1. MAPK/ERK Pathway
  2. JNK
  3. JNK3 inhibitor-8

JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD).

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

JNK3 inhibitor-8 Chemical Structure

JNK3 inhibitor-8 Chemical Structure

CAS No. : 3034676-53-1

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Description

JNK3 inhibitor-8 is a potent, delective, orally active and cross the blood-brain barrier JNK3 inhibitor with IC50 values of 21, 2203, >10000 nM for JNK3, JNK2, JNK1, respectively. JNK3 inhibitor-8 shows significant neuroprotective effects. JNK3 inhibitor-8 has the potential for the research of Alzheimer’s disease (AD)[1].

IC50 & Target[1]

JNK3

21 nM (IC50)

JNK2

2203 nM (IC50)

JNK1

>10000 nM (IC50)

In Vitro

JNK3 inhibitor-8 (compound 3h; 10, 20 µM; 24, 48 h) increases primary rat cortex neuron cell viability when treatment with 10 μM amyloid-β1-42[1].
JNK3 inhibitor-8 (10, 20 µM) decreases the expression of p-c-jun (S63), p-c-jun (S73), PARP and p-Tau 10 μM amyloid-β1-42 stitumed[1].

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

Cell Viability Assay[1]

Cell Line: primary rat cortex neuron cells
Concentration: 10, 20 µM
Incubation Time: 24, 48 h
Result: Increased cell viability when treatment with 10 μM amyloid-β1-42.

Western Blot Analysis[1]

Cell Line: primary rat cortex neuron cells
Concentration: 10, 20 µM
Incubation Time:
Result: Decreased the expression of p-c-jun (S63) and p-c-jun (S73) in 0.5 μM anisomycin or 10 μM amyloid-β1-42 stitumed, and decreased the expression of PARP and p-Tau expression when treatment with 10 μM amyloid-β1-42.
In Vivo

JNK3 inhibitor-8 (30, 60 mg/kg; p.o.; daily for 4 weeks) shows significant neuroprotective effects in mice[1].
Pharmacokinetic Parameters of JNK3 inhibitor-8 in Sprague-Dawley rats[1].

compound 2h
admin. PO
dose (mg/kg) 3
AUClast (h ng/ml) 727.09
C0 or Cmax (ng/mL) 423.17
Tmax (h) 0.39
T1/2 (h) 0.97
Sprague-Dawley rats, 3 mg/kg p.o.[1]

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

Animal Model: 6 month-old APP/PS1 AD mice[1]
Dosage: 30, 60 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Decrease in escape time and distance traveled, showed a significantly higher level of altered behavioral ability compared to APP/PS1 and vehicle control in the Y-maze test, improved memory and cognitive function.
Animal Model: 10 month-old 3xTg AD mice[1]
Dosage: 30, 60 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Decreased the escape time and the distance, increased TSPQ and TSTZ levels, significantly decreased the expression of pTau levels and improved memory and cognitive function.
Molecular Weight

579.62

Formula

C32H30FN7O3

CAS No.
SMILES

O=C(N1C[C@@H](NC2=NC=CC(N3C4=C(N=C3C5=CC6=C(C=C5)C=CC=C6)C(F)=CC(OC(NC)=O)=C4)=N2)CCC1)C7CC7

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
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JNK3 inhibitor-8 Related Classifications

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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.

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JNK3 inhibitor-8
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HY-149280
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