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Cat. No.: HY-184652

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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 LRRK2^G2019S, 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.

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

Formula: C₂₀H₂₁ClN₆O₂
Molecular Weight:412.87

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

LRRK2/JNK3-IN-1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Protocols (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

JNK3

22.1 nM (IC₅₀)

JNK1

MKNK2

LRRK2^G2019S

3.9 nM (IC₅₀)

LRRK2

3.24 nM (IC₅₀)

All JNK Isoforms :

All CaMK Isoforms :

All Casein Kinase Isoforms :

In Vitro

LRRK2/JNK3-IN-1 (Compound 17) (2 h) shows low-nanomolar inhibitory activity against both LRRK2^G2019S 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 LRRK2^G2019S (IC₅₀ = 0.87 nM) in HEK293 cell NanoBRET assays transiently expressing NanoLuc‑LRRK2^G2019S^[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. Further protocols information, click here.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	AUC_0-∞	CL	V_ss	C_max	T_max	Bioavailability
Mice^[1]	2 mg/kg	p.o.	4.4 h	437 ng·h/mL	393 ng·h/mL	5.22 L/h/kg	7.5 L/kg	/	/	/
Mice^[1]	5 mg/kg	i.v.	/	1325 ng·h/mL	1352 ng·h/mL	/	/	343 ng/mL	0.72 h	84.9 %

In Vivo

LRRK2/JNK3-IN-1 (Compound 17) (500 mg/kg; p.o.; single dose) shows good in vivo tolerability in male ICR mice, with no significant effects on body weight or major organs. LRRK2/JNK3-IN-1 efficiently penetrates the blood-brain barrier, suggesting its potential for research on central nervous system disorders^[1].

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

Molecular Weight 412.87
Formula C₂₀H₂₁ClN₆O₂
SMILES

ClC1=CNC2=C1C(NCCCN(C)C3=O)=NC(NC4=CC3=CC=C4OC5CC5)=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kim K, et al. Polypharmacological Targeting of G2019S Mutant LRRK2 and JNK3 for the Discovery of a Lead Compound against Parkinson's Disease. J Med Chem. 2026 Jun 22. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocols
Purity & Documentation
References

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LRRK2/JNK3-IN-1

All JNK Isoforms

All CaMK Isoforms

All Casein Kinase Isoforms