Apoptose

<p>hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.</p>

<p>Ferroptosis-IN-14 (compund 36) exhibits the most potent anti-ferroptotic activity with an EC50 value of 0.58 ± 0.02 μM, demonstrating excellent anti-ferroptotic efficacy, as well as stability in microsomes and plasma.</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>Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.</p>

<p>Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase.</p>

<p>KB03-SLF is a protease with the capability to target specific proteins and regulate intracellular protein levels by inducing protein degradation. This mechanism renders KB03-SLF potentially valuable in the suppression of related diseases.</p>

<p>SLF TFA, a synthetic FKBP ligand, binds FKBP51 (3.1 μM) and inhibits FKBP12 (IC50 2.6 μM); used in PROTAC synthesis.</p>

<p>Euphornin is a natural product that can be used as a reference standard. The CAS number of Euphornin is 80454-47-3.</p>

<p>GA-Mk is a triterpenoid from Ganoderma lucidum mycelia, inhibits HeLa cell growth, and induces apoptosis via mitochondria; used in cervical cancer studies.</p>

<p>YW-N-7 (TFA) is a PROTAC designed to target, inhibit, and degrade RET kinase, demonstrating a DC50 of 88 nM. It exhibits antitumor activity in xenograft mouse models driven by KIF5B-RET, making it a valuable compound for cancer research.</p>

<p>Poly (I:C):Kanamycin (1:1) is an equimolar mixture of Poly(I:C) and kanamycin. TLR3 agonist commonly used as a vaccine adjuvant; enhanced Poly(I:C) stability.</p>

<p>Rasfonin, a fungal metabolite from T. terrophilus, halts mouse splenocyte growth; IC50: 0.7 μg/ml (ConA), 0.5 μg/ml (LPS).</p>

<p>p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.</p>

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

<p>Anti-Mouse PD-L1 Antibody (10F.9G2) is an IgG-class antibody against mouse PD-L1.</p>

<p>A-1208746 is an inhibitor of MCL-1 with a Ki value of 0.454 nM. This compound effectively activates caspase-3/-7, induces apoptosis in H929 cells, and reduces mitochondrial membrane potential. Additionally, A-1208746 synergizes with Navitoclax, making it applicable in cancer research.</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>Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density</p>

<p>VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation.</p>

<p>Pomalidomide-PEG3-CO2H is a cereblon ligand-PEG3 linker for PROTACs.</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>Rosamultic acid is a useful organic compound for research related to life sciences and the catalog number is T125342.</p>

<p>BTK-IN-37 (compound 8d), a BTK inhibitor, demonstrates potent apoptotic effects on cancer cells by targeting BTK with K_i and IC_50 values of 5.07 nM and 3.6 nM, respectively. Additionally, this compound selectively promotes the enrichment of genes associated with necroptosis and pyroptosis.</p>

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

<p>Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].</p>

<p>"Urelumab (BMS-66513), a humanized IgG4 mAb CD137 agonist, boosts T-cell/NK cell-mediated cytotoxicity and anti-tumor activity."</p>

<p>Kusunokinin is a useful organic compound for research related to life sciences and the catalog number is T124612.</p>

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

<p>Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.</p>

<p>PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.</p>

<p>MD-222: a first-in-class, highly potent PROTAC that degrades MDM2, activates p53, and exhibits anticancer properties.</p>

<p>FAK-IN-25 (4c) is an inhibitor of FAK with an IC50 value of 50.98 nM. It induces apoptosis and causes cell cycle arrest in the G1 phase, making it relevant for cancer research.</p>

<p>CGP 3466B (Omigapil) is an oral drug inhibiting GAPDH nitrosylation and apoptosis, potentially treating Alzheimer's and CMD.</p>

<p>H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.</p>

<p>PAK4-IN-3 (compound 27e) is a PAK4 inhibitor exhibiting an IC50 of 10 nM and demonstrates antiproliferative effects on A549 cells with an IC50 of 0.61μM.</p>

<p>PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 77 nM. This compound can activate Jurkat T cells and effectively block the PD-1/PD-L1 immune checkpoint.</p>

<p>Antitumor agent-187 (compound I3), a photosensitizer derived from 5,15-diarylporphyrin, exhibits anticancer activity with a peak absorption wavelength of ~668 nm. This compound induces apoptosis and is applicable in photodynamic therapy (PDP). It selectively accumulates in tumor sites and possesses real-time fluorescence imaging capabilities.</p>

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

<p>Ac-VDVAD-CHO (TFA) is a caspase-2/3 inhibitor with IC50 values of 46 nM and 15 nM, respectively.</p>

<p>Betamethasone (NSC-39470), a glucocorticoid steroid, has immunosuppressive and anti-inflammatory properties.</p>

<p>GBM CSCs-IN-1 (Compound (−)-20), a rocaglate derivative, potently inhibits glioblastoma stem cells (GBM CSCs) and exhibits an EC50 of 45 nM by targeting the RNA helicase DDX3. Additionally, it induces apoptosis in these cells.</p>

<p>PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in</p>

<p>MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.</p>

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

<p>KRASG12C IN-16 (Compound SK-17) is a selective, covalent, and orally active KRASG12C inhibitor. It can induce apoptosis and effectively prevent the activation of the MAPK and PI3K/mTOR signaling pathways. Additionally, KRASG12C IN-16 exhibits antitumor activity against pancreatic cancer.</p>

<p>UBX1325, a potent Bcl-xL inhibitor, induces cell death in aging cells, useful for age-related eye disease research.</p>

<p>8-hydroxy Efavirenz, a main efavirenz metabolite by CYP2B6, causes apoptosis in rat neurons at 0.01 μM.</p>

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

<p>Compound 29c, a Thalidomide-linker conjugate for potent PROTAC BRD2/BRD4 degrader-1, targets BET proteins.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>GPX4-IN-14 (compound 2c) acts as a GPX4 inhibitor, exhibiting both free radical scavenging activity (with a maximum scavenging rate of 72.52%) and anti-tumor proliferation activity in vitro. This compound targets GPX4 protein, elevating lipid peroxide and intracellular Reactive Oxygen Species (ROS) levels, which induces ferroptosis and contributes to its anti-tumor proliferation effects.</p>

<p>Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist.</p>

<p>Flu-BakBH3 peptide, derived from Bak's BH3 domain, binds tightly to a crucial pocket of Bcl-XL, essential for its anti-death role.</p>

<p>Z-LEHD-FMK is a selective and potent caspase-9 inhibitor that protects against reperfusion injury and slows apoptosis.Z-LEHD-FMK exhibits antitumor and</p>

<p>PI3K/AKT-IN-4 (compound 3), a diterpenoid extracted from the roots and rhizomes of Salvia castanea Dielsf., exhibits antitumor properties by inhibiting cell viability and proliferation (IC 50 =4.72 μM) and promoting apoptosis in Hep3B cells. This compound obstructs the G0/G1 phase of the cell cycle, triggers mitochondrial dysfunction, and induces oxidative stress. Moreover, PI3K/AKT-IN-4 combats hepatocellular carcinoma through the inhibition of the PI3K-Akt signaling pathway and by interacting with PARP1 and CDK2 targets.</p>

<p>Prolgolimab (BCD-100) is an anti-PD-1 antibody used in melanoma research.</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>Boc-AEVD-CHO, a selective Caspase 8 inhibitor, facilitates apoptosis research and the investigation of immune and inflammatory diseases [1] [2].</p>

<p>IPH10 is an anticancer agent with strong antitumor effects in vivo and exhibits no liver or kidney toxicity. It significantly increases the reactive oxygen species (ROS) levels in tumor cells, decreases mitochondrial membrane potential, and induces apoptosis (apoptosis) in these cells.</p>

<p>MALT1-IN-13 (compound 10m) is an inhibitor of the mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1), forming a covalent and irreversible bond with the MALT1 protease, thereby inhibiting its activity with an IC50 of 1.7 μM. It suppresses the proliferation of ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1 cells. Additionally, MALT1-IN-13 regulates the mTOR and PI3K-Akt pathways.</p>

<p>RIPK2-IN-4 is a potent and specific inhibitor of RIPK2 with an IC50 value of 5 nM.</p>

<p>Thalidomide-NH-amido-C6-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, designed for the synthesis of PROTAC.</p>

<p>TOFA-Plasmalogen (compound 1), a derivative of glyceraldehyde, exhibits ferroptosis-inducing properties. This compound promotes lipid peroxidation in cell membranes, leading to cytotoxic effects with an inhibition concentration (IC 50 = 32.87 μM).</p>

<p>MTX-23, an AR-targeted Proteolysis Targeting Chimera (PROTAC), effectively degrades both AR-V7 and AR-FL, inhibiting the proliferation of CaP cells and inducing</p>

<p>Lw13 is a PROTAC targeting Hsp90, exhibiting maximal degradation efficacy at a concentration of 0.05 μM in Siha cells. Lw13 induces apoptosis and demonstrates potent antitumor activity both in vitro and in vivo.</p>

<p>Lincydomine relaxes smooth muscles, treats unstable angina, and opens human and guinea pig respiratory tracts.</p>

<p>EGFRkinase inhibitor 7 (compound 18i) is an EGFR inhibitor with an IC50 of 42.3 nM, exhibiting anticancer properties. This compound demonstrates significant in vitro cytotoxicity and capacity to induce apoptosis. Furthermore, EGFRkinase inhibitor 7 displays anti-proliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively.</p>

<p>Eucalyptol, a natural monoterpenoid and cyclic ether found in eucalyptus species, effectively controls excessive airway mucus secretion and asthma by inhibiting pro-inflammatory cytokines. It serves as an efficacious treatment for non-purulent sinusitis, reducing inflammation and pain when applied topically, and demonstrating leukemic cell-killing capabilities in vitro.</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>Thalidomide-NH-C8-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand and a specific linker.</p>

<p>Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic.</p>

Compound Ru2 (Antitumor photosensitizer-6) exhibits synergistic type I/II photosensitization and photocatalytic activities under illumination at 595 nm. It causes oxidative redox imbalance within cells, affecting biosynthesis and metabolic processes, leading to cell apoptosis (Apoptosis). Compound Ru2 is applicable in studies of photodynamic therapy (PDT).

<p>NCA029 is a potent activator of human caseinolytic protease P (HsClpP) with an EC50 of 0.15 μM. It targets HsClpPP and triggers an ATF3-dependent integrated stress response, resulting in the death of colon cancer cells.</p>

<p>Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium-labeled form of Oxybenzone. Commonly used as a UV filter in tanning and skin protection products, Oxybenzone (Benzophenone 3) acts as an endocrine-disrupting chemical (EDC) that can cross both the placental and blood-brain barriers. It impairs autophagy, alters epigenetic states, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.</p>

<p>Compound AuL9, also known as iNOS/TopoI-IN-1, is a multi-target hybrid molecule possessing anti-tumor, anti-inflammatory, and antioxidant properties. This compound effectively inhibits the growth of MCF-7 and MDA MB-231 breast cancer cells in vitro, exhibiting IC50 values of 3.5 μM and 6.3 μM respectively. It also prompts DNA damage and apoptosis in these cells by inhibiting human topoisomerase I (TopoI) with a K_i of 2.72 μM. Additionally, iNOS/TopoI-IN-1 reduces the expression of iNOS by suppressing the activation of NF-kB, with a K_i of 1.49 μM.</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>Furazolidone (Furoxone), a nitrofuran derivative, inhibits AML1-ETO transformed cells with IC50 value of 12.7 μM.</p>

<p>EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-cancer.</p>

<p>PZ703b hydrochloride, a Bcl-xl PROTAC, triggers apoptosis and halts cancer growth; used in bladder cancer studies.</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>TopoII/tubulin-IN-1 (Compound 1B8) is an inhibitor of TopoII/tubulin. It effectively suppresses the proliferation of tumor cells and reduces ROS levels, while inducing apoptosis and cell cycle arrest, without showing significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 exhibits antitumor activity.</p>

<p>EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.</p>

<p>Thalidomide-PEG2-NH2: synthetic E3 ligase ligand-linker, combines Thalidomide-based cereblon and PROTAC linker.</p>

<p>Anticanceragent 178 (compound C2) is a potent anticancer compound. It effectively inhibits the proliferation and metabolic activity of MDA-MB 231 cells, with IC50 values of 1.1 and 4.2 μM, respectively. Additionally, Anticanceragent 178 induces ferroptosis and necroptosis in cells.</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>PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis.</p>

<p>KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.</p>

<p>TrxR1-IN-2 (Compound 6a) acts as a TrxR1 inhibitor that covalently bonds with the Cys475 and Sec498 sites of TrxR1. This interaction hampers TrxR1 activity, resulting in a redox homeostasis disruption and inducing apoptosis and ferroptosis.</p>

<p>Anticanceragent 204 (Compound 6) is a fluorinated derivative of cinnamamides with anticancer activity. It can arrest the cell cycle of HepG2 cells in the G1 phase and induces apoptosis by reducing mitochondrial membrane polarization (MMP) levels.</p>

<p>ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax.</p>

<p>Thalidomide-O-amido-C8-NH2 hydrochloride, a synthetic cereblon ligand-linker for PROTAC synthesis.</p>

<p>EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2, with IC50 values of 2.7 and 3.0 μM, respectively. It can induce apoptosis and cause cell cycle arrest at various stages. This compound is applicable in cancer research.</p>

<p>pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.</p>

<p>Enniatin A1, a cyclic hexadepsipeptide from Fusarium, induces apoptosis and disrupts ERK, inhibiting ACAT (IC50: 49 μM).</p>

<p>Pidilizumab (CT-011), a humanized IgG1κ anti-PD-1 monoclonal antibody, serves as a DLL1 antagonist with potential applications in researching hematologic</p>

<p>Sasanlimab (PF-06801591), a humanized IgG4-κ antibody, selectively targets PD-1 and is primarily produced in Chinese Hamster Ovary (CHO) cells [1].</p>

<p>15-acetoxyscirpenol: ASM that induces apoptosis, inhibits Jurkat T cell growth dose-dependently, and activates caspases other than caspase-3.</p>

<p>TNF/IFNγ-IN-1 (TGA) is a TNF and IFN-γ inhibitor with antioxidant and anti-inflammatory activities for neurodegenerative diseases such as Alzheimer.</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>HDAC-IN-77 (HL-5s), an HDAC inhibitor, has the capability to induce ferroptosis and suppress the Nrf2/HO-1 signaling pathway. This compound is utilized in cancer research.</p>