ikk-α

Tizoxanide (Desacetyl-nitazoxanide) is a metabolite of lamivudine. Lamivudine (2', 3'-dideoxy-3'-thiacytidine, commonly called 3TC) is a potent nucleoside analog reverse transcriptase inhibitor (nRTI).

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19 0.96 μM).

ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective inhibitor of IKK-β with an IC50 of 8.5 nM.

BMS-345541 (IKK Inhibitor III) is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.

CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.

Vinpocetine (RGH-4405) is a selective inhibitor of cyclic GMP phosphodiesterase (PDE).

Oxaprozin (Oxaprozinum) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of oxaprozin is as a Cyclooxygenase Inhibitor. The chemical classification of oxaprozin is Nonsteroidal Anti-inflammatory Compounds.

BAY32-5915 is an inhibitor of IKKalpha.

SC-514 (GK 01140) is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.

Dehydrocostus Lactone ((-)-Dehydrocostus lactone) shows anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.

2-AMINO-5-PHENYL-THIOPHENE-3-CARBOXYLIC is Inhibitior of IKKβ.

ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β. ACHP has anti-HIV-1 activity and inhibits HIV-1 long terminal repeat (LTR)-driven gene expression through inhibition of NF-κB activation, inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR, and inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR. ACHKP has anti-HIV-1 activity and inhibits TNF-α-induced recruitment of NF-κB (p65) to the HIV-1 LTR.

Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

LY2409881 trihydrochloride is a novel specific inhibitor of IKK2 (IC50: 30 nM); IC50 for IKK1 and other common kinases is at least one log higher.

CAY10575 (IKK2-IN-3) is a potent IKK2 inhibitor with potential anti-inflammatory activity for the study of inflammatory and endocrine diseases.

Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an antioxidant effect.

BOT-64 is an IKK-2 inhibitor which targets the Ser177 and or Ser181 residues in the kinase's activation loop domain.BOT-64 is a cell-permeable benzoxathiole compound

JTP-0819958 is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM[1]. JTP-0819958 suppress LUBAC-mediated NF-kB activation in vitro[2].

Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin A shows estrogenic activity with ligand-binding activity of estrogen receptor, transcriptional activity of estrogen-responsive element-luciferase reporter genes. Broussonin A c

Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.

IKK2-IN-4(IKK2 Inhibitor VI) is a highly potent IKK-2 inhibitor with an IC50 value of 25 nM. IKK2-IN-4 inhibited the production of TNF-α in PBMC induced by LPS.