SC75741 NF-κB inhibitor

Cat.No.S7273

SC75741 is a potent NF-κB inhibitor with EC50 of 200 nM. This compound efficiently blocks influenza virus propagation.
SC75741 NF-κB inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 565.67

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 cells Function assay 5 h Inhibition of NF-kappaB in A549 cells after 5 hrs by reporter gene assay, EC50=0.2 μM 17869512
PBMC Proliferation assay Antiproliferative activity against human PBMC, IC50=2.2 μM 17869512
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 565.67 Formula

C29H23N7O2S2

Storage (From the date of receipt)
CAS No. 913822-46-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1C2=NC(=CS2)C(=O)NC3=NC4=C(N3)C=C(C=C4)C(=O)C5=CC=CC=C5)C6=NC=NC7=C6SC=C7

Solubility

In vitro
Batch:

DMSO : 41 mg/mL ( (72.48 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
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Mechanism of Action

Features
NF-κB-selective inhibitor.
Targets/IC50/Ki
NF-κB [1]
(Cell-based NF-κB reporter gene assay)
200 nM(EC50)
In vitro
SC75741 shows immunosuppressive activity by inhibiting human PBMC proliferation with IC50 of 2.2 μM. [1] This compound inhibits replication of influenza A and B viruses by inhibiting NF-κB-mediated signalling on a transcriptional level. Moreover, it shows a high barrier for development of resistant virus variants. [2]
Kinase Assay
NF-κB reporter gene assay
The NF-κB reporter gene assay is prepared with A549-NF-κB-SEAP cell line according to manufacturer’s instructions. In short, A549 cells stably transfected with pNF-κB-SEAP reporter gene plasmid are plated and allowed to attach overnight. The cells are subsequently incubated for 5 h with described compounds at 100, 30, 10, 3, 1, 0.3, 0.1, and 0 μM and then stimulated with 10 ng/ml TNF-α for 22 h. The supernatant of the cell is analyzed for SEAP activity using a chemiluminescent SEAP reporter gene assay.
In vivo
SC75741 (15 mg/kg i.p.) reduces virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection. [2]
References

Applications

Methods Biomarkers Images PMID
Western blot TRIM44 / Vimentin / E-cadherin / Slug / p-p65 / p-AKT S7273-WB1 30922374
Immunofluorescence NF-κB(p65) S7273-IF1 27447570

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