ikkε

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).

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

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.

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

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

TBK1 IKKε-IN-3, a potent IP6K inhibitor, exhibits IC50 values of 3, 8.65, and 3.72 μM for IP6K1, IP6K2, and IP6K3, respectively. It is applicable in obesity disease research. [1]

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.

BAY32-5915 is an inhibitor of IKKalpha.

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).

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.

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

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.

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.

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

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

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

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].

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.

MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.

MRT199665 is an effective and ATP-competitive, selective MARK SIK AMPK inhibitor (IC50s of 2 2 3 2 nM, 10 10 nM, and 110 12 43 nM for MARK1 MARK2 MARK3 MARK14, AMPKα1 AMPKα2, and SIK1 SIK2 SIK3, respectively). MRT199665 suppresses the phosphorylation of S