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JNK-IN-8

Catalog No. T2668 CAS 1410880-22-6

Synonyms: JNK Inhibitor XVI

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.

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JNK-IN-8, CAS 1410880-22-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 70.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 218.00
50 mg	In stock	$ 363.00
100 mg	In stock	$ 536.00
200 mg	In stock	$ 761.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 100%

Purity: 99.24%

Purity: 98.25%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.
Targets&IC50	JNK1:4.7 nM, JNK2:18.7 nM, JNK:1 nM
In vivo	JNK-IN-8 (10 mM) effectively inhibits the phosphorylation of c-Jun stimulated by IL-1β in IL-1R cells. It displays significant selectivity for the 1,4-bis(phenylamino) and 1,3-aminobenzoic acid structural regions compared to imatinib, covalently binding to the Cys154 target via an N,N-dimethylbutenamide linkage. JNK-IN-8 inhibits the phosphorylation of c-Jun in HeLa (EC50: 486 nM) and A375 (EC50: 338 nM) cells. Its binding with PIK3C3, IRAK1, PIP5K3, and PIP4K2C significantly enhances selectivity and elimination rates. JNK-IN-8 inhibits JNK2 through Cys116.
Kinase Assay	A375 cells are pre-treated with 1 μM JNK-IN-8 for the indicated amounts of time. Remove the medium and wash 3 times with PBS. Resuspend the cell pellet with 1 mL Lysis Buffer (1% NP-40, 1% CHAPS, 25 mM Tris, 150 mM NaCl, Phosphatase Inhibitor Cocktail, and Protease Inhibitor Cocktail). Rotate end-to-end for 30 min at 4°C. Lysates are cleared by centrifugation at 14000 rpm for 15 min in the Eppendorf. The cleared lysates gel filtered into Kinase Buffer (0.1% NP-40, 20 mM HEPES, 150 mM NaCl, Phosphatase Inhibitor Cocktail, Protease Inhibitor Cocktail) using Bio-Rad 10DG colums. The total protein concentration of the gel-filtered lysate should be around 5-15 mg/mL. Cell lysate is labeled with the probe from ActivX at 5 μM for 1 hour. Samples are reduced with DTT, and cysteines are blocked with iodoacetamide and gel filtered to remove excess reagents and exchange the buffer. Add 1 volume of 2X Binding Buffer (2% Triton-100, 1% NP-40, 2 mM EDTA, 2X PBS) and 50 μL streptavidin bead slurry and rotate end-to-end for 2 hours, centrifuge at 7000 rpm for 2 min. Wash 3 times with 1X Binding Buffer and 3 times with PBS. Add 30 μL 1X sample buffer to beads, heat samples at 95°C for 10 min. Run samples on an SDS-PAGE gel at 110V. After transferred, the membrane is immunoblotted with JNK antibody[1].
Cell Research	JNK-IN-8 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. HEK-293 cells stably expressing Interleukin Receptor 1 (HEK293-IL1R) are cultured in Dulbecco's Modified Eagle's medium (DMEM) supplemented with 10% FBS, 2 mM glutamine and 1×antimycotic/antibiotic solution. Cells are serum starved for 18 h before incubation with DMSO or JNK-IN-8, stimulated with 2 μM Anisomycin for 1h and lysates are clarified by centrifugation for 10 min at 16000 g and 4°C[1].

Synonyms	JNK Inhibitor XVI
Molecular Weight	507.59
Formula	C29H29N7O2
CAS No.	1410880-22-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (183.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Zhang T, et al. Chem Biol, 2012, 19(1), 140-154. 2. Goh ET, et al. Biochem J, 2012, 441(1), 339-346. 3. Liu Q, et al. Chem Biol, 2013, 20(2), 146-159.

Citations

1. Zhou S, Niu R, Sun H, et al. The MAP3K1/c-JUN signaling axis regulates glioblastoma stem cell invasion and tumor progression. Biochemical and Biophysical Research Communications. 2022, 612: 188-195.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library MAPK Inhibitor Library Covalent Inhibitor Library Reprogramming Compound Library Anti-Diabetic Compound Library Pyroptosis Compound Library

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Keywords

JNK-IN-8 1410880-22-6 MAPK Tyrosine Kinase/Adaptors JNK c-Kit JNKIN8 JNK Inhibitor XVI Inhibitor JNK IN 8 inhibit inhibitor

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