Apoptosi

<p>GGTI2417 blocks Geranylgeranyltransferase I, targeting RalB for apoptosis and RalA to stop growth.</p>

<p>PIM447 (LGH447) is a pan-PIM kinase inhibitor with anti-tumor and bone protective effects. PIM447 reduces the viability, and motility of HuH6 cell.</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>TL02-59: Fgr inhibitor (IC50=0.03nM), also targets Lyn (0.1nM), Hck (160nM), halts acute myelogenous leukemia growth.</p>

<p>Prostaglandin A1, a dehydration derivative of Prostaglandin E1, demonstrates inhibitory effects on tumor growth, inflammation, virus replication, platelet aggregation, and excitotoxin-induced neuron apoptosis [1].</p>

<p>Antitumor Agent-110 (Compound 13), an imidazotetrazine anticancer agent, exhibits excellent permeability.</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>MRT199665, a selective MARK/SIK/AMPK inhibitor, blocks SIK CRTC3 S370 phosphorylation and triggers apoptosis in AML cells.</p>

<p>Ac-Val-Ala-Asp-CHO (Ac-VAD-CHO) serves as a pan-caspase inhibitor and preserves mitochondrial membrane potential (MMP) while preventing the release of</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>SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.</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>RET-IN-5 is a potent inhibitor of RET (IC50: 4.57 nM).</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>Anticancer agent 128 (compound 1) is an IAP inhibitor that covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, exhibiting IC50 values of 24.9 nM, 19</p>

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

<p>Merodantoin induces apoptosis in KRAS-mutant cancer cells via ROS-autophagy and Akt pathway.</p>

<p>BQZ-485, a potent GDI2 inhibitor, interacts with Tyr245 to disrupt the native GDI2-Rab1A interaction.</p>

<p>SC 67655 is a peptidomimetic that specifically suppresses human leukocyte antigen DRB10401-restricted T cell proliferation.</p>

<p>AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.</p>

<p>Ponicidin, a diterpenoid from Rabdosia rubescens, has immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer properties.</p>

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

<p>HM90822 is an IAP antagonist that inhibits XIAP and cIAP1/2 protein expression, induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.</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>BTM-3566 triggers ISR via OMA1, induces apoptosis in cancer cells, and is used to research DLBCL.</p>

<p>PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor demonstrating an inhibition concentration (IC50) of 0.6 ± 0.1 nM.</p>

<p>BHD, a reversible male contraceptive agent, effectively induces spermatogenic cell apoptosis and causes abnormalities in seminiferous tubules in vivo at doses</p>

<p>Q-VD-OPh: broad-spectrum, non-toxic caspase inhibitor; cost-effective, specific for apoptotic inhibition.</p>

<p>WYE-125132: potent mTOR inhibitor, IC50 0.19 nM, selective over PI3Ks/hSMG1/ATR.</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>Anticancer agent 127 (142D6), an IAP inhibitor, covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, with IC50 values of 12 nM, 14 nM, and 9 nM,</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>Potent EGFR blocker; acts on WT, L858R/T790M (IC50: 1.7 nM), less on T790M/C797S; stalls cell cycle, induces apoptosis, deters metastasis.</p>

<p>SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.</p>

<p>CPUY201112, a novel inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells.</p>

<p>Anticancer agent 105, a thienopyrimidine scaffold-based compound, exhibits selective toxicity towards melanoma and induces apoptosis.</p>

<p>Bcl-2-IN-12 (Compound 1) is a potent Bcl-2 inhibitor with an IC50 value of 6 nM, utilized in cancer research [1].</p>

<p>Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.</p>

<p>Atiprimod Dimaleate is a JAK2 inhibitor.</p>

<p>RET-IN-13: potent quinoline RET inhibitor; IC50 = 0.5 nM (WT), 0.9 nM (V804M); potential for RET-related tumor/intestinal disease research.</p>

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

<p>2-Chlorophenoxazine is an Akt inhibitor that demonstrates an in vitro inhibitory concentration (IC50) of 2-5 μM and has the capacity to induce apoptosis.</p>

<p>RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their</p>

<p>TMX-2164: strong, irreversible BCL6 inhibitor, IC50=152 nM, long-lasting action, inhibits cell proliferation.</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>FHND5071, a potent and selective RET kinase inhibitor, exerts antitumor effects through the inhibition of RET autophosphorylation and may be utilized for tumor</p>

<p>USP7-IN-3 is a potent and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7).</p>

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

<p>GSK2245035: selective nasal TLR7 agonist, boosts Type-1 IFN (pEC50: 9.3 IFNα, 6.5 TFNα), curbs Th2 cytokines in blood cultures.</p>

<p>PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-</p>

<p>Z-YVAD-CMK is an inhibitor of both caspase-1 and caspase-3, as referenced in [1].</p>

<p>Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures.</p>

<p>WEHI-345 analog is an Src inhibitor.</p>

<p>BET-IN-20 (compound 10), a BRD4 BD1 inhibitor (IC 50 =1.9 nM), exhibits significant anticancer properties. It promotes apoptosis in acute myeloid leukemia (AML) cells and arrests the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits both c-Myc and CDK6, and enhances PARP cleavage [1].</p>

<p>Thaspine: inhibits topoisomerase IB, reduces VEGF, stops endothelial cell growth via PI3K/MAPK pathways.</p>

<p>Calicheamicin (Calicheamicin γ1) is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.</p>

<p>Antitumor agent-97 (compound 42), an anticancer agent, effectively inhibits proliferation and autophagy in MGC 803 cells, induces apoptosis, and enhances ROS</p>

<p>Vatalanib hydrochloride (PTK787 hydrochloride) is a VEGF inhibitor that reduces the number and area of Aβ plaques in the cortex of 5xFAD mice.</p>

<p>RIP2 kinase inhibitor 2 is a receptor-interacting protein-2 kinase inhibitor.</p>

<p>p-Tolylmaleimide (p Tolylmaleimide) is an inhibitor of the water channel and binds to Aquaporin Z.</p>

<p>Nanatinostat (CHR-3996) is an HDAC inhibitor with selectivity and oral bioavailability, for HDAC1/2/3 .anti-proliferation apoptosis.</p>

<p>M3541: an oral ATM inhibitor with antitumor effects, hinders DNA repair and promotes cancer cell death.</p>

<p>Alrizomadlin is an orally active MDM2 inhibitor. APG-115 shows significant dose-dependent inhibitory effects on TP53wt AML cell lines.Cost-effective and quality-assured.</p>

<p>CDC801 is an inhibitor of PDE4 and TNF-α with IC50s of 1.1 μM and 2.5 μM, respectively.</p>

<p>PP5-IN-1 is a serine/threonine protein phosphatase-5 (PP5) inhibitor with potential anticancer activity that induces apoptosis in cancer cells.</p>

<p>MC4033 exhibits inhibitory concentration 50 (IC50) values of 39.4 µM in HCT116, 52.1 µM in H1299, 41 µM in A549, and 30.1 µM in U937 [1].</p>

<p>LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).</p>

<p>CDDO-2P-Im shows chemopreventive effect and reduces the size and severity of the lung tumors in the mouse lung cancer model.</p>

<p>ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar</p>

<p>CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.</p>

<p>AZA197 (AZA-197) is a selective Cdc42 inhibitor.</p>

<p>GP 1a: potent CB2 receptor agonist (EC50=7.1), 30x CB2 over CB1 preference, boosts P-ERK1/2, aids skin healing, anti-inflammatory.</p>

<p>RH01386, a small molecule, prevents ER stress in β cells, inhibits proapoptotic genes, and may treat type 2 diabetes by restoring insulin secretion.</p>

<p>NSC-697923 inhibits UBE2N, triggers p53-dependent and JNK-mediated apoptosis, blocks DNA damage and NF-κB signaling in neuroblastoma cells.</p>

<p>Elobixibat (A 3309) blocks IBAT in mice/humans/dogs (IC50: 0.13/0.53/5.8 nM); used for constipation research.</p>

<p>GCN2-IN-7 is an inhibitor of the environmental sensing protein GCN2 with antitumor activity for the study of melanoma.</p>

<p>CDDO-3P-Im is an orally active inhibitor of necroptosis with chemopreventive effects. CDDO-3P-Im can be used in studies about ischemia/reperfusion.</p>

<p>Ac-DEVD-CHO is a specific Caspase-3 inhibitor (Ki: 230 pM).Ac-DEVD-CHO has an inhibitory effect in SLNT-induced apoptosis.</p>

<p>KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP.KSQ-4279 has anticancer activity and is used in the study of non-small cell lung cancer, osteosarcoma,</p>

<p>VU0661013 is an effective and selective inhibitor of MCL-1.</p>

<p>JHU395, an oral prodrug of glutamine antagonist DON, shows stable antitumor effects on MPNST in vitro and vivo.</p>

<p>Tefinostat (CHR-2845) is a potent monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor.</p>

<p>DuP-697 is an irreversible, specific COX-2 inhibitor with IC50 values ​​of 10 nM and 800 nM for human COX-2 and COX-1.Cost-effective and quality-assured.</p>

<p>PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1 and TNKS2.PARP1/2/TNKS1/2-IN-1 has anti-tumor activity and induces apoptosis.</p>

<p>HM43239: oral FLT3 inhibitor; IC50: FLT3 WT 1.1nM, ITD 1.8nM, D835Y 1.0nM; blocks p-STAT5/p-ERK; affects SYK, JAK1/2, TAK1; halts leukemia cell growth.</p>

<p>Mcl-1 inhibitor22 (Example 36) is an MCL-1 inhibitor that suppresses its anti-apoptotic function by blocking the interaction between MCL-1 and pro-apoptotic proteins. It exhibits antiproliferative activity against various cancer cell lines and can be utilized for cancer research.</p>

<p>L-threo-Sphingosine C-18 is a protein kinase C inhibitor.</p>

<p>Top/HDAC-IN-3 (Compound 31) is a dual inhibitor of Topoisomerase and HDAC with oral activity. It induces DNA damage by elevating reactive oxygen species (ROS) levels, consequently inhibiting the clonal formation and migration of cancer cells, and triggering apoptosis (Apoptosis) and cell cycle arrest. Top/HDAC-IN-3 demonstrates a significant antitumor effect in NSCLC models, exhibiting a tumor growth inhibition (TGI = 77.5%, 100 mg/kg) superior to that of the HDAC inhibitor SAHA and the combination of SAHA with the topoisomerase inhibitor Irinotecan.</p>

<p>(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) sodium is a synthetic derivative of oleic acid (OA) that binds to the plasma membrane, altering lipid composition. This compound exhibits antitumor properties.</p>

<p>Antitumor agent-42 inhibits microtubule multimerisation and NO release, exhibiting anti-angiogenic, colony-forming and apoptosis-inducing effects.</p>

<p>CRI9 effectively inhibits the c-MET/PI3K/Akt/mTOR axis, suppressing the proliferation of hepatocellular carcinoma (HCC) cells. This compound exhibits potent cytotoxicity against HCC cells and induces apoptosis.</p>

<p>Oxamic acid is an inhibitor of LDH-A and exhibits antitumor activity. It demonstrates antiproliferative effects on cancer cells and can induce apoptosis.</p>

<p>Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.</p>

<p>PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).</p>

<p>SMO-IN-5 (Compound 25(B31)) is an effective inhibitor of smoothened (SMO), which suppresses the Hedgehog (Hh) signaling pathway. This compound inhibits cellular proliferation and induces apoptosis, demonstrating antitumor activity.</p>

<p>RET-IN-9 is a potent RET kinase inhibitor, potentially useful for studying RET-related diseases, including lung and thyroid cancer.</p>

<p>Samuraciclib (CT7001) is an oral CDK7 inhibitor with 41 nM IC50, notable for its high selectivity and potency against breast cancer cells.</p>

<p>EGFR/VEGFR2-IN-3 (compound 9) is an effective inhibitor of EGFR and VEGFR-2, demonstrating IC50 values of 0.129 µM for EGFR, 0.142 µM for VEGFR-2, and 3.428 µM for COX-2. This compound exhibits cytotoxic properties and induces cell apoptosis (apoptosis) as well as cell cycle arrest at the G2/M phase.</p>

<p>Ivaltinostat (CG-200745) is an oral panHDAC inhibitor, inducing apoptosis and enhancing cancer drug sensitivity.</p>

<p>Compound W10 is a dual inhibitor of Topo I (IC50: 0.90μM) and COX-2 (IC50: 2.31μM), inducing cancer cell apoptosis via mitochondria.</p>

<p>GI-Y2 is a GSDMD inhibitor that suppresses macrophage pyroptosis induced by oxidized low-density lipoprotein (ox-LDL). In vivo, GI-Y2 dose-dependently reduces atherosclerotic plaques and decreases lesion size and fibrosis in the aortic root of ApoE-/- mice. GI-Y2 holds potential for research in pyroptosis and cardiovascular diseases, such as atherosclerosis.</p>