a 97-kinase profiling screen, and also shows inhibitory activity against JNK1, JNK2, and MKNK2. LRRK2/JNK3-IN-1 can be used for the research of Parkinson's disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C20H21ClN6O2
- Peso molecular:412.87
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
JNK3 22.1 nM (IC50) |
JNK1 |
MKNK2 |
LRRK2G2019S 3.9 nM (IC50) |
LRRK2 3.24 nM (IC50) |
LRRK2/JNK3-IN-1 (Compound 17) (2 h) shows low-nanomolar inhibitory activity against both LRRK2G2019S and wild-type in enzymatic activity assays, with IC50 values of 3.90 nM and 3.24 nM, respectively, and also displays inhibitory activity against JNK3 with an IC50 of 22.1 nM[1].
LRRK2/JNK3-IN-1 (1 μM) displays favorable overall selectivity in a 97-kinase selectivity profiling screen [S(1%) = 0.04], and shows potent or moderate inhibition against JNK1 (remaining activity 0.15%), JNK3 (0.25%), JNK2 (4.1%), MKNK2 (0.40%), CSNK1D (0.90%), FAK (3.0%), ALK (4.3%), PLK4 (5.1%), and CSNK1G2 (6.0%)[1].
LRRK2/JNK3-IN-1 (1 h) demonstrates picomolar cellular activity against LRRK2G2019S (IC50 = 0.87 nM) in HEK293 cell NanoBRET assays transiently expressing NanoLuc‑LRRK2G2019S[1].
LRRK2/JNK3-IN-1 (1 h) exhibits very weak cellular inhibitory activity against JNK3 (IC50 = 14,890 nM) in HEK293 cell NanoBRET assays transiently expressing NanoLuc‑JNK3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male ICR mice (7 weeks old, 29-32 g) following a single oral administration[1]
-
Dosage:500 mg/kg
-
Administration:Oral gavage (p.o.)
-
Result:Showed no evident signs of systemic toxicity over a 14-day observation period and was well tolerated.
Demonstrated steady and continuous body weight gain comparable to the control group, with no weight loss or growth retardation.
Revealed no significant differences in major organ weights (liver, kidney, lung, spleen, and heart) between treated and control groups, indicating no organ-specific toxicity.
Efficiently penetrated the blood-brain barrier with a brain-to-plasma partition coefficient (Kp) of 91.9%.
Chemical Information
-
Peso molecular 412.87
-
Fòrmula C20H21ClN6O2
-
SMILES
ClC1=CNC2=C1C(NCCCN(C)C3=O)=NC(NC4=CC3=CC=C4OC5CC5)=N2
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LRRK2/JNK3-IN-1 Related Classifications
HY-184652 Related Classifications
Powered by Bioz
- LRRK2/JNK3-IN-1
- LRRK2
- JNK
- CaMK
- Casein Kinase
- LRRK2 Inhibitor
- LRRK2G2019S
- JNK3 Inhibitor
- JNK1
- JNK2
- MKNK2
- CSNK1D
- CSNK1G2
- ALK
- PLK4
- FAK
- Parkinson's disease
- brain penetration
- blood-brain barrier
- HEK293 cells
- male ICR mice
- polypharmacology
- structure-based drug design
- neuroinflammation
- CNS drug
- kinome-wide selectivity
- Inhibitor
- inhibitor
- inhibit