Apoptose

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

ZINC00784494 is a selective inhibitor of LCN2 (lipocalin-2), which inhibits cancer cell proliferation and reduces p-AKT , and promotes apoptosis. IBC.

Lepadin H, a marine alkaloid and ferroptosis inducer, exhibits significant cytotoxicity by promoting p53 expression, escalating ROS production, and enhancing

APE1-IN-2 (AP1), a Pt(IV) proagent, targets APE1 protein, induces DNA damage, and triggers apoptosis with anticancer effects.

13h (hGGPPS-IN-3), a strong C2-ThP-BPs hGGPPS blocker, triggers MM cell apoptosis and shows in vivo anti-myeloma effects.

Antitumor Agent-92, a derivative of Icaritin, halts cell cycle, triggers cell death, and is promising for liver cancer study.

RIP1 Kinase Inhibitor 8 (Compound 77), a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor, exhibits an IC50 of 20 nM and effectively

Antitumor Agent-110 (Compound 13), an imidazotetrazine anticancer agent, exhibits excellent permeability.

S-Adenosyl-L-methionine (SAMe) 1,4-butanedisulfonate functions as an orally active methyl group donor and serves as a dietary supplement known for its

Sirt1/2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1/2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively.

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

Ac-YVAD-pNA, a specific substrate for Caspase-1, serves to detect Caspase-1 activity, a crucial mediator of inflammatory processes [1] [2].

Cis-3,4',5-Trimethoxy-3'-hydroxystilbene, a stilbene derivative, induces apoptosis through the mitochondrial release of cytochrome c and suppresses tubulin polymerization. It is also noted for its application in leukemic research [1].

Purinostat mesylate, a selective HDAC inhibitor (IC50: 0.81-11.5 nM), induces apoptosis and has potent anti-leukemic effects.

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage.

AR420626: selective FA3R agonist, guards against SALS, effects blocked by BHB, a FA3R antagonist.

Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

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.

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.