JNK-IN-8 (Synonyms: JNK Inhibitor XVI)

Name: JNK-IN-8
Brand: MedChemExpress
SKU: HY-13319
Rating: 5.0 (38 reviews)

Cat. No.: HY-13319 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC₅₀s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

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

JNK-IN-8 Chemical Structure

CAS No. : 1410880-22-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 98	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 98	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 445	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 740	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 935	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 38 publication(s) in Google Scholar

Other Forms of JNK-IN-8:

JNK-IN-8 (GMP) Get quote

36 Publications Citing Use of MCE JNK-IN-8

: JNK-IN-8 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 May 4;37(1):99. [Abstract]; A co-inhibitor of JNK and integrin β obviously decreases phosphorylation levels of JNK and c-JUN and expression of LOXL2 as compared with JNK inhibitor alone or integrin β1 alone.

: JNK-IN-8 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2014 Oct 17;289(42):28753-64. [Abstract]; Effect of the JNK inhibitor (JNK IN 8) on the induction of MKP-1 and MKP-2. RAW264.7 cells are first pretreated with vehicle (DMSO), 3 μM JNK IN 8, 10 μM of U0126, or a combination of both JNK IN 8 and U0126, for 30 min, and then stimulated with LPS for 60 min. Representative images are shown in the panels.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JNK Isoform Specific Products:

View All Isoforms

JNK1 JNK2 JNK3 JNK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

JNK-IN-8 (JNK Inhibitor XVI) is a potent JNK inhibitor with IC₅₀s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively^[1].

IC₅₀ & Target^[1]

JNK3

1 nM (IC₅₀)

JNK1

4.7 nM (IC₅₀)

JNK2

18.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.338 μM Compound: 72	Inhibition of JNK3-mediated c-jun phosphorylation in human A375 cells after 1 hr incubation Inhibition of JNK3-mediated c-jun phosphorylation in human A375 cells after 1 hr incubation	[PMID: 25415535]
HeLa	IC₅₀	0.486 μM Compound: 72	Inhibition of JNK3-mediated c-jun phosphorylation in human HeLa cells after 1 hr incubation Inhibition of JNK3-mediated c-jun phosphorylation in human HeLa cells after 1 hr incubation	[PMID: 25415535]

In Vitro

JNK-IN-8 inhibits phosphorylation of c-Jun, a direct substrate of JNK kinase. JNK-IN-8 inhibits c-Jun phosphorylation in HeLa and A375 cells with EC₅₀ of 486 nM and 338 nM, respectively. JNK-IN-8 also exhibits exceptional selectivity based upon KinomeScan and enzymatic profiling. Cumulatively these combined profiling technologies demonstrate that both JNK-IN-8 and JNK-IN-12 are remarkably selective covalent JNK inhibitors and are appropriate for interrogating JNK-dependent biological phenomena^[1].
JNK-IN-8, a selective pan-JNK inhibitor, is discovered to inhibit JNK kinase by broad-base kinase selectivity profiling of a library of acrylamide kinase inhibitors based on the structure of imatinib using the KinomeSca approach. JNK-IN-8 possess distinct regio-chemistry of the 1,4-dianiline and 1,3-aminobenzoic acid substructures relative to imatinib and uses an N,N-dimethyl butenoic actemide warhead to covalently target Cys154. JNK-IN-8 adopts an L-shaped type I binding conformation to access Cys 154 located towards the lip of the ATP-binding site^[2].

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

Molecular Weight

507.59

Formula

C₂₉H₂₉N₇O₂

CAS No.

1410880-22-6

Appearance

Solid

Color

White to yellow

SMILES

CC1=CC(NC(C2=CC=CC(NC(/C=C/CN(C)C)=O)=C2)=O)=CC=C1NC3=NC=CC(C4=CN=CC=C4)=N3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 35 mg/mL (68.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9701 mL	9.8505 mL	19.7009 mL
5 mM	0.3940 mL	1.9701 mL	3.9402 mL
10 mM	0.1970 mL	0.9850 mL	1.9701 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (4.93 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.93 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(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

Purity: 99.67%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (243 KB) LCMS (98 KB) Elemental Analysis Report (101 KB)

Handling Instructions (2659 KB)

References

[1]. Zhang T, et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54. [Content Brief]

[2]. Liu Q, et al. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol. 2013 Feb 21;20(2):146-59. [Content Brief]

Kinase Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Zhang T, et al. Discovery of potent and selective covalent inhibitors of JNK. Chem Biol. 2012 Jan 27;19(1):140-54. [Content Brief] [2]. Liu Q, et al. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol. 2013 Feb 21;20(2):146-59. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9701 mL	9.8505 mL	19.7009 mL	49.2523 mL
	5 mM	0.3940 mL	1.9701 mL	3.9402 mL	9.8505 mL
	10 mM	0.1970 mL	0.9850 mL	1.9701 mL	4.9252 mL
	15 mM	0.1313 mL	0.6567 mL	1.3134 mL	3.2835 mL
	20 mM	0.0985 mL	0.4925 mL	0.9850 mL	2.4626 mL
	25 mM	0.0788 mL	0.3940 mL	0.7880 mL	1.9701 mL
	30 mM	0.0657 mL	0.3283 mL	0.6567 mL	1.6417 mL
	40 mM	0.0493 mL	0.2463 mL	0.4925 mL	1.2313 mL
	50 mM	0.0394 mL	0.1970 mL	0.3940 mL	0.9850 mL
	60 mM	0.0328 mL	0.1642 mL	0.3283 mL	0.8209 mL

JNK-IN-8 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:

JNK-IN-81410880-22-6JNK Inhibitor XVIJNKc-Jun N-terminal kinaseInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

JNK-IN-8 (Synonyms: JNK Inhibitor XVI)

Customer Review

Other Forms of JNK-IN-8:

JNK-IN-8 Related Antibodies

36 Publications Citing Use of MCE JNK-IN-8

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JNK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

JNK-IN-8 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

JNK-IN-8 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report