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JSH-23 NF-κB inhibitor

Name: JSH-23
Brand: Selleck Chemicals
SKU: S7351
Availability: InStock
Rating: 5 (166 reviews)

Cat.No.S7351

JSH-23 is an inhibitor of NF-κB transcriptional activity, which inhibits LPS-stimulated nuclear factor (NF)-κB transcriptional activity in RAW 264.7 cells with an IC50 value of 7.1 μM, and interferes with LPS-induced NF-κB nuclear translocation without affecting IκB degradation.

Chemical Structure

Molecular Weight: 240.34

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Quality Control

Batch: Purity: 99.58%

99.58

Related Targets	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Other NF-κB Products	Omaveloxolone (RTA-408) DCZ0415 BAY 11-7082 (BAY 11-7821) QNZ (EVP4593) SC75741 Caffeic Acid Phenethyl Ester DHA (Dihydroartemisinin) Andrographolide Evodiamine Withaferin A (WFA)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
HK-2 cells	Function assay	100 μM	3 h	pretreatment with JSH-23 effectively blocked Ang II-induced nuclear p65 accumulation	30874544
U2OS/DR-GFP cells	Function assay	10 and 20 µM		JSH-23 treatment significantly decreased the HR frequency	30770924
MCF-7:5C	Function assay	20 μmol/L	3 and 6 days	JSH-23 completely blocked E2-induced apoptosis in MCF-7:5C cells	30224430
MCF-7:2A	Function assay	20 μmol/L	3 and 6 days	JSH-23 increased E2-induced apoptosis in MCF-7:2A cells	30224430
BMDM	Function assay	60 μM	19-24 h	JSH-23 (60 μM) induced a decrease of IL-1β release	30138321
HL60 cells	Function assay	10 μM	48 h	JSH-23 (10 μM) obviously decreased NF-κB DNA binding activity	30125548
BV2 cells	Function assay	30 μM	1 h	pretreatment of JSH-23 decreased the levels of IL-6 and NO production in LPS-stimulated microglia.	29890414
A549 cells	Cell viability assay	5, 10, 20, 30, 40 and 50 μM	24 h	with the increase in JSH-23 concentration, the inhibition rate for cell viability was gradually increased, and significant differences existed when the JSH-23 concentration was greater than 20 μM.	28281961
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (199.71 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (20.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	240.34	Formula	C₁₆H₂₀N₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	749886-87-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC(=C(C=C1)NCCCC2=CC=CC=C2)N

Mechanism of Action

Targets/IC₅₀/Ki	NF-κB (RAW 264.7 cells) 7.1 μM
In vitro	JSH-23 inhibits LPS-induced nuclear translocation of NF-κB p65 without affecting IκBα degradation. This compound inhibits LPS-induced apoptotic chromatin condensation, while does not show significant cytotoxic effects on the RAW 264.7 cells at <100 μM. It also decreases NO production and neuronal migration in LPS activated cultures primary cultures from developing mouse cerebellum. Moreover, this chemical augments cisplatin cytotoxicity in ovarian cancer cells with CI values ranging from 0.35 to 0.85.
Kinase Assay	Measurement of NF-κB transcriptional activity
Kinase Assay	Macrophages RAW 264.7 transfected stably with reporter plasmid of pNF-κB-SEAP-NPT are treated with 1 μg/ml LPS and/or sample for 16 hours. As the reporter, SEAP activity in the cell-free culture media is measured as followed. Single cell-derived stable transfectants are plated in 5 ml of T-25 flask, and the media is decanted 24 h later. At this time, cells are washed twice with phosphate-buffered saline, and incubations are initiated by addition of new media. This compound is added to the culture medium after 24 h of incubations. Aliquots (25 ml) of medium from a control or chemical-treated cultures are taken at 0, 3, 20, 24, 48, and 72 h, heated at 65°C for 5 min to eliminate the alkaline phosphatase activity, and used immediately or stored at -20°C. Mixtures consisting of dilution buffer (25 ml), assay buffer (97 ml), culture media (25 ml), and 4-methylumbelliferyl phosphate (MUP, 1 mM, 3 ml) in each well of the 96-well plates are incubated for 60 min in the dark at room temperature. Fluorescence emits the product of the SEAP/MUP is measured at 449 nm using a 96-well plate fluorometer after excitation at 360 nm.
In vivo	JSH-23 (3 mg/kg) significantly reverses the nerve conduction and nerve blood flow deficits by decreasing neuroinflammation and improving antioxidant defence in diabetic rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15280016/ [2] https://pubmed.ncbi.nlm.nih.gov/20955790/ [3] https://pubmed.ncbi.nlm.nih.gov/24418212/ [4] https://pubmed.ncbi.nlm.nih.gov/21447040/