tank-1

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

Lanepitant (LY303870) is a nonpeptide neurokinin-1 (NK-1) antagonist with analgesic activity that inhibits neurogenic dura mater inflammation and is used for the prevention of migraine.

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

MRT-68601 HCl, a potent TBK1 (TANK-binding kinase-1), inhibits the formation of autophagosomes in lung cancer cells.

2,3,4,5-Tetrachlorophenol is a metabolite of the insecticide γ-lindane.1It is toxic to fathead minnows and rainbow trout (LC50s = 0.496 and 0.304 mg/L, respectively, in tank water).2 1.Chadwick, R.W., and Freal, J.J.The identification of five unreported lindane metabolites recovered from rat urineBull. Environ. Contam. Toxicol.7(2)137-146(1972) 2.Holcombe, G.W., Phipps, G.L., Knuth, L., et al.The acute toxicity of selected substituted phenols, benzenes and benzoic acid esters to fathead minnows Pimephales promelasEnviron. Pollut.35(4)367-381(1984)

BDW568, a prodrug of BDW-OH, serves as a stimulator of interferon genes (STING) agonist. This compound effectively induces STING transcriptional activity, evidenced by a reporter assay in THP-1 cells, with an EC50 value of 7.6 µM. Furthermore, at a concentration of 50 µM, BDW568 prompts phosphorylation of TANK-binding kinase 1 (TBK1) and IFN regulatory factor 3 (IRF3) within THP-1 cells, showcasing its biochemical activity in cellular signaling pathways.

STING agonist D61 is a compound that activates the stimulator of interferon genes (STING), leading to the induction of IFN3-inducible secreted alkaline phosphatase (SEAP) and IFN-β-inducible reporter genes in cellular assays, with half-maximal effective concentrations (EC50s) of 52.9 and 116 nM, respectively. At concentrations of 4, 6, and 8 µM, D61 enhances the production of IFN-β and chemokine (C-X-C motif) ligand 10 (CXCL10) mRNA, as well as the phosphorylation of TANK-binding kinase 1 (TBK1), IRF3, and STING in THP-1 monocytes. Additionally, when administered at a dose of 0.25 mg/kg every other day, D61 effectively reduces tumor volume in a CT26 murine colon cancer model without impacting the body weight of the subjects.

TBK1-IN-1 is a specific and potent TANK-binding kinase 1 (TBK1) inhibitor (IC50: 22.4 nM) with anticancer activity.TBK1-IN-1 inhibits the expression of TBK1 downstream target genes, cxcl10 and ifnβ.

Potent TBK1 (TANK-binding kinase-1) inhibitor (IC50 = 6 nM). Inhibits the formation of autophagosomes in lung cancer cells. Newman et al (2012) TBK1 kinase addiction in lung cancer cells is mediated via autophagy of Tax1bp1/Ndp52 and non-canonical NF-κB signalling. PLoS ONE 7 e50672 PMID:23209807 |McIver et al (2012) Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKKe kinases. Bioorg.Med.Chem.Lett. 22 7169 PMID:23099093