Apoptose

<p>Antiproliferative agent-23: destabilizes microtubules, induces apoptosis in cancer cells via mitochondrial path, and triggers ER stress.</p>

<p>(R)-1-(2-((2-MeO-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(CF3O)benzyl)piperidine-3-carboxamide HCl is anti-apoptotic and anti-cancer.</p>

<p>HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), &gt;30-fold selectivity over other HDACs.</p>

<p>Boc-D-FMK is an irreversible, cell-permeable, and broad-spectrum caspase inhibitor and inhibits apoptosis stimulated by TNF-α (IC50: 39 μM).</p>

<p>Sotigalimab (APX 005) is a monoclonal antibody targeting CD40 with anticancer activity for the study of metastatic pancreatic cancer.</p>

<p>Potent PROTAC degrader for FLT3/CDK9, induces apoptosis, and shows promise for FLT3-ITD mutated AML research.</p>

<p>Caspase-3 inhibitor. Inhibits MG 132-induced small cell lung cancer cell death in vitro.</p>

<p>Chloranil (tetrachloro-p-benzoquinone) induces inflammation and neurological dysfunction and can be used to model inflammation in mice.</p>

<p>Dc-y13-27, a derivative of DC-Y13, is a potent YTHDF2 inhibitor (KD: 37.9 μM).</p>

<p>NSC90616 is a mutant p53 rescue compound [1] .</p>

<p>sEH inhibitor-19 (Compound (R)-14i) is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.2 nM. This compound suppresses the expression of TNF-α and IL-6 and exhibits anti-inflammatory effects in mouse models of acute pancreatitis and Carrageenan-induced edema.</p>

<p>AVJ16 as a member of the insulin growth factor 2 mRNA-binding protein family, binds to the mRNA of certain genes to regulate protein translation.</p>

<p>Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.</p>

<p>5α-dihydro Levonorgestrel is a metabolite of the synthetic progestin levonorgestrel .</p>

<p>Tralokinumab: human IgG4 monoclonal antibody, blocks IL-13, may treat atopic dermatitis.</p>

<p>2-Acetamidophenol (Orthocetamol) has analgesic and antipyretic effects. 2-Acetamidophenol is an isomer of Paracetamol (4-acetamidophenol).</p>

<p>Ianalumab (VAY-736) is a decarboxylated humanized antibody against BAFF-R.</p>

<p>Verdinexor (KPT-335) (KPT-335), a specific XPO1/CRM1 inhibitor, are orally bioavailable.</p>

<p>ERK-IN-6, a potent agent, inhibits ESCC growth and induces apoptosis through the ERK pathway.</p>

<p>Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.</p>

<p>HTR2A antagonist 1 (Compound 15f) is an HTR2A antagonist with an IC50 of 42.79 nM. It induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells by activating the p53/p21/caspase 3 signaling pathway. HTR2A antagonist 1 exhibits good liver microsomal stability and is useful for colorectal cancer research.</p>

<p>NQO2-IN-1, a resveratrol analog, is a potent NQO2 inhibito,antitumor,generation of ROS and up-regulation of DR5 (death receptor 5) to promote apoptosis.</p>

<p>Aspochalasin D, isolated from A. microcysticus, shows antibacterial properties and cytotoxicity affecting Ba/F3-V12 cells, with IC50s of 0.49 and 1.9 μg/ml.</p>

<p>Fludioxonil (CGA 173506), a phenylpyrrole fungicide, inhibits the growth of B. cinerea from strawberry and blackberry crops.</p>

<p>Apoptosis Inducer 29 (compound Y9) demonstrates anticancer efficacy in non-small cell lung cancer by inducing lysosomal dysfunction and apoptosis, and exhibits superior performance to Gboixn both in vitro and in vivo.</p>

<p>MEDI-7352 is a human bispecific antibody targeting NGF/bNGF and TNF. It can be utilized in research focused on osteoarthritis (OA) pain.</p>

<p>MRIA9 inhibits SIK1/2/3 &amp; PAK2/3 with IC50: SIK1 (516 nM), SIK2 (180 nM), SIK3 (127 nM); ATP-competitive.</p>

<p>This Bim peptide belongs to the pro-apoptotic group of the Bcl-2 family of proteins.</p>

<p>FGFR1/VEGFR2-IN-3 (Compound 8m) acts as a dual inhibitor of FGFR1 and VEGFR2. This compound exhibits both anti-cancer cell proliferation and anti-migration activities, and it also has the capability to induce cell apoptosis (apoptosis).</p>

<p>ROS inducer 5 (compound 6e) induces intracellular ROS accumulation and subsequent nuclear fragmentation. It can provoke apoptosis in MCF-7 cells with an IC50 of 3.85 μM. ROS inducer 5 is useful for cancer research applications.</p>

<p>PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.</p>

<p>EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.</p>

<p>Peginterferon beta-1a: first pegylated interferon for cancer, RMS research; induces tumor cell apoptosis.</p>

<p>Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.</p>

<p>PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.</p>

<p>Tibulizumab (LY 3090106) is a bispecific antibody for BAFF &amp; IL-17A; Kds: 60 &amp; 14 pM; for autoimmune research.</p>

<p>M24 inhibits Mcl-1 (Ki = 0.33μM), blocks HepG2 cell growth, and triggers apoptosis.</p>

<p>Cannflavin A, isolated from Cannabis sativa L., exhibits anti-cancer, neuroprotective, and anti-inflammatory activities by inhibiting Aβ1-42 aggregation and</p>

<p>KTX-582: potent IRAK4/Ikaros degrader (DC50=4/5nM), induces MYD88 MT DLBCL apoptosis &amp; tumor regression in lymphoma.</p>

<p>Thalidomide-5,6-Cl is a cereblon ligand derivative that recruits CRBN protein and forms PROTACs with a linker.</p>

<p>Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding &amp; osteoclastogenesis, induces PC12 cell apoptosis.</p>

<p>Carbonic anhydrase inhibitor33 (11D) is a dual inhibitor that targets both CA (carbonic anhydrase) IX/XII and CDK6. It exhibits Ki values of 19.7 nM for hCA IX and 26.1 nM for hCA XII. Additionally, Carbonic anhydrase inhibitor33 (11D) can induce G1 phase cell cycle arrest and apoptosis, making it relevant for research in non-small cell lung cancer (NSCLC).</p>

<p>CDK2-IN-45 is a CDK2 inhibitor with an IC50 value of 0.64 μM. It effectively inhibits the proliferation of DU-145 and PC-3 cell lines, with IC50 values of 2.20 μM and 4.17 μM, respectively. Additionally, CDK2-IN-45 induces G0/G1 phase cell cycle arrest and apoptosis. It is utilized in prostate cancer research.</p>

<p>Thalidomide-PEG conjugate for E3 ligase in PROTACs; has cereblon ligand and 3-unit PEG linker.</p>

<p>CPM-1285 induces apoptosis by effectively inhibiting the function of intracellular Bcl-2 and associated death antagonists.</p>

<p>FD2157, a photosensitive PI3K inhibitor, exhibits inhibitory IC50 values of 43 nM for PI3Kα, 83 nM for PI3Kβ, 84 nM for PI3Kγ, and 14 nM for PI3Kδ.</p>

<p>Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.</p>

<p>Pep19-2.5: Synthetic antitoxin peptide inhibits LP/LPS signals via PRRs, preventing inflammation and pyroptosis.</p>

<p>Boc-Asp(OBzl)-CMK, an inhibitor of IL-1 converting enzyme (ICE, caspase1), prevents the death of CHP100 neuroblastoma cells and inhibits IL-1β release induced by the viral coat protein [1].</p>

<p>Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].</p>

<p>4-Nitro-3-cresol exhibits ciliate toxicity against Tetrahymena pyriformis and is widely used in biochemical experiments and drug synthesis research.</p>

<p>Pacmilimab (CX-072) is a Probody immune checkpoint inhibitor targeting programmed death ligand 1 (PD-L1) with anti-tumor activity for the study of solid tumors.</p>

<p>Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.</p>

<p>Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.</p>

<p>Pantinin-1 is an antimicrobial peptide found in the venom of the emperor scorpion (Pandinus imperator). This compound exhibits strong antibacterial activity against Gram-positive bacteria and fungi, but has weaker effects on Gram-negative bacteria. Additionally, Pantinin-1 demonstrates very low hemolytic activity on human red blood cells and possesses anticancer properties, specifically inducing apoptosis in tumor cells.</p>

<p>Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.</p>

<p>A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle</p>

<p>F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.</p>

<p>Compound 106 (compound 10ic) induces apoptosis in B16-F10 melanoma cells and potently inhibits metastatic nodules in mouse models of lung metastatic melanoma,</p>

<p>Antitumor agent-112 (compound 3a) is a potent antitumor agent that induces apoptosis and exhibits cytotoxic activity on A549 cells, with an IC50 value of 91.35</p>

<p>Pyridinium bisretinoid A2E (A2E) TFA, a fluorophore derived from retinal pigment epithelium (RPE) lipofuscin, initiates blue-light-induced apoptosis, mediates</p>

<p>Apoptosis Inducer 11 (compound 3u) promotes apoptosis via the mitochondrial pathway and elicits a G2/M block alongside a marked reduction in the S phase within</p>

<p>Thalidomide-O-amido-C8-NH2 is a thalidomide-based ligand-linker for PROTAC synthesis.</p>

<p>WK369 is an innovative small molecule inhibitor of BCL6, demonstrating remarkable bioactivity against ovarian cancer by inducing cell cycle arrest and triggering apoptosis. It binds directly to the BCL6-BTB domain, obstructing the interaction between BCL6 and SMRT, which results in the reactivation of p53, ATR, and CDKN1A.</p>

<p>Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.</p>

<p>2'-Epi-2'-O-Acetylthevetin B (GHSC-74), a cardiac glycoside extractable from Cerbera manghas L.</p>

<p>OPBP-1 is a D-peptide developed through phage display screening, molecular docking, and molecular dynamics simulations. It exhibits high stability, strong antitumor activity, and oral bioavailability. OPBP-1 selectively binds to the PD-L1 protein, significantly blocking the interaction between PD-1 and PD-L1, which helps restore and enhance T lymphocyte function while reducing the proportion of myeloid-derived suppressor cells (MDSCs), counteracting tumor-induced immune evasion. OPBP-1 is applicable for research in cancer immunotherapy.</p>

<p>PROTACGPX4 degrader-2 (compound 18a) is a proteolysis-targeting chimera (PROTAC) that targets the degradation of glutathione peroxidase 4 (GPX4), with a DC50, 48h value of 1.68 μM. It induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. Additionally, PROTACGPX4 degrader-2 exhibits antiproliferative activity.</p>

<p>HDAC6-IN-28 (compound 10C) is a potent inhibitor of HDAC6 with an IC50 of 261 nM. It significantly induces apoptosis in B16-F10 cells and causes S phase arrest. Additionally, HDAC6-IN-28 effectively increases the expression of acetylated-α-tubulin both in vitro and in vivo.</p>

<p>Antitumor agent-170 (Compound C6) inhibits PD-1/PD-L1 interaction and PARP7 with IC50 values of 0.342 μM and 7.05 nM, respectively. It shows high affinity for human PD-L1, with a Ki of 9.31 nM, and can restore T cell function while increasing IFN-γ secretion. In mouse models, Antitumor agent-170 exhibits antitumor effects against melanoma and demonstrates favorable pharmacokinetic properties.</p>

<p>Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of an E3 ligase ligand and a linker, used in the synthesis of the Aster-APROTAC degrader.</p>

<p>Aphidicolin blocks DNA synthesis, hinders herpes virus growth, and stimulates apoptosis in leukemia cells; it's a mold-derived DNA polymerase inhibitor.</p>

<p>Stem bromelain: cysteine protease from pineapple stem with fibrinolytic, anti-inflammatory, antitumoral properties.</p>

<p>Ara-SH, a derivative of Cytarabine with a mercaptopropionic acid substitution, serves as the initiator for the self-assembly of a smart, co-loaded Cytarabine</p>

<p>Thalidomide-O-C8-Boc: CRBN ligand for PROTAC creation, derived from Thalidomide.</p>

<p>DJ4 induces a dose-dependent pro-apoptotic effect in the micromolar range.</p>

<p>N-Stearoyltyrosine (N-(1-Oxooctadecyl)-L-tyrosine) is an analog of Anandamide. It exhibits neuroprotective effects by safeguarding the CA1 region of the hippocampus in a gerbil ischemia-reperfusion model. Additionally, N-Stearoyltyrosine inhibits free radical generation, enhances antioxidant capacity, and reduces IR-induced apoptosis (cell apoptosis).</p>

<p>IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor, demonstrating an IC50 of 8.7 nM.</p>

<p>BCL-XL-IN-3 (Compound 11) is an inhibitor of BCL-XL, with a Ki of less than 0.01 nM. It suppresses cell viability in both normal Molt-4 cells and digitonin-permeabilized Molt-4 cells, with EC50 values of 77.8 nM and 0.07 nM, respectively. BCL-XL-IN-3 can be utilized as an ADC toxin for synthesizing Clezutoclax.</p>

<p>TV 3279 is a ChE-MAI inhibitor with neuroprotection via anti-apoptotic protein induction and blocks pro-apoptotic enzymes in cells.</p>

<p>(E/Z)-Squalene modulates ROS, triggers apoptosis/necrosis, reduces liver cholesterol and triglycerides.</p>

<p>SFI003 is a novel SRSF3 inhibitor that exerts anticancer activity against colorectal cancer by modulating the SRSF3 / DHCR24 / ROS axis and driving apoptosis in</p>

<p>Tubulysin B: a potent, cytotoxic microtubule-disrupting peptide from Archangium geophyra and Angiococcus disciformis.</p>

<p>Reveromycin A from Streptomyces sp. inhibits epidermal growth, tumors, and C. albicans; affects osteoclasts. IC50: 0.7-1.9 μg/ml; MIC: 2 μg/ml.</p>

<p>POV-PC is an oxidized phospholipid that inhibits VSMC growth under high serum conditions and induces cell apoptosis under low serum conditions.</p>

<p>KHKI-01215 is a NUAK2 inhibitor with anticancer activity, inhibiting the proliferation of SW480 cancer cells and inducing apoptosis.</p>

<p>SDU-071 is a BRD4-p53 inhibitor, suppressing MDA-MB-231 cell proliferation, inducing cell cycle arrest and apoptosis.</p>

<p>LY3415244 is a human bispecific antibody (bsAb) that targets B7-H1/PD-L1/CD274 and TIM-3/HAVCR2/CD366. This compound is applicable in the study of advanced solid tumors.</p>

<p>Ascochlorin, an isoprenoid antibiotic, inhibits STAT3 to combat tumors, induces apoptosis, and reduces inflammation.</p>

<p>PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.</p>

<p>2,5-Dimethylcyclohexa-2,5-diene-1,4-dione inhibits the viability of HL60 and K562 cells and exhibits antibacterial and anticancer properties.</p>

<p>RIP1-IN-1 is an orally bioavailable RIP1 inhibitor with a high binding affinity (Kd: 110 nM). This compound exhibits significant activity against necroptosis and effectively suppresses necrosome formation by inhibiting the phosphorylation of RIP1, RIP3, and MLKL pathways. RIP1-IN-1 can inhibit necroptosis and is applicable in research on acute liver injury.</p>

<p>AZD-4877: Potent Eg5 inhibitor, IC50 = 2 nM, alters mitosis, induces apoptosis, has antitumor effects.</p>

<p>PROTAC-O4I2, a PROTAC ligand targeting splicing factor 3B1 (SF3B1), induced FLAG-SF3B1 degradation in K562 cells with an IC50 value of 0.244 μM.</p>

<p>6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study</p>

<p>Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with anticancer properties.</p>

<p>RWJ-56110 dihydrochloride is a potent PAR-1 inhibitor (IC50=0.44μM), blocking platelet aggregation, angiogenesis, and induces apoptosis. No PAR-2/3/4 effect.</p>

<p>WEHI-3773 is an inhibitor of the interaction between VDAC2 and either BAK or BAX. It prevents BAX-mediated apoptosis (Apoptosis) by blocking the recruitment of BAX to the mitochondria through VDAC2. Conversely, WEHI-3773 promotes BAK-mediated apoptosis (Apoptosis) by limiting VDAC2's inhibitory sequestration of BAK. This compound shows promise for research in the field of cancer therapy.</p>

<p>PTD-p65-P1: a NF-kappaB inhibitor blocking activation from multiple inflammatory stimuli.</p>

<p>XZ739: Cereblon-based PROTAC, degrades BCL-XL (DC50 2.5 nM in MOLT-4, 16hr), induces caspase apoptosis.</p>