Apoptosis

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

<p>Echitamine chloride, an alkaloid in Alstonia scholaris, has anti-cancer properties and inhibits pancreatic lipase (IC50: 10.92 µM).</p>

<p>Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft), a monopegylated interferon-alpha (IFN-α), is utilized in the study of myeloproliferative neoplasms [1].</p>

<p>Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1 [1] .</p>

<p>Inuviscolide induces apoptosis, G2/M arrest in melanoma, and has anti-cancer, anti-inflammatory effects.</p>

<p>7,3′,5′-Trihydroxyflavanone, a flavanoid derivative, promotes apoptotic cell death in MCF-7 cells by augmenting Bax expression.</p>

<p>AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity.</p>

<p>Tengonermin (ARENEGYR), a vascular agent, is TNF-α fused with CNGRCG peptide, enhancing chemo and T-cell access in tumors.</p>

<p>HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4</p>

<p>Compound (Ra)-10, also known as Mcl-1 inhibitor 14, is a potent inhibitor of myeloid cell leukemia-1 (MCL-1), exhibiting a K_i of 0.018 nM, and holds potential</p>

<p>Ac-LEVD-CHO, a caspase-4 inhibitor, is a peptide with the sequence Ac-Leu-Glu-Val-Asp-al [1].</p>

<p>Taxamairin B is a potent anti-inflammatory compound that inhibits the expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and reduces the</p>

<p>APG-1387 inhibits IAPs, degrades cIAP1/2, XIAP, boosts chemosensitivity, and induces apoptosis in NPC.</p>

<p>G-Glu-Val (γ-glutamyl-L-valine, H-Glu-Val -OH), a flavour-regulating dipeptide, is a major contributor to "mellow".</p>

<p>p38-α MAPK-IN-8 (Compound 13) is a lipophilic cationic derivative. It exhibits cytotoxicity toward various tumor cells, inducing cell cycle arrest and apoptosis, as well as increasing reactive oxygen species (ROS) production and causing mitochondrial membrane potential depolarization. Its antitumor activity may be related to the p38α MAPK pathway, making it a potential candidate for cancer research.</p>

<p>SB-1295, an orally active CDK9/T1 inhibitor with an IC50 of 0.17 μM, exhibits antiproliferative effects on HCT 116 and MIA PaCa-2 cells.</p>

<p>SH-5, an AKT inhibitor potentiates apoptosis and inhibits invasion through the suppression of anti-apoptotic, proliferative and metastatic gene products</p>

<p>Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with 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>Suramin is an RdRp and PTPase inhibitor with anti-parasitic, anti-tumor, and anti-angiogenic activities, inhibiting sirtuins and DNA topoisomerase II.</p>

<p>SP3N hydrochloride is a specific degrader of the prolyl isomerase (FKBP12). Its alkylamine moiety is metabolized into an active aldehyde (SP3CHO), which recruits the SCFFBXO22 ligase for the degradation of FKBP12. SP3N hydrochloride is applicable in cancer research.</p>

<p>AXL/Angiokinase-IN-1 (compound 11b) is an inhibitor of AXL/triple angiokinase, with an IC50 of 3.75 nM for AXL expression. This compound suppresses epithelial-mesenchymal transition (EMT) in Bxpc-3 cells and prevents metastasis in lung cancer cells. Additionally, AXL/Angiokinase-IN-1 impairs the functions of vascular and fibroblast cells and induces apoptosis in both cancer and fibroblast cells. It is characterized by low toxicity and favorable metabolic stability.</p>

<p>Psalmotoxin 1 is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker.</p>

Targaprimir-96 TFA is a selective inhibitor of miR-96 in cancer, inducing apoptosis with high affinity for pri-miR-96 but not affecting healthy cells.

<p>Ferroptosis-IN-17 (Compound 18) is an inhibitor of ferroptosis with an EC50 value of 0.57 μM. It effectively reduces the accumulation of intracellular ferrous ions and lipid peroxidation while restoring levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). In rat plasma, Ferroptosis-IN-17 demonstrates good solubility and notable metabolic stability. This compound holds potential for research in tumor suppression, neurodegenerative diseases, and cardiovascular disorders.</p>

<p>Mumefural, from Prunus mume fruit, hinders platelets, has anti-thrombotic properties, and boosts cognition.</p>

<p>Nemorosone, a PPAP from C. rosea, inhibits neuroblastoma and pancreatic cancer cell growth, induces apoptosis, and reduces mouse xenograft tumors.</p>

<p>Eriosematin has anti-proliferative and apoptosis-inducing properties and is a compound extracted from the root of Flemingia philippinensis in the Philippines.</p>

<p>AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG</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>DJ4 induces a dose-dependent pro-apoptotic effect in the micromolar range.</p>

<p>Lacto-N-fucopentaose I is a milk oligosaccharide.</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

<p>Apoptosis Inducer 13 (Compound Ru4) promotes apoptosis in cancer cells while also suppressing their migration and invasion.</p>

<p>PD-L1/LpxC-IN-1 (Compound 12b) is an inhibitor of PD-L1 and LpxC, with IC50 values of 5.2 μM and 0.081 μM, respectively. This compound disrupts bacterial lipopolysaccharide biosynthesis, leading to bacterial cell lysis and death. It effectively inhibits Gram-negative bacteria, exhibiting a minimum inhibitory concentration (MIC) of 0.25-0.5 μg/mL against K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028, and P. aeruginosa ATCC 9027. Additionally, PD-L1/LpxC-IN-1 modulates the immune response by downregulating the expression of inflammatory cytokines IL-2 and IFN-γ, and upregulating CD4+ and CD8+ cells, thus activating the immune system and mitigating excessive inflammatory responses. In a mouse model of K. pneumoniae ATCC 13883 infection, PD-L1/LpxC-IN-1 demonstrated antibacterial activity.</p>

<p>FeTPPS, a decomposition catalyst for 5,10,15,20-tetrakis(4-sulfonatophenyl) porphyrin iron(III) chloride peroxynitrite, neuroprotective.</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>RD-23 is an orally active and selective RET PROTAC degrader. It facilitates the ubiquitination and degradation of the RETG810C mutant with a DC50 value of 11.7 nM. Additionally, RD-23 inhibits the activation of downstream Shc signaling and induces apoptosis (Apoptosis). It is useful for studying RET-related cancers.</p>

<p>DCZ3301 is a novel aryl-guanidino inhibitor.</p>

<p>Apoptosis inducer37 (Derivative 10) is an agent that induces apoptosis and exhibits anticancer properties by causing cell cycle arrest at the S-G2/M phase and promoting cell apoptosis. It significantly inhibits HCT116, SKOV3, and HepG2 cancer cells with IC50 values of 24.98 μM, 26.15 μM, and 23.09 μM, respectively. Apoptosis inducer37 demonstrates antitumor activity and can be utilized in ovarian cancer research.</p>

<p>ZC0109 inhibits IDO1 (50 nM) &amp; TrxR1 (3.0 μM), induces ROS, arrests G1/S phase, causing cancer cell apoptosis.</p>

<p>VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 of 0.509 µM and an IC50 value of 7.48 μM for inhibiting MCF-7 cell proliferation. Its anticancer activity is exerted through cell cycle arrest, induction of apoptosis (Apoptosis), and modulation of gene expression, making it suitable for breast cancer research.</p>

<p>CRP protein and its fragment (174-185, RS-83277) boost human monocyte and macrophage cancer-killing effects in vitro.</p>

<p>Thalidomide-O-amido-PEG4-propargyl is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].</p>

<p>Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2/M cell cycle arrest and apoptosis.</p>

<p>CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC</p>

<p>BRD4 Inhibitor-39 (compound 12m) is an orally active inhibitor of BRD4 with an IC50 of 0.02 μM. It can induce apoptosis and demonstrates antitumor activity.</p>

<p>Distamycin A (NSC-82150), oligopeptide antibiotic, binds A/T rich DNA, affects cleavage sites, enhances apoptosis.</p>

U7D-1: First-class USP7 PROTAC degrader, DC50 33 nM, anticancer, induces apoptosis in Jeko-1.

VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.

<p>Antitumor Agent-116 (Compound 6C) is an anti-tumor agent that exhibits anti-proliferative properties and induces apoptosis.</p>

<p>Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthetic conjugate compound that combines a Thalidomide-based cereblon ligand and a linker, which is commonly</p>

<p>SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells.</p>

<p>BCL6-IN-10 (Compound WK499) is an inhibitor of BCL6, disrupting its interaction with the SMRT protein and promoting apoptosis, cell cycle arrest, and DNA damage</p>

<p>4-oxo-27-TBDMS Withaferin A, a withaferin A derivative, is an anticancer agent cytotoxic to A2780, not A2780/CP70.</p>

<p>Cell-permeable CaM agonist; activates phosphodiesterase, binds to Ca2+ channels, inhibits cytotoxicity (IC50=52μM), protects cells, reduces inflammation.</p>

Thalidomide-O-amido-PEG4-azide is a polyethylene glycol (PEG) derivative serving as a linker for Proteolysis Targeting Chimeras (PROTACs) synthesis [1].

<p>p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.</p>

Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding & osteoclastogenesis, induces PC12 cell apoptosis.

<p>CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor.</p>

<p>Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. It effectively blocks estrogen production and inhibits the proliferation of breast cancer cell lines such as MCF-7, arresting the cell cycle in the G1 phase and inducing apoptosis. Aromatase-IN-5 shows promise for breast cancer research.</p>

<p>VEGFR-2-IN-36 (compound 15) serves as a potent VEGFR-2 inhibitor, exhibiting an IC50 value of 0.067 μM, and acts as an apoptosis inducer with demonstrated</p>

Thalidomide-O-PEG4-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

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

<p>Topo I/II-IN-2 (Compound 3g) is an inhibitor of both Topo I and Topo II. It exhibits inhibitory activity against NCI-H446 and NCI-H1048 cells with IC50 values of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial apoptosis, disrupts mitochondrial function, and stimulates activity generation. Additionally, it inhibits the PI3K/Akt/mTOR pathway, effectively preventing the proliferation, invasion, and migration of small cell lung cancer (SCLC) cells in vitro.</p>

<p>PKM2 modulator 1 (compound C998) is an effective PKM2 inhibitor with antiproliferative activity. It induces apoptosis and holds potential for research in glioblastoma studies.</p>

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.

<p>Thalidomide-PEG3-NH2: a cereblon-based E3 ligase ligand-linker for PROTAC tech.</p>

<p>TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with</p>

FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits

<p>Hydrocinchonine is an Alkaloid from Olea europaea and is found in fruits.</p>

<p>EM 163是一种 TIR-TIR 相互作用抑制剂，它是MyD88蛋白的TIR（Toll/白细胞介素-1受体）结构域拟态。EM 163针对IL-1受体中的TIR 结构域，阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B（SEB）引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中，EM 163阻断p38的激活和IL-1β对化学诱导的长期电位（LTP）引发的蛋白质合成的抑制作用。</p>

<p>IRF1-IN-2 is a small molecule IRF1 inhibitor that suppresses pyroptosis, protecting against radiation-induced skin damage.</p>

<p>KRN 5500, a derivative of the nucleoside antibiotic spicamycin, has a wide range of antitumor activity against human cancer cell lines.</p>

<p>GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM.</p>

<p>ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.</p>

<p>Emfizatamab (GNC-038) is a tetravalent antibody that activates CD3 and 4-1BB on T cells while targeting CD19 or PD-L1 on tumor cells, resulting in T-cell-mediated cytotoxicity against human leukemia and lymphoma cells.</p>

<p>EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.</p>

<p>5-Fluorouracil-13C,15N2 is a standard for quantifying 5-fluorouracil via GC/LC-MS and blocks DNA synthesis, causing cell apoptosis.</p>

<p>Dapirolizumab is an anti-CD40 monoclonal antibody used in research on systemic lupus erythematosus (SLE) and other autoimmune diseases.</p>

<p>Top1-IN-2 (Compound 1a) is an inhibitor of topoisomerase 1 (Top1). It suppresses the growth of P-gp drug-resistant tumor cells and induces apoptosis.</p>

<p>Thrombospondin-1 (1016-1023) (human, bovine, mouse) is part of Thrombospondin-1 (TSP-1), a peptide with CD47 agonism.</p>

<p>2-aminobenzo[d]thiazol-6-ol: antimicrobial, antioxidant, anticancer; may trigger cancer cell apoptosis.</p>

<p>ADPM06: nonporphyrin PDT agent; leads in apoptosis, strong IC50 in µM against human tumors.</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>FG-3019 (Pamrevlumab), a human antibody, targets CTGF, potentially treating idiopathic pulmonary fibrosis.</p>

<p>Secalonic acid D, from Aspergillus aculeatus, is anti-tumor, activates GSK3-β, degrades β-catenin, inhibits c-Myc, and induces apoptosis.</p>

<p>Thalidomide-based E3 ligase ligand-linker for PROTAC, with cereblon ligand and C8-NH2 hydrochloride.</p>

<p>SDH-IN-26 (Compound C3) is a succinate dehydrogenase (SDH) inhibitor with significant inhibitory activity against various plant pathogenic fungi, including solanrhizoctonia and Botrytis cinerea. It exhibits an EC50 value of 0.270 μg/mL against solanrhizoctonia. SDH-IN-26 compromises fungal cell membrane integrity, increases membrane permeability, disrupts cell structure, reduces mitochondrial count, and affects normal hyphal growth. It also decreases mitochondrial membrane potential, inducing apoptosis. SDH-IN-26 holds potential for studying plant diseases caused by fungi.</p>

<p>RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.</p>

<p>"(±)-Enterodiol, the racemate of Enterodiol, is metabolized from lignans found in whole-grain cereals, nuts, legumes, flaxseed, and vegetables by human intestinal bacteria. This compound exhibits apoptotic effects in colorectal cancer (CRC) cells and has been identified to possess anti-cancer activities [1] [2]."</p>

<p>Cholesteryl Hemisuccinate Tris Salt is a cholesteryl ester with anticancer activity.Cholesteryl hemisuccinate has antitumor activity and inhibits tumor growth.</p>

<p>CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target inhibitor of CYP51/PD-L1, displaying IC50 values of 0.17 and 0.021 μM, respectively.</p>

<p>IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.</p>

<p>NecroIr2, an iridium(III) compound, induces necroptosis in Cisplatin-resistant A549R lung cancer cells and disrupts mitochondria.</p>

<p>PEAQX tetrasodium hydrate: potent/selective oral NMDA antagonist, IC50 270 nM (1A/2A), 29600 nM (1A/2B).</p>

<p>PD-1-IN-20 is the less active enantiomer of PD-1-IN-1.</p>

<p>Anticancer Agent 153 (Compound 3) promotes apoptosis through the generation of Reactive Oxygen Species (ROS) and elevates the loss of Mitochondrial Membrane</p>

<p>Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.</p>

<p>Compound Rh1 (Anticancer agent 132) acts as an inducer of apoptosis and autophagy, exhibiting both antitumor and antimetastatic activities.</p>