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Chemical Structure| 1410880-22-6 Chemical Structure| 1410880-22-6

Structure of JNK-IN-8
CAS No.: 1410880-22-6

Chemical Structure| 1410880-22-6

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JNK-IN-8 is a potent JNK inhibitor with IC50 values of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

Synonyms: JNK Inhibitor XVI; c-Jun N-terminal Kinase Inhibitor XVI

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Product Details of JNK-IN-8

CAS No. :1410880-22-6
Formula : C29H29N7O2
M.W : 507.59
SMILES Code : O=C(NC1=CC=C(NC2=NC=CC(C3=CC=CN=C3)=N2)C(C)=C1)C4=CC=CC(NC(C=CCN(C)C)=O)=C4
Synonyms :
JNK Inhibitor XVI; c-Jun N-terminal Kinase Inhibitor XVI
MDL No. :MFCD22124890
InChI Key :GJFCSAPFHAXMSF-UXBLZVDNSA-N
Pubchem ID :57340686

Safety of JNK-IN-8

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of JNK-IN-8

MAPK
TLR

Isoform Comparison

Biological Activity

Target
  • JNK1

    JNK1, IC50:4.7 nM

  • JNK2

    JNK2, IC50:18.7 nM

  • JNK3

    JNK3, IC50:1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BV2 microglial cells 10 mM JNK-IN-8 treatment inhibited the activation of BV2 microglial cells and reduced the expression of TNF-α, IL-1β, and IL-6 J Cell Physiol. 2020 Mar;235(3):2792-2799.
MDS-L cells 10 μM To investigate the inhibitory effect of JNK-IN-8 on WFA-induced C-JUN phosphorylation, results showed that JNK-IN-8 pretreatment inhibited WFA-induced C-JUN phosphorylation. Oncotarget. 2017 Aug 24;8(44):77436-77452.
WPMY-1 cells 2 μM 48 h Inhibition of c-JUN phosphorylation, mimicking the effect of lactate on p62 expression. Cell Rep. 2022 May 10;39(6):110792.
Normal human mammary epithelial cells 2μM 24 h To test the effect of the JNK inhibitor on apoptosis of mammary epithelial cells in suspension culture, results showed that the JNK inhibitor strongly suppressed apoptosis induced by suspension culture. Cell Rep. 2017 Nov 14;21(7):1910-1921.
PC-3 cells 1 μM and 2 μM JNK-IN-8 counteracted the reduction in phosphorylation levels of JNK and C-Jun, induced by ASPA knockdown, in a dose-dependent manner Mil Med Res. 2023 Jun 5;10(1):25.
SKMEL2 cells 200 nM 48 h To study the effect of JNK-IN-8 on AP-1 activity, results showed that JNK-IN-8 suppressed AP-1 activity in NT cells but failed to rescue AP-1 activation in GRAMD1B knockdown cells. Cancer Discov. 2023 Jan 9;13(1):194-215.
H1 hESCs 1 μM 1 day JNK inhibitor treatment significantly improved DE differentiation efficiency and reduced differentiation variability Nat Genet. 2019 Jun;51(6):999-1010.
HUES8 hESCs 1 μM 1 day JNK inhibitor treatment significantly improved DE differentiation efficiency and reduced differentiation variability Nat Genet. 2019 Jun;51(6):999-1010.
HUES6 hESCs 1 μM 1 day JNK inhibitor treatment significantly improved DE differentiation efficiency and reduced differentiation variability Nat Genet. 2019 Jun;51(6):999-1010.
BJ hiPSCs 1 μM 1 day JNK inhibitor treatment significantly improved DE differentiation efficiency and reduced differentiation variability Nat Genet. 2019 Jun;51(6):999-1010.
CV hiPSCs 1 μM 1 day JNK inhibitor treatment significantly improved DE differentiation efficiency and reduced differentiation variability Nat Genet. 2019 Jun;51(6):999-1010.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NF2 LOF mutants-induced IOMM-Lee xenograft tumor model Intraperitoneal injection 10 mg/kg Every other day for 15 days JNK-IN-8 significantly attenuated the NF2 LOF mutants-induced IOMM-Lee xenograft tumor growth Nat Commun. 2024 Nov 21;15(1):10106
Rats Transient middle cerebral artery occlusion (tMCAO) model Intraperitoneal injection 20 mg/kg Single dose, 2 hours after MCAO JNK-IN-8 treatment significantly improved neurological functional recovery in MCAO rats, inhibited microglial activation and JNK/NF-κB signaling pathway, and reduced the production of pro-inflammatory cytokines J Cell Physiol. 2020 Mar;235(3):2792-2799.
Mice SUM149 xenograft model Intraperitoneal injection 15 mg/kg and 30 mg/kg Daily for 34 days JNK-IN-8 significantly suppressed tumor growth and reduced CSC phenotype Oncogene. 2017 May 4;36(18):2599-2608
Mice Abca4−/−Rdh8−/− mice Intraperitoneal injection 4 mg/kg body weight Once daily for 4 days To evaluate the effect of JNK signaling inhibition on light-induced photoreceptor degeneration and apoptosis. Results showed JNK–IN-8 alleviated thinning of the photoreceptor layer, reduced apoptotic cells, and decreased protein levels of p-c-Jun, cleaved caspase-3, and γH2AX. J Biol Chem. 2020 May 15;295(20):6958-6971

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.85mL

1.97mL

0.99mL

19.70mL

3.94mL

1.97mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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