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.

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

JNK3 inhibitor-4 Chemical Structure

JNK3 inhibitor-4 Chemical Structure

CAS No. : 2409109-65-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

JNK3 inhibitor-4 Related Antibodies

Top Publications Citing Use of Products

View All JNK Isoform Specific Products:

View All Isoforms
JNK1 JNK2 JNK3 JNK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

JNK3 inhibitor-4 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JNK3 inhibitor-4
Cat. No.:
HY-151929
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.