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GS143 is a β-TrCP1 ligase inhibitor. GS143 inhibits IκBα ubiquitination (IC50 = 5.2 μM) without affecting proteasome activity. GS143 blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. GS143 suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.
| Molecular Weight | 466.46 |
| Formula | C28H19FN2O4 |
| CAS Number | 916232-21-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IκB/IKK Products |
|---|
| BAY 11-7082
BAY 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation (IC50 ~ 10 μM). BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). |
| SC-514
SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) with IC50 of 3-12 μM. |
| TPCA-1
TPCA-1 is an inhibitor of IKK-2 with IC50 of 17.9 nM. |
| BMS-345541 hydrochloride
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IC50 values of 0.3 μM and 4 μM for IKK-2 and IKK-1 respectively). BMS-345541 binds at an allosteric site of IKK. |
| Bardoxolone Methyl
Bardoxolone Methyl is an IKK inhibitor with potent pro-apoptotic and anti-inflammatory activities, as well as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway. |
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