research use only
Cat.No.S7273
| Related Targets | HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD |
|---|---|
| Other NF-κB Inhibitors | Omaveloxolone (RTA-408) DCZ0415 BAY 11-7082 (BAY 11-7821) JSH-23 QNZ (EVP4593) Caffeic Acid Phenethyl Ester DHA (Dihydroartemisinin) Andrographolide Evodiamine Withaferin A (WFA) |
| 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 | ||||||
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In vitro |
DMSO
: 41 mg/mL
(72.48 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
Calculation results:
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.
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| Molecular Weight | 565.67 | Formula | C29H23N7O2S2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 913822-46-5 | Download SDF | Storage of Stock Solutions |
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| 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 | ||
| Features |
NF-κB-selective inhibitor.
|
|---|---|
| Targets/IC50/Ki |
NF-κB
(Cell-based NF-κB reporter gene assay) 200 nM(EC50)
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| In vitro |
SC75741 shows immunosuppressive activity by inhibiting human PBMC proliferation with IC50 of 2.2 μM. 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.
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| Kinase Assay |
NF-κB reporter gene assay
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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.
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| In vivo |
SC75741 (15 mg/kg i.p.) reduces virus replication and cytokine expression in mice lungs after H5N1 influenza virus infection.
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References |
|
| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | TRIM44 / Vimentin / E-cadherin / Slug / p-p65 / p-AKT |
|
30922374 |
| Immunofluorescence | NF-κB(p65) |
|
27447570 |
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