Apoptose

<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>Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and</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>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>Platycoside G3 is a useful organic compound for research related to life sciences. The catalog number is T124100 and the CAS number is 849758-44-7.</p>

<p>Poly(I:C) potassium is a synthetic RNA analog, activates TLR3/RIG-I, used as a vaccine adjuvant, and induces apoptosis in cancer cells.</p>

<p>Ptd-p65-p1 Peptide TFA inhibits NF-kappaB, has a cell-penetrating antennapedia sequence, and selectively blocks NF-kappaB activation.</p>

<p>Tubulin Inhibitor 34 (compound b5), a potent anticancer agent, inhibits tubulin polymerization and induces G2/M arrest and apoptosis.</p>

<p>BM-962 (Compound 31) is a potent small-molecule inhibitor with an IC50 value of 4 nM (Ki=0.8 nM) for Bcl-2 and an IC50 of 3.9 nM (Ki&lt;1 nM) for Bcl-xL. It inhibits H1417 and H146 cell lines with IC50 values of 9 and 13 nM, respectively, and shows potential for use in cancer research.</p>

<p>PZ703b is a novel BCL-XL PROTAC degrader with enhanced BCL-2 inhibition.</p>

<p>PL120131 is a PD-1/PD-L1 inhibitory peptide that disrupts the interaction between PD-1 and PD-L1 by binding to PD-1. This compound can inhibit the apoptosis signaling pathway mediated by PD-1, thereby preventing apoptosis (apoptosis) in Jurkat cells and primary lymphocytes. Additionally, PL120131 supports cytotoxic T lymphocytes (CTL) in exhibiting antitumor activity.</p>

<p>RIPK3-IN-3 (compound 20) is a selective RIPK3 inhibitor that demonstrates potent activity with an IC50 value of 10 nM.</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>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>Sandacanol (Sandranol) is an olfactory receptor (OR10H1) agonist.Sandacanol induces cell cycle arrest and partial apoptosis in bladder cancer cells.</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>

<p>MSU-42011: oral RXR-like agonist, inhibits iNOS &amp; p-ERK, antitumor in lung cancer model, effective preclinical treatment.</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>NecroIr2, an iridium(III) compound, induces necroptosis in Cisplatin-resistant A549R lung cancer cells and disrupts mitochondria.</p>

<p>2-aminobenzo[d]thiazol-6-ol: antimicrobial, antioxidant, anticancer; may trigger cancer cell apoptosis.</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>Lesigercept is a humanized antibody that targets IGHE.</p>

<p>Peptide from c-Jun (33-57) blocks JNK binding, inhibits phosphorylation, upregulates p21, and induces HeLa cell apoptosis.</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>NCT-58 is a potent HSP90 inhibitor that blocks Akt, downregulates HER family, and induces apoptosis in HER2+ breast cancer without triggering HSR.</p>

<p>TD1092, a pan-IAP degrader, activates caspase 3/7, induces apoptosis in cancer cells, inhibits NF-κB, and is used in cancer research.</p>

<p>Oral nitroimidazole antibiotic; treats anaerobic infections; may cause inflammation and muscle contractions with long-term use.</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>AZT triphosphate TFA, a Zidovudine metabolite, inhibits HIV &amp; HBV replication and triggers mitochondrial apoptosis.</p>

<p>Mofarotene (Ro-40-8757) is a small molecule compound that shows considerable antitumor activity in many cancer cell lines and can be used for the treatment of</p>

<p>Mcl-1 Inhibitor 12 (Example 10), with a K i of 0.22 nM, functions as an MCL-1 inhibitor. It is utilized in cancer research [1].</p>

<p>Amino-PEG6-Thalidomide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules.</p>

<p>Ono 3403, a synthetic serine protease inhibitor, blocks TNF-alpha, NO production, and has antitumor properties.</p>

<p>SZUH280 is a potent, selective PROTAC (proteolysis targeting chimera) HDAC8 (histone deacetylase 8) degrader, demonstrating a DC50 of 0.58 μM in A549 cells.</p>

<p>Asunercept (APG101/CAN008) is a CD95-Fc protein targeting CD95L, used in GBM, MDS, and GvHD research.</p>

<p>Calcimycin hemimagnesium is an antibiotic, ionophore, and ATPase inhibitor that boosts intracellular Ca2+, causing cell death and apoptosis.</p>

<p>Thalidomide-NH-PEG4-COOH is a E3 ligase ligand-linker for synthesizing the selective degrader dCBP-1 targeting p300/CBP.</p>

<p>Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 ( PD-L1 ) [1] .</p>

<p>3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor.</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>HJC0416 hydrochloride: potent oral STAT3 inhibitor, better anticancer effects than Stattic, promising for breast cancer research.</p>

<p>FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.</p>

<p>BM-1197, a highly potent and specific dual inhibitor of Bcl-2 and Bcl-xL, effectively targets these proteins with IC50 values of 3.5 nM and 5.2 nM for Bcl-2 and</p>

<p>ReACp53 inhibits amyloid formation, restores p53 in cancer cells and HGSOC-derived organoids.</p>

<p>Oxythiamine (Hydroxythiamin) is a TK inhibitor that inhibits cancer cell proliferation, induces cell cycle arrest, and induces apoptosis.</p>

<p>PROTAC Bcl-xL degrader-1 targets Bcl-xL &amp; IAP E3 ligases, degrades Bcl-xL, toxic to human platelets &amp; MyLa 1929 (IC50: 62 nM, 8.5 μM).</p>

<p>VB-85247 is a STING agonist that, by activating the STING pathway, induces the upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as the maturation and activation of dendritic cells. It can lead to the regression of tumors within the bladder and is applicable in bladder cancer research.</p>

<p>Compound 5b (Anti-inflammatory agent 61) is a potent anti-inflammatory agent that diminishes TNF-α expression in LPS-induced inflammation within RAW 264.7 cells</p>

<p>PNT100: 24-base DNA oligo targeting BCL-2 regulatory region; halts tumor cell growth, induces death.</p>

<p>QN523 has drug-like traits, kills cancer cells in vitro, effective in vivo against pancreatic cancer, works via autophagy.</p>

<p>Chalcones A-N-5, a non-cytotoxic trihydroxy chalcone, aids cell growth &amp; neuroprotection, inhibits ferroptosis, and targets AD research.</p>

<p>Sanggenon G inhibits XIAP by binding its BIR3 domain; affinity is 34.26 μM, boosting caspase activation.</p>

<p>AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.</p>

<p>Onfekafusp alfa (L19TNF), a trimeric fusion of L19 scFv and human TNF, targets malignant glioma.</p>

<p>Izuralimab is a bispecific IgG1 antibody that targets both the inducible T-cell costimulator (ICOS/CD278) and PD-1 [1].</p>

<p>Pexelizumab is a humanized antibody targeting C5 to inhibit apoptosis and treat cerebral IR injury and myocardial infarction.</p>

<p>Thalidomide-O-amido-PEG2-C2-NH2, which combines an E3 ligase ligand with a linker, serves as an immunomodulator for cancer treatment.</p>

<p>P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).</p>

<p>MEK/PI3K-IN-2 is a potent dual inhibitor (MEK1 IC50: 352 nM, PI3Kα: 107 nM, PI3Kδ: 137 nM) that reduces pAKT, pERK1/2, and hinders tumor cell growth.</p>

<p>Thymidine 3',5'-diphosphate tetrasodium inhibits staphylococcal nuclease, SND1 &amp; tyrosyl nuclease; has anti-tumor properties &amp; catalyzes biochemical reactions.</p>

<p>PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis.</p>

<p>Galloflavin Potassium is an inhibitor of lactate dehydrogenase.</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>Apolizumab (Hu1D10) is a humanized antibody targeting HLA-DR beta-chain; induces apoptosis in CLL cells in vitro.</p>

<p>Antitumor agent-100 hydrochloride (compound A6), serving as both an apoptosis inducer and molecular glue, exhibits superior anti-tumor activity [1].</p>

<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

<p>MK-0731 inhibits kinesin spindle protein, disrupting mitosis and triggering apoptosis in KSP-overexpressing tumor cells.</p>

<p>Kurzipene D: anticancer, induces apoptosis, halts HepG2 at S phase, anti-tumor in zebrafish, inhibits tumor growth and spread.</p>

<p>PROTAC Bcl-xL ligand-1 serves as a ligand targeting Bcl-xL, essential in synthesizing PROTACs [1].</p>

<p>Thalidomide-based E3 ligase linker for PROTACs with a 3-unit PEG chain.</p>

<p>Thalidomide-NH-PEG3-COOH is a cereblon-based E3 ligase ligand-linker for PROTAC synthesis.</p>

<p>Anticancer agent 52 exhibits potent cytotoxicity, induces apoptosis, and has potential in bladder cancer research.</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>INF 195 is an inflammasome NLRP3 inhibitor that can be used to study myocardial ischemia and myocardial infarction.</p>

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

<p>NS3694 is an inhibitor of apoptosis and inhibits apoptosome formation and caspase activation.</p>

<p>α-Tubulin polymerization-IN-1 (Compound 8l) functions as an inhibitor of α-tubulin polymerization. This compound modulates the NRF2/KEAP-1 signaling pathway and induces ROS production in PC-3 cells, leading to apoptosis. It inhibits the proliferation of PC-3 cells with a GI50 of 0.17 µM, causing cell cycle arrest in the G2/M phase. Additionally, α-Tubulin polymerization-IN-1 demonstrates antitumor activity in mouse models.</p>

<p>NSC 295642: phosphatase inhibitor, boosts phospho-Erk in cells, aids cancer research.</p>

<p>PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal</p>

<p>H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.</p>

<p>Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.</p>

<p>ASR-488, an activator of the mRNA-binding protein CPEB1, promotes apoptosis and suppresses the growth of bladder cancer [1].</p>

<p>Zeluvalimab (AMG-404) is a monoclonal antibody designed to target the PD-1 receptor, and is utilized in cancer research [1].</p>

<p>Dehydrobruceine B, from Brucea javanica, enhances Cisplatin-induced apoptosis by affecting AIF, Bax, and Keap1-Nrf2.</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>Peptide is p53's amino acids 17-26, contacts Mdm-2 binding domain, also called p53N.</p>

<p>Mcl1-IN-12 has anti-tumor activity.It is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively.</p>

<p>DMUP inhibits CD47-SIRPα, induces apoptosis, boosts macrophage activity in A549 cells, and has antitumor properties.</p>

<p>R1-ICR-5 is a selective PROTAC degrader targeting serine/threonine-protein kinase 1 (RIPK1). Mediated by VHL, R1-ICR-5 promotes the degradation of RIPK1, disrupting the TNFR1 and TLR3/4 signaling hubs, enhancing NF-κB, MAPK, and IFN signal output, and facilitating RIPK3 activation and necroptosis induction. R1-ICR-5 holds potential for research in cancer and inflammatory diseases.</p>

<p>SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.</p>

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

<p>Odoroside A, from Nerium oleander leaves, induces cancer cell death via ROS/p53, causing apoptosis and cell cycle arrest.</p>

<p>Tripchlorolide is a useful organic compound for research related to life sciences and the catalog number is T126047.</p>

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

<p>RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.</p>

<p>DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.</p>

<p>Lorigerlimab (MGD019) is a bispecific IgG4 DART that blocks PD-1/CTLA-4, enhancing T-cells for mCRPC research.</p>

<p>SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and</p>

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

<p>Tetrathiomolybdate (TM) promotes the dimerization of the metal-binding domain (WLN4) of the cellular copper efflux protein ATP7B through its characteristic</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>Cytostatin: Natural antitumor, inhibits cell adhesion, blocks B16 melanoma, induces apoptosis, selectively targets PP2A (IC50 = 29 nM).</p>

<p>Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific</p>