Apoptose

<p>Bcl-2-IN-13 is a potent inhibitor of Bcl-2, exhibiting an IC50 of 17 nM, and holds potential for use in cancer research [1].</p>

<p>CR-1-31-B, a synthetic rocaglate, inhibits eIF4A, hinders protein synthesis initiation, and induces apoptosis in cancer cells.</p>

<p>eIF4A3-IN-18, a silvestrol analogue with EC50s: 0.8/35/2 nM, inhibits eIF4F complex and is cytotoxic (LC50: 0.06 nM) for cancer research.</p>

<p>HS148 selectively inhibits DAPK3 (Ki 119 nM), reducing gastric cancer progression via ULK1-dependent autophagy and tumor suppression pathways.</p>

<p>Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC) with IC50 values of 4</p>

<p>c-Met/HDAC-IN-3: dual inhibitor; IC50: c-Met 12.5 nM, HDAC1 26.97 nM; induces apoptosis, G2/M arrest.</p>

<p>SWS1, a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM), displays anticancer activity by augmenting tumor-infiltrating lymphocytes and demonstrating anti</p>

<p>PD-1-IN-1 is a programmed cell dealth-1inhibitor. PD-1-IN-1 can be used as an immune modulator.</p>

<p>PF-07284892 (ARRY-558) is an orally active allosteric SHP2 inhibitor (IC50 = 21 nM) that reduces pERK expression and may be employed in solid tumour research.</p>

<p>Ataquimast is used in curing advanced receptor-positive breast cancer.</p>

<p>N-Oleoyl serinol, a ceramide analog, plays a crucial role in stem cell therapy by inhibiting the development of teratomas in stem cells. It triggers apoptosis in remaining pluripotent embryoid body-derived cells (EBCs), thwarts teratoma formation, and promotes the enrichment of EBC cells that proceed to neural differentiation post-transplantation [1].</p>

<p>Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.</p>

<p>BTM-3528 is a mitochondrial protease OMA1 activator that induces an overactivation of the mitochondrial integrated stress response (ISR).</p>

<p>Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide derived from bovine lactoferrin spanning residues 17-41, exhibits broad-spectrum antimicrobial properties against Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. Additionally, this compound demonstrates antitumor activities [1] [2].</p>

<p>BMS-561392 formate, the formate derivative of BMS-561392, functions as a TNF alpha-converting enzyme (TACE) inhibitor and an ADAM17 blocker. It is utilized in the research of inflammatory bowel disease [1] [2].</p>

<p>GCN2-IN-6: Potent, oral GCN2/PERK inhibitor; IC50s - GCN2: 1.8 nM (enzymatic), 9.3 nM (cellular); PERK: 0.26 nM (enzymatic), 230 nM (cellular).</p>

<p>AGN194204 (IRX4204), an oral RXR agonist, inactive against RAR, has Kd 0.4-3.8 nM &amp; EC50 0.08-0.8 nM, with anti-inflammatory and anticarcinogenic properties.</p>

<p>HDAC-IN-59 (compound 13a), a potent histone deacetylase (HDAC) inhibitor, enhances intracellular reactive oxygen species (ROS) production, induces DNA damage,</p>

<p>DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP.</p>

<p>MI-219 is a human double minute 2 (HDM2) inhibitor.</p>

<p>Compound A5b, also known as JMJD3/HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone</p>

<p>BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM).</p>

<p>Boserolimab (MK-5890) is a chimeric, humanized IgG1κ antibody that targets the signaling regulatory protein CD27 in mice.</p>

<p>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.</p>

<p>Tubulin Polymerization-IN-56 (compound 8l), an indazole derivative, potently inhibits tubulin polymerization by targeting the colchicine site, which induces</p>

<p>NBI-961, a potent NEK2 inhibitor, suppresses proteasomal degradation and effectively induces G2/mitosis arrest and apoptosis within diffuse large B cell</p>

<p>HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1.</p>

<p>Cerivastatin is an HMG-CoA reductase inhibitor with anticancer and lipid-lowering effects and can be used to study primary hyperlipidemia.</p>

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

<p>PD-1/PD-L1-IN-22 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interactions that blocks PD-1/PD-L1 interactions (IC50: 0.732 μM).</p>

<p>c-Met-IN-10: potent kinase inhibitor (IC50=16 nM), halts cancer cell activity/movement, induces apoptosis, for anticancer research.</p>

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

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

<p>4E2RCat is an inhibitor of eIF4E-eIF4G interaction (IC50 = 13.5 μM) and is capable of blocking coronavirus replication as monitored by viral protein expression</p>

<p>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.</p>

Atiprimod Dimaleate is a JAK2 inhibitor.

<p>Topoisomerase II inhibitor 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].</p>

<p>NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].</p>

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

<p>GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively</p>

<p>CIL62 is a caspase-3/7-independent inducer of cell death. The mechanism of action of CIL62 is Necrostatin-1 dependent cell death [1].</p>

<p>K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM.</p>

<p>CHM-1 is an inducer of apoptosis, and displays potent antitumor ability in human hepatocellular carcinoma by activation of Cdc2 kinase activity.</p>

<p>MY-673, a colchicine binding site inhibitor (CBSI), impedes tubulin polymerization and disrupts the ERK signaling pathway, consequently modulating SMAD4 protein</p>

<p>eIF4A3-IN-9, a silvestrol analogue, disrupts eIF4F complex assembly; EC50s: 29/450/80 nM (myc/tub-LUC, MB-231 cells); for cancer research.</p>

<p>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.</p>

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

<p>Mcl-1 Inhibitor 17 is a compound that functions as an inhibitor of the Mcl-1 protein, specifically designed for use in cancer and other disease research [1].</p>

<p>DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM respectively. It hinders the proliferation of cancer cells such as MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 values of 0.3 μM, 2.7 μM, and 2.41 μM respectively. Additionally, DLC-50 induces apoptosis in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase.</p>

<p>Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.</p>