Apoptose

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

<p>Apoptosisinducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer cells, demonstrating an IC50 of 12.8 μM and inducing early apoptosis in these cells. Additionally, it can bind to DNA molecules as well as Bax and Bcl-2 proteins, thereby inducing DNA damage.</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>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>Mcl-1 antagonist 1 is a Mcl-1 protein antagonist.</p>

<p>PRMT5-IN-31 (Compound 3m), a selective PRMT5 inhibitor (IC50: 0.31 μM), increases hnRNP E1 protein levels by occupying the substrate site of PRMT5 and</p>

<p>Oral nitroimidazole antibiotic; treats anaerobic infections; may cause inflammation and muscle contractions with long-term use.</p>

<p>cytoplasmic peptide of the neurotrophin receptor p75NTR</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>Nofazinlimab (CS1003) is a human anti-PD-1 IgG4 monoclonal antibody for the study of unresectable hepatocellular carcinoma (uHCC).</p>

<p>Antitumor agent-201 (Compound 10) is a Golgi apparatus-targeting chloride ion transport activator with an EC50 for promoting transmembrane chloride ion transport of 1.53 mol% and an IC50 against HepG2 cells of 7.13 μM. By selectively acting on the Golgi apparatus, Antitumor agent-201 disrupts chloride ion homeostasis, decreases the expression of key proteins such as GM130 and GRASP55, and alters Golgi structure and function. This process induces Golgi apparatus autophagy, triggers apoptosis in cancer cells, and causes cell cycle arrest at the G2/M phase, thereby exhibiting anticancer activity. Antitumor agent-201 is applicable for research in the field of cancer-related diseases.</p>

<p>anti-TNBC agent-1 targets TNBC effectively, with IC50 of 0.20-0.27 μM, inducing apoptosis and G1 arrest in SUM-159 cells.</p>

<p>12-Deoxyphorbol 13-palmitate, a monomer derived from the roots of Euphorbia fischeriana, exhibits notable antitumor activity. This compound induces cell cycle arrest and apoptosis in gastric cancer cells by modulating key cell cycle regulators, such as cyclin B, cyclin A, and CDC2. Additionally, 12-Deoxyphorbol 13-palmitate significantly diminishes liver fibrosis by targeting APOL2 and impairing the APOL2–SERCA2–PERK–HES1 signaling pathway.</p>

<p>Avotaciclib hydrochloride, a CDK1 inhibitor, is the hydrochloride salt of Avotaciclib and exhibits potential therapeutic use in specific malignancies, including</p>

<p>Phenamet is a bioactive chemical.</p>

<p>Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.</p>

<p>Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].</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>Prolgolimab (BCD-100) is an anti-PD-1 antibody used in melanoma research.</p>

<p>Thalidomide-NH-PEG2-COOH: a synthesized E3 ligase ligand-linker with cereblon ligand and PROTAC linker.</p>

<p>BMf-BH3 is a Bcl-2 family peptide, key in HDAC inhibition affecting acetylation balance.</p>

<p>Conjugated 18-C ω-6 fatty acid from Jacaranda seeds, induces cancer cell apoptosis via oxidative stress; metabolizes to cytotoxic CLA.</p>

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

<p>Camrelizumab (SHR-1210) is a human IgG4-κ monoclonal antibody with high affinity and directed against PD-1.Camrelizumab binds PD-1 with a binding affinity of up</p>

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

<p>JGB1741, a SIRT1 inhibitor (IC50=15µM), modulates apoptosis markers and p53 acetylation in breast cancer research.</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>DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.</p>

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

<p>TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα ( K D = 6.8 nM).</p>

<p>U7D-1: First-class USP7 PROTAC degrader, DC50 33 nM, anticancer, induces apoptosis in Jeko-1.</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>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>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>Ajoene from garlic has antibacterial, anticancer, antiplatelet, and antioxidant effects; it combats various bacteria, yeasts, and cancer cells.</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>FTO-IN-14 (Compound F97) is an inhibitor of the RNA demethylase Fat mass and obesity-associated protein (FTO), with an IC50 of 0.45 μM. It modulates the expression of the ASB2, RARA, and MYC proteins. FTO-IN-14 demonstrates antiproliferative activity in AML cancer cells, with IC50 values of 0.7-5.5 μM against MOLM13, NB4, HEL, OCI-AML3, MV4-11, and MONOMAC6, and induces apoptosis in NB4 cells. Additionally, FTO-IN-14 exhibits antitumor activity in a mouse NB4 xenograft model.</p>

<p>SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.</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>Amino-PEG6-Thalidomide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules.</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>PK095 is a proprietary compound in the guanidine - based F1F0-ATPase inhibitor family.</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>Chlopynostat (Compound 6c) is an HDAC1 inhibitor with an IC50 value of 67 nM. It induces apoptosis by inhibiting HDAC1, thereby reversing STAT4/p66Shc defects.</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>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>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>