2. MAPK/ERK Pathway
  3. JNK
  4. JNK3 inhibitor-4

JNK3 inhibitor-4 is a potent inhibitor of JNK3 (IC50=1.0 nM) based on 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile. JNK3 inhibitor-4 shows excellent selectivity over other protein kinases including isoforms JNK1 (IC50=143.9 nM) and JNK2 (IC50=298.2 nM). JNK3 inhibitor-4 has neuroprotective effect and predicated blood-brain barrier permeability.

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JNK3 inhibitor-4 Chemical Structure

JNK3 inhibitor-4 Chemical Structure

CAS No. : 2409109-65-3

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Based on 1 publication(s) in Google Scholar

JNK3 inhibitor-4 Related Antibodies

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Description

JNK3 inhibitor-4 is a potent inhibitor of JNK3 (IC50=1.0 nM) based on 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile. JNK3 inhibitor-4 shows excellent selectivity over other protein kinases including isoforms JNK1 (IC50=143.9 nM) and JNK2 (IC50=298.2 nM)[1]. JNK3 inhibitor-4 has neuroprotective effect and predicated blood-brain barrier permeability[1].

IC50 & Target[1]

JNK3

1.0 nM (IC50)

JNK1

143.9 nM (IC50)

JNK2

298.2 nM (IC50)

In Vitro

JNK3 inhibitor-4 (compound 15d) (1, 5, 10, 20 μM; 24 h and 48 h) inhibits Aβ1-42 induced Aβ1-42-induced cellular toxicity in primary rat cortex neuron[1].
JNK3 inhibitor-4 (10 μM and 20 μM; 24 h and 48 h) inhibits c-jun phosphorylation and APP phosphorylation induced by 10 μM Aβ1-42 or 0.5 μM Anisomycin (HY-18982) in primary rat cortex neuron[1].
JNK3 inhibitor-4 (50 μM; 4 h) shows high permeability in Caco-2 assay and is predicted as BBB permeable (CNS+) based on effective permeability coefficient (Pe) value > 4 in PAMPA assay[1].
JNK3 inhibitor-4 also shows inhibitory potency on GSK3α (h), GSK3β (h), JNK1, 2, MKK6, MOK, SAPK2a (h), SAPK2a (T106 M) (h), SAPK2b (h), MKK4, JNK1α1 (h), and JNK2α1 (h). These shows IC50 values of 5.78, 11.7, 15.1, 1.18, 3.10, 1.19, 0.280, 0.970, 0.860, and 0.340 μM, respectively[1].

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

JNK3 inhibitor-4 Related Antibodies

Western Blot Analysis[1]

Cell Line: Primary rat cortex neuron
Concentration: 10 μM and 20 μM
Incubation Time: 24 hours
Result: Monomeric Aβ1-42 induced c-jun phosphorylation dose-dependently and that was inhibited by JNK3 inhibitor-4 in concentration-dependent manner.

Cell Viability Assay[1]

Cell Line: Primary rat cortex neuron
Concentration: 1, 5, 10, 20 μM
Incubation Time: 24 hours and 48 hours
Result: Showed neuroprotective effect and increased cell viability under Aβ1-42 treatment.
In Vivo

JNK3 inhibitor-4 improves memory for the Alzheimer’s disease mouse model. JNK3 inhibitor-4 (compound 15d) (10 or 30 mg/kg; i.v.; 3 times/week for 1 month in 9-month-old APP/PS1 3Tx3Tg mice) results significantly higher spontaneous alteration and response latency of mouse (at 27th or 30th days) compared to the APP/PS1vehicle groups in Y-maze test and passive avoidance test, with a dose correlation[1].
JNK3 inhibitor-4 (30 mg/kg; p.o.; single dose) shows blood-brain barrier permeability with brain to plasma ratio of 0.02 in SD rats[1].
Pharmacokinetics in rats[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) BA (%)
IV 1 718.0 0.22
PO 3 337.5 377.82 0.63 0.34 15.67

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

477.56

Formula

C28H27N7O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CCC1=CN=C(N1C2=NC(N[C@H]3CCCN(C3)C(C4CC4)=O)=NC=C2)C5=CC6=C(C=C5)C=CC=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0940 mL 10.4699 mL 20.9398 mL
5 mM 0.4188 mL 2.0940 mL 4.1880 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0940 mL 10.4699 mL 20.9398 mL 52.3494 mL
5 mM 0.4188 mL 2.0940 mL 4.1880 mL 10.4699 mL
10 mM 0.2094 mL 1.0470 mL 2.0940 mL 5.2349 mL
15 mM 0.1396 mL 0.6980 mL 1.3960 mL 3.4900 mL
20 mM 0.1047 mL 0.5235 mL 1.0470 mL 2.6175 mL
25 mM 0.0838 mL 0.4188 mL 0.8376 mL 2.0940 mL
30 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7450 mL
40 mM 0.0523 mL 0.2617 mL 0.5235 mL 1.3087 mL
50 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0470 mL
60 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8725 mL
80 mM 0.0262 mL 0.1309 mL 0.2617 mL 0.6544 mL
100 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5235 mL
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JNK3 inhibitor-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNK3 inhibitor-42409109-65-3JNKc-Jun N-terminal kinaseAlzheimer’s diseaseInhibitorinhibitorinhibit

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