a-549

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

Lonidamine (Diclondazolic Acid) is an indazole carboxylic acid derivative, principally inhibiting aerobic glycolytic activity, by its effect on mitochondrially-bound hexokinase (HK).

Chloramphenicol (Chloromycetin) is a broad-spectrum antibiotic that inhibits the biosynthesis of bacterial proteins. Chloramphenicol acts primarily on the 50S subunit of the bacterial 70S ribosome and is active against peptidyltransferases, inhibiting the formation of peptide bonds.

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

SBI-797812 is structurally similar to active-site directed inhibitor of NAMPT(NAMPT with EC50 of 0.37 μM).

GPNA hydrochloride is specific glutamine (Gln) transporter ASCT2(SLC1A5) inhibitor. GPNA reversibly induces apoptosis in A549 cells. GPNA hydrochloride is a well-known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride also inhibits

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.

Prucalopride (R-93877) is a selective, high-affinity 5-HT4A/4B receptor agonist (Ki: 2.5/8 nM). It has >290-fold selectivity for 5-HT4A/4B receptor than other 5-HT receptor subtypes.

Cyasterone (Cyasteron), a natural EGFR inhibitor, can inhibit the growth of A549 and MGC823 cells, via regulating EGFR signaling pathway, it may be a promising anti-cancer agent. Cyasterone has antifeeding activity.

Sertaconazole is a broad-spectrum antifungal.

Flupentixol dihydrochloride is used in therapy of schizophrenia as well as in anxiolytic and depressive disorders.

Sphondin has anticonvulsant, anti-inflammatory, and anti-proliferative activities, it possessed an inhibitory effect on IL-1beta-induced increase in the level of COX-2 protein and PGE(2) release in A549 cells.

MM41 is a human telomeric and gene promoter DNA quadruplex stabilizer with an IC50 of <10 nM against the MIA PaCa-2 pancreatic cancer cell line.

Tanespimycin (KOS 953) is an Hsp90 inhibitor (IC50=5 nM) and is selective. Tanespimycin depletes intracellular STK38/NDR1 and decreases STK38 kinase activity. Tanespimycin also downregulated stk38 gene expression.

Sertaconazole nitrate (FI-7045), a topical broad-spectrum antifungal, is developed to supply an additional agent for the treatment of superficial cutaneous and mucosal infections.

5'-Fluoroindirubinoxime (5'-FIO) is a potent FLT3 inhibitor( IC50 : 15 nM).

DMG-PEG2000 (DMG-PEG2000) can be used for the preparation of lipid nanoparticles for oral delivery of plasmid DNA in vivo to improve the mucus permeability and delivery efficiency of nanoparticles. DMG-PEG 2000 can be used for the preparation of siRNA transfected liposomes, which can improve the transfection efficiency.

NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-) is a potent NF-κB signaling pathway inhibitor. It is a 4-arylidene crucumin analogue. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.

SU0268 is a potent and specific 8-Oxoguanine DNA glycosylase 1 (OGG1) inhibitor that regulates inflammatory responses during Pseudomonas aeruginosa infection.

M2N12 is a potent and highly selective inhibitor of cell division cycle 25C protein phosphatase (Cdc25C, IC50 = 0.09 μM) and also exhibits anti-tumor activity. Additionally, M2N12 shows promising activity against Cdc25A (IC50 = 0.53 μM) and Cdc25B (IC50 = 1.39 μM).

Demethoxydeacetoxypseudolaric acid B analog has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM. and is semi-synthesized by efficient routines from Pseudolaric acid B.

GPX4-IN-15 (Compound C1) is an inhibitor of GPX4, demonstrating an inhibition rate of 19.8% at a concentration of 1 μM. This compound effectively inhibits the proliferation of cancer cell lines MDA-MB-468, BT-549, and MDA-MB-231, with IC50 values of 0.86 μM, 0.96 μM, and 0.48 μM respectively.

Aromatase-IN-4 (Compound 6a) is an inhibitor of the enzyme aromatase. It displays anticancer properties, with GI50 values for different cell lines as follows: 2.95 μM for MDAMB-231, 3.35 μM for MCF-7, 2.27 μM for A-549, 8.46 nM for NCI-H23, and 1.56 μM for A-498. Aromatase-IN-4 effectively blocks the estrogen production that depends on aromatase.