Apoptosis

<p>BAI1 hydrochloride is a selective inhibitor of the apoptosis factor BAX, functioning through an allosteric mechanism. By binding to BAX, it allosterically inhibits its activation, showcasing potential applications in the research of diseases mediated by BAX-dependent cell death [1].</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>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>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>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].</p>

<p>MC2590 is a histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.</p>

<p>BMS-561392 (DPC333) is a tumor necrosis factor-α ( TNF-α) Invertase inhibitor.</p>

<p>MAO-B-IN-26 (Compound IC9) serves as both a MAO-B and acetylcholinesterase inhibitor.</p>

<p>INU-152: pan-RAF inhibitor with potent anti-tumor effects on BRAFV600E cancers, inhibits MAPK in mutant cells, minimal side effects on RAS-mutant melanoma.</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>A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1].</p>

<p>Famitinib malate (SHR1020) is a potent oral kinase inhibitor targeting c-kit, VEGFR-2, and PDGFRβ, with IC50s 2.3, 4.7, 6.6 nM, useful for cancer research.</p>

<p>15-Deoxy-Δ12,14-Prostaglandin A1, a deoxyanalog of prostaglandins, inhibits NF-κB signaling and induces apoptosis. It also prevents TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecules (CAM) and reduces monocyte arrest [1].</p>

<p>CP-24879 HCl, a Δ5D/Δ6D dual-inhibitor, reduces liver lipid buildup and inflammation.</p>

<p>INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15.</p>

<p>Ezatiostat HCl (TLK199) inhibits glutathione S-transferase, GSTP1-1 specifically, and may treat cytopenias.</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>

Docebenone is a selective and orally active inhibitor of 5-LO.

<p>CDKI-83, a potent CDK9 inhibitor, inhibits tumor growth with GI50 &lt;1μM and triggers apoptosis in A2780 cells, showing promise as an anti-cancer agent.</p>

<p>LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.</p>

C 87: Small-molecule TNF-α inhibitor, binds TNFα, inhibits cytotoxicity with IC50 of 8.73 μM, blocks signaling.

<p>YM458 inhibits EZH2 (490 nM) and BRD4 (34 nM), curbing tumor cell growth and inducing apoptosis.</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>Rac-CCT-250863, a potent Nek2 inhibitor, exhibits selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A.</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>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>(S)-Sabutoclax ((S)-BI-97C1), an optically pure derivative of apogossypol, serves as a pan-active inhibitor of the antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. It effectively blocks the binding of BH3 peptides to key proteins in the family, including Bcl-XL, Bcl-2, Mcl-1, and Bfl-1, displaying inhibitory concentration (IC50) values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. Furthermore, (S)-Sabutoclax demonstrates potent efficacy in inhibiting the growth of various cancer cell lines, such as those from human prostate cancer, lung cancer, and lymphoma, with half-maximal effective concentration (EC50) values of 0.13, 0.56, and 0.049 μM, respectively. This compound is utilized in research focusing on apoptosis-based cancer therapies [1].</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>Cu(II)-Elesclomol is a complex formed by the anticancer agent Elesclomol and Cu(II), which has anticancer activity and can be used in the study of leukemia.</p>

<p>MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.</p>

<p>PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.</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>GGTI2417 blocks Geranylgeranyltransferase I, targeting RalB for apoptosis and RalA to stop growth.</p>

<p>FLT3-IN-14: FLT3 inhibitor; FLT3-WT IC50=5.6nM, FLT3-ITD IC50=1.4nM; blocks Y591 phosphorylation; G1 arrest; pro-apoptotic.</p>

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

<p>TL02-59: Fgr inhibitor (IC50=0.03nM), also targets Lyn (0.1nM), Hck (160nM), halts acute myelogenous leukemia growth.</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>Zn(BQTC) inhibits mtDNA and nDNA, damages mitochondria/nuclei, triggers apoptosis, and targets A549R cancer cells.</p>

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

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

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

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

<p>eIF4A3-IN-17, a silvestrol analogue, disrupts eIF4F assembly; EC50: 0.9-15 nM. Used in cancer pathogenesis research.</p>

<p>WEHI-345 analog is an Src inhibitor.</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>SAFit1 is an inhibitor of FK506 binding protein 51 (FKBP51)-specific (Ki: 4±0.3 nM).</p>

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

<p>iMAC2 hydrochloride, a potent inhibitor of the mitochondrial apoptosis-induced channel (MAC), demonstrates an IC50 of 28 nM and an LD50 of 15000 nM. It exhibits an anti-apoptotic effect by blocking the release of cytochrome c [1].</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>MY-673, a colchicine binding site inhibitor (CBSI), impedes tubulin polymerization and disrupts the ERK signaling pathway, consequently modulating SMAD4 protein</p>

<p>Lepadin H, a marine alkaloid and ferroptosis inducer, exhibits significant cytotoxicity by promoting p53 expression, escalating ROS production, and enhancing</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>HJC0152 (free base) is an orally active, potent STAT3 inhibitor that impedes cell cycle progression, induces apoptosis, and notably reduces MDA-MB-231 xenograft</p>

<p>BPR1J-340, a novel potent FLT3 inhibitor, shows anticancer promise, with IC50 ~25 nM and GC50 ~5 nM, causing apoptosis in AML cells.</p>

<p>SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.</p>

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

<p>FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer properties.</p>

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

<p>Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.</p>

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

<p>Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures.</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>c-Met-IN-10: potent kinase inhibitor (IC50=16 nM), halts cancer cell activity/movement, induces apoptosis, for anticancer research.</p>

<p>Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).</p>

<p>Bcl-2-IN-11 (compound 6) is a potent and selective inhibitor of Bcl-2 activity, exhibiting an IC50 of 0.9 nM, and demonstrates minimal inhibition against Bcl-xl</p>

<p>Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM).</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>M3541: an oral ATM inhibitor with antitumor effects, hinders DNA repair and promotes cancer cell death.</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>VU0661013 is an effective and selective inhibitor of MCL-1.</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>PP5-IN-1 is a serine/threonine protein phosphatase-5 (PP5) inhibitor with potential anticancer activity that induces apoptosis in cancer cells.</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>Nanatinostat (CHR-3996) is an HDAC inhibitor with selectivity and oral bioavailability, for HDAC1/2/3 .anti-proliferation apoptosis.</p>

<p>JHU395, an oral prodrug of glutamine antagonist DON, shows stable antitumor effects on MPNST in vitro and vivo.</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>Tefinostat (CHR-2845) is a potent monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor.</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>AZA197 (AZA-197) is a selective Cdc42 inhibitor.</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>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>GCN2-IN-7 is an inhibitor of the environmental sensing protein GCN2 with antitumor activity for the study of melanoma.</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>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>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>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>LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).</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>Elobixibat (A 3309) blocks IBAT in mice/humans/dogs (IC50: 0.13/0.53/5.8 nM); used for constipation research.</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>HDAC-IN-81 (Compound 11g) is an HDAC inhibitor capable of effectively inhibiting HDAC1 with an IC50 value of 4.5 nM. Additionally, it exhibits anticancer activity by inhibiting cell proliferation and can induce cell apoptosis (apoptosis).</p>

<p>GLI1-IN-1 (CBC-1), a GLI-1 inhibitor, exhibits superior water solubility and anticancer properties. It effectively induces apoptosis and inhibits colorectal cancer growth by targeting the Hedgehog (HH) pathway (IC 50 = 1.3 μM) [1].</p>

<p>Compound 2c is a potent p38α MAPK inhibitor with antitumor effects, enhancing apoptosis and ROS.</p>

<p>FAK-IN-4 (Compound 7d) has anticancer activities that can induce cell apoptosis. FAK-IN-4 is potential inhibitor of FAK [1].</p>

<p>CRT0066101 is a potent, orally active PKD inhibitor with IC 50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively [1]. Additionally, it inhibits PIM2 with an IC 50 of approximately 135.7 nM and demonstrates anticancer effects [2].</p>

<p>Compound 5f, a potent tubulin polymerization inhibitor (IC50 = 1.09 μM), blocks cell migration, tube formation, and has anti-angiogenic effects.</p>

<p>ST362, an anticancer agent, acts by disrupting DNA repair and halting growth in prostate, colon, lung and breast cancer cells.</p>

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