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IKK-IN-3 is a highly potent and selective inhibitor of IkappaB kinase 2 (IKK2 or IKKβ). It exhibits impressive inhibitory activity against IKK2 (IC50 = 19 nM), while also demonstrating significant efficacy against IKK1 (or IKKα) with an IC50 value of 400 nM.

IKK-IN-1 is an inhibitor of IKK ([Ikappa]B kinase), a protein known to regulate the NF-[kappa]B signaling pathway.

IKK-IN-4 is a potent and selective inhibitor of IkappaB kinase 2 with IC50 values of 45 nM against IKKβ and 650 nM against IKKα [1].

IKK 16 hydrochloride is a selective inhibitor of IKK2 (IC50: 40 nM), the IKK complex (IC50: 70 nM), and IKK1 IκB kinase (IKK) (IC50: 200 nM), as well as leucine-rich repeat kinase-2 (LRRK2; IC50: 50 nM).

IKK 16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

IKKγ NBD Inhibitory Peptide acetate is a NEMO-binding domain peptide (NBD peptide) acetate corresponding to the NEMO amino-terminal alpha-helical region. IKKγ NBD Inhibitory Peptide acetate is shown to block TNF-alpha-induced NF-kB activation.

TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM, respectively).

TBK1 IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε.

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.

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

IKKβ-IN-1 is a potent, orally active inhibitor of IkappaB (IKK-β) with an IC50 of 0.20 μM. It reduces the inhibition of PGE2 and TNF-α production in murine macrophages and protects mice from infection shock-induced death.

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.

IKKß-IN-124 is an allosteric inhibitor of IκBα phosphorylation and NF-κB transcriptional activity through selective capture of the inactive conformation and hence blockade of IKKβ S177/S181 phosphorylation.

TBK1 IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].

TBK1 IKKε-IN-6 (example 110) is a potent inhibitor of TBK1 and IKKε, exhibiting IC50 values below 100 nM for both enzymes.

IKKγ NBD Inhibitory Peptide TFA is a specific NF-κB inhibitor that hinders the interaction between the IKKγ NEMO-binding domain (NBD) and IKKα and IKKβ, effectively preventing TNF-α-induced NF-κB activation. It has been demonstrated to significantly suppress inflammation and improve neurological deficits induced by cerebral ischemia [1] [2] [3].

Wedelolactone (IKK Inhibitor II) inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα.

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.

PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM.

Nikkomycin Z (Nikkomycin Z from Streptomyces tendae) is a competitive chitin synthase inhibitor.It inhibitor of the growth of filamentous fungi, insects, acarids and yeasts.

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.

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.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

A cell-permeable synthetic peptide NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region is shown to block TNF-alpha-induced NF-kB activation. The interaction of IKγNEMO with the IKK complex is vital for t

Nikkomycin pseudo-J is a nikkomycin isolated from Streptomyces tendae.

Nikkomycin M is used as an insecticide.

TBK1 IKKε-IN-1 is a dual inhibitor of TBK1 and IKKε with IC50 values of less than 100 nM.

Nikkomycin is used as an insecticide.

Nikkomycin J is used as an insecticide from Streptomyces tendae.

Nikkomycin N is a bioactive chemical.

FIKK9.1-IN-1 (Compound 1), an antimalarial agent (IC50: 2.68 μg/mL), serves as a FIKK9.1 inhibitor by interacting with the ATP-binding residues within FIKK9.1, thereby disrupting the parasite life cycle and resulting in parasite death [1].

GSK8612 is a highly selective and potent inhibitor of Tank-binding Kinase-1 (TBK1, pIC50: 6.8).

1. Pristimerin (Celastrol methyl ester) has anticancer activity , treatment with Pristimerin may be a potential strategy for the suppression of hypoxia-induced metastasis through the reversal of hypoxia-induced stem cell characteristics and EMT in cancer cells. 2. Pristimerin down-regulates the expression of pro-inflammatory mediators through blocking of NF-κB activation by inhibiting interconnected ROS IKK NF-κB signaling pathways, can effectively inhibit both arthritic inflammation and cartilage and bone damage in the joints.

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.

1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK/NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.

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).

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).

TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes.

IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor that blocks IκBα phosphorylation in the NF-κB pathway.

INH14 is a novel inhibitor of the IKKα β-dependent TLR inflammatory response (IC50s: 8.97 3.59 μM for IKKα IKKβ).

1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS/D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK/NFκB and Jak2/STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.

GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. It suppresses NF-κB activation and transcription of target genes without inhibiting proteasome activity. GS143 has anti-asthm[atic] properties.

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.

BMS-345541 hydrochloride is a selective IKK inhibitor, targeting IKK2 and IKK1 with IC50 values of 0.3 μM and 4 μM, respectively.

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).

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

IMD-0560 is a novel inhibitor of IκB kinase β.

Euscaphic acid has anti-diabetic, and anti-inflammatory activities, it inhibits LPS-induced inflammatory responses by interference with the clustering of TRAF6 with IRAK1 and TAK1, resulting in blocking the activation of IKK and MAPKs signal transduction