AP-1/NF-κB activation inhibitor 1

Name: AP-1/NF-κB activation inhibitor 1
Brand: MedChemExpress
SKU: HY-133987
Rating: 4.5 (1 reviews)

Cat. No.: HY-133987 Purity: 99.03%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC₅₀=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.

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

AP-1/NF-κB activation inhibitor 1 Chemical Structure

CAS No. : 188936-12-1

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 220	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 220	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 670	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 930	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE AP-1/NF-κB activation inhibitor 1

•Arthritis Res Ther. 2023 Jul 19;25(1):121. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	1 μM Compound: 39	Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay Inhibition of AP-1-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay	[PMID: 24831826]
Jurkat	IC₅₀	1 μM Compound: 39	Inhibition of NF-kappaB-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay Inhibition of NF-kappaB-mediated transcriptional activation in human Jurkat cells by luciferase reporter gene assay	[PMID: 24831826]

Molecular Weight

344.25

Formula

C₁₃H₁₁F₃N₄O₄

CAS No.

188936-12-1

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CN=C(C(F)(F)F)N=C1NN2C(C(C)=CC2=O)=O)OCC

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 : 250 mg/mL (726.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9049 mL	14.5243 mL	29.0487 mL
5 mM	0.5810 mL	2.9049 mL	5.8097 mL
10 mM	0.2905 mL	1.4524 mL	2.9049 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: ≥ 2.08 mg/mL (6.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 99.03%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (257 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Palanki MS, et al. Novel inhibitors of AP-1 and NF-kappaB mediated gene expression: structure-activity relationship studies of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)++ +pyrimidi ne-5-carboxylate. Bioorg Med Chem Lett. 2000;1 [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.9049 mL	14.5243 mL	29.0487 mL	72.6216 mL
	5 mM	0.5810 mL	2.9049 mL	5.8097 mL	14.5243 mL
	10 mM	0.2905 mL	1.4524 mL	2.9049 mL	7.2622 mL
	15 mM	0.1937 mL	0.9683 mL	1.9366 mL	4.8414 mL
	20 mM	0.1452 mL	0.7262 mL	1.4524 mL	3.6311 mL
	25 mM	0.1162 mL	0.5810 mL	1.1619 mL	2.9049 mL
	30 mM	0.0968 mL	0.4841 mL	0.9683 mL	2.4207 mL
	40 mM	0.0726 mL	0.3631 mL	0.7262 mL	1.8155 mL
	50 mM	0.0581 mL	0.2905 mL	0.5810 mL	1.4524 mL
	60 mM	0.0484 mL	0.2421 mL	0.4841 mL	1.2104 mL
	80 mM	0.0363 mL	0.1816 mL	0.3631 mL	0.9078 mL
	100 mM	0.0290 mL	0.1452 mL	0.2905 mL	0.7262 mL