Apoptose

WNY1613: Potent PI3Kδ inhibitor with anti-NHL properties, induces apoptosis in cells, affects phosphorylation in vitro/in vivo.

Pelcitoclax (APG-1252) is a powerful inhibitor of the Bcl-2 and Bcl-xl proteins, displaying significant antineoplastic and pro-apoptotic properties[1].

Compound D16 (Anticancer agent 168) is an inhibitor of DNA2 that induces apoptosis and cell-cycle arrest predominantly in the S-phase.

HA-14-1, a small molecule, binds the surface pocket of Bcl-2 proteins (IC50= ~ 9 µM), including Bcl-xl and Bcl-W, and disrupts their interaction with the Bak peptide. This action induces apoptosis by activating Apaf-1 and caspase-9 and -3. Additionally, HA-14-1 effectively induces apoptosis in human acute myeloid leukemia (HL-60) cells, with a 50 µM concentration resulting in a 90% loss of cell viability.

PLK1-IN-4 is a selective PLK1 inhibitor, antiproliferative , induces cell cycle arrest and apoptosis, making it suitable for hepatocellular carcinoma research.

Photosensitizer-2 (compound 1), an organic D-π-A sensitizer, exhibits antitumor properties and potent phototoxicity due to an acrylic acid moiety.

M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.

LY303511, a structural analog of LY294002, selectively inhibits mTOR-dependent phosphorylation of S6K, unlike its counterpart, which acts as a phosphatidylinositol 3-kinase (PI3K) inhibitor. It effectively reduces cell proliferation in human lung epithelial adenocarcinoma cells by hindering G2/M phase progression and suppressing casein kinase 2 activity. Additionally, LY303511 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitivity in HeLa cells resistant to TRAIL-induced apoptosis and blocks voltage-gated potassium (Kv) channels.

WEHI-345 is a potent and selective RIPK2 inhibitor which shows NOD signalling events yet prevents inflammatory cytokine production.

"HSP90/mTOR-IN-1 is a dual Hsp90/mTOR inhibitor (IC50: 69/29 nM), halting SW780 cell growth and inducing apoptosis/autophagy in cancer research."

Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.

Bcl-2-IN-16 is a Bcl-2 (B-cell lymphoma 2) inhibitor [1].

MTP, a PKM2 inhibitor, promotes apoptosis in cancer cells via caspase-3 activation while also inducing autophagy and enhancing ROS generation.

NSC194598 is a p53 DNA-binding inhibitor, demonstrating an in vitro IC50 of 180 nM and an in vivo range of 2-40 μM.

HAPSBC, an S-benzyl iron chelator, modulates the intracellular distribution of ^59Fe [1].

10-OAHSA is a newly discovered endogenous lipid categorized within the group of branched fatty acid esters of hydroxy fatty acids (FAHFAs). This specific FAHFA comprises oleic acid esterified to 10-hydroxy stearic acid. It stands out among its FAHFA counterparts for its potential bioactive properties, similar to other members of its family such as PAHSAs, which are notably prevalent in the adipose tissue of AG4OX mice exhibiting glucose tolerance due to overexpression of the Glut4 glucose transporter specifically in adipose tissue. Like other FAHFAs, 10-OAHSA may play significant roles in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, which suggests its importance in managing metabolic syndrome and inflammation.

Potent γ-secretase inhibitor; IC50: 1.2 nM (cell), 6.2 nM (cell-free); lowers Aβ in mice/guinea pigs' brain, CSF, plasma.

viFSP1, a species-independent FSP1 inhibitor, effectively induces ferroptosis in FSP1-dependent cells by targeting the highly conserved NAD(P)H binding pocket of FSP1, directly inhibiting its activity. This action results in lipid peroxidation and exhibits anticancer activity [1].

PIM447 (LGH447) is a pan-PIM kinase inhibitor with anti-tumor and bone protective effects. PIM447 reduces the viability, and motility of HuH6 cell.

Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on