Apoptose

<p>Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.</p>

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

<p>Pralnacasan blocks IL-18, IL-1β, IFN-γ. It’s a potent oral enzyme inhibitor with use in arthritis therapy (Ki: 1.4 nM).</p>

<p>Multi-kinase-IN-4 (compound 5d) is a multi-targeted kinase inhibitor active against VEGFR2, EGFR, HER2, and CDK2, with respective IC50 values of 0.33, 0.22, 0.</p>

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

<p>MPT0B014 is a potent tubulin polymerization inhibitor. MPT0B014 can induce cancer cell apoptosis.</p>

<p>Thalidomide-Piperazine-PEG2-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand with a PEG2 linker.</p>

<p>Baceridin, a cyclic hexapeptide and proteasome inhibitor, can be isolated from the culture medium of Epiphytic Bacillus.</p>

<p>Calphostin C is a protein kinase C inhibitor.</p>

<p>Ac-LEHD-AMC, a fluorogenic caspase-9 substrate, releases fluorescent AMC upon cleavage, aiding caspase-9 activity measurement.</p>

<p>Anti-MousePD-1(LALA-PG) Antibody (RMP1-14) is an IgG2a, κ antibody inhibitor derived from mice that targets and inhibits mouse PD-1.</p>

<p>The compound is a negative control peptide for the Bax inhibitor peptides V5 and P5.</p>

<p>Antiangiogenic agent 6 (Pt-1) effectively inhibits angiogenesis and induces necroptosis in tumor cells.</p>

<p>Sodium valproate is an anti-epileptic, boosting brain GABA levels and possibly affecting potassium channels for membrane stability.</p>

<p>PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker</p>

<p>PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.</p>

<p>TQB-2858 is a bifunctional fusion protein composed of an anti-PD-L1 monoclonal antibody fused with the extracellular domain of the TGF-β receptor. It exhibits high affinity for PD-L1, TGF-β1, and TGF-β3, and demonstrates a high target occupancy rate for PD-L1. TQB-2858 can be used in research on osteosarcoma and alveolar soft part sarcoma (ASPS).</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>Ajoene from garlic has antibacterial, anticancer, antiplatelet, and antioxidant effects; it combats various bacteria, yeasts, and cancer cells.</p>

<p>DiPT-4, a dual TOP1/PARP1 inhibitor, effectively induces DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells, with potential to</p>

<p>Necroptosis-IN-3 (Cyclohexanecarboxamide, N-(2-thienylmethyl)-) (Compound 69) is a Necroptosis inhibitor that inhibits TNF-α induced necroptosis.</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>A-1155905 is an MCL-1 inhibitor with anticancer activity, demonstrating a half maximal inhibitory concentration (IC50) of 33.5 Nm and a dissociation constant (Ki) of 0.58 nM. This compound selectively binds to MCL-1 and possesses sufficient affinity to disrupt the MCL-1-Bim complex in live cells. The induction of death in MCL-1-dependent cell lines by A-1155905 is reliant on caspase proteins and occurs through apoptosis.</p>

<p>Zalypsis, a transcription factor inhibitor, is used potentially for the treatment of lymphoma, and cervical carcinoma.</p>

<p>NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1/CDK1 levels, leading to G2/M cell cycle arrest and initiating apoptosis through caspase-9/caspase-3 cleavage.</p>

<p>MAO-B-IN-30 is a selective and potent MAO-B inhibitor that crosses the blood-brain barrier with antiproliferative activity and inhibits both MAO-A and MAO-B.MAO-B-IN-30 reduces the levels of TNF-alpha, IL-6, and NF-kB in organisms, and can be used to study Parkinson's-type neurological disorders.</p>

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

<p>Thalidomide-O-C7-acid: A cereblon ligand from Thalidomide linked via a PROTAC-used linker.</p>

<p>PH14, a dual PI3K/HDAC inhibitor, demonstrates potent inhibition with IC50 values of 20.3 nM for PI3Kα and 24.5 nM for HDAC3.</p>

<p>PB28: A potent σ2 agonist (Ki 0.68 nM), σ1 antagonist (Ki 0.38 nM), with anti-tumor properties and inhibits SARS-CoV-2 interactions.</p>

<p>DAPK Substrate Peptide is a synthetic peptide substrate for death-associated protein kinase (DAPK) (Km = 9 μM).</p>

<p>PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]</p>

<p>c-Met-IN-24 (compound 3g) serves as a dual-target inhibitor for STAT-3 (=4.7 μM) and c-MET (=12.67 μM), exhibiting anticancer properties. It arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells, making it applicable in the research of central nervous system cancers.</p>

<p>Citreoviridin from Penicillium citreoviride blocks brain Na+/K+-ATPase; boosts Na+/K+- and Mg2+-ATPase in microsomes dose-dependently.</p>

<p>Toremifene citrate is a selective estrogen receptor modulator (SERM). It is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on the mammary and uterine tissue.</p>

<p>AZD1152 is a pro-drug of Barasertib (AZD1152)-hQPA. Which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.</p>

<p>TNF-α-IN-9 is an NDM-1 inhibitor-3 analog and is a TNF-α inhibitor.TNF-α-IN-9 shows low inhibitory activity.</p>

<p>YN14-H is a PROTAC degrader that targets KRASG12C. It effectively inhibits the growth of NCI-H358 and MIA PaCa-2 cells, with IC50 values of 0.042 μM and 0.021 μM, respectively, and DC50 values of 28.9 nM and 18.1 nM. YN14-H significantly induces apoptosis and suppresses cell migration. It demonstrates favorable pharmacokinetics and excellent in vivo antitumor activity.</p>

<p>Ranevetmab (NV-01), a caninized anti-NGF mAb, relieves pain in DJD research.</p>

<p>Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.</p>

<p>Isoharringtonine, an alkaloid from Cephalotaxus koreana, inhibits and induces apoptosis in cancer cells.</p>

<p>(+)-Mcl-1 inhibitor 22 (Example 37) is an MCL-1 inhibitor that impedes the anti-apoptotic function of MCL-1 by blocking its interaction with pro-apoptotic proteins. It demonstrates antiproliferative activity against various cancer cell lines and is applicable for cancer research.</p>

<p>Apoptosisinducer 33 (compound H2) is a hydrazone derivative. It exhibits antioxidant and antimicrobial properties, capable of inhibiting the growth of Staphylococcus aureus, Escherichia coli, and Candida albicans. Additionally, Apoptosisinducer 33 can suppress tumor cell proliferation and induce apoptosis (apoptosis), making it useful for tumor research.</p>

<p>JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations.</p>

<p>PROTAC EGFR degrader 5 effectively breaks down EGFR Del19 in HCC827 cells at 34.8 nM, inducing apoptosis and G1 arrest.</p>

<p>Alkyl phosphates like (E)-C-HDMAPP activate γδ-T cells, resist hydrolysis, and boost TNF-α synthesis and γδ-T cell count in vivo.</p>

<p>RET-IN-26 (compound D5) is a kinase inhibitor that selectively targets the RET protein with an IC50 value of 0.33 μM [1].</p>

<p>Pamlectabart is a humanised antibody targeting TNFRSF17/BCMA, (ADC) Pamlectabart tismanitin multiple myeloma.</p>

<p>Bcl-2-IN-2 is a highly potent and selective inhibitor targeting Bcl-2 and Bcl-xL.</p>

<p>EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.</p>