Apoptosi

<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>CWI1-2 is a potent IGF2BP2 inhibitor that inhibits its interaction with M6A-modified target transcripts by binding IGF2BP2.</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>RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.</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>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>CBI1 is a covalent BAX inhibitor. It selectively derivatizes BAX at C126 and inhibits BAX activation by triggering a ligand or through point mutations. CBI1 prevents the lipidation and oligomerization of BAX by t-2-hex. It also inhibits BAX activation induced by BH3 ligands, F116A mutation, or t-2-hex.</p>

<p>PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.</p>

<p>β-Apopicropodophyllin, a natural product isolated from Hyptis wticillata, promotes apoptosis through mechanisms including microtubule disruption, DNA damage,</p>

<p>Antitumor agent-150 (V10) is a breast cancer treatment that functions as a PROTAC degrader of MDM2.</p>

<p>N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP</p>

<p>C-Peptide 1 (rat) is a polypeptide isolated from proinsulin. C-Peptide acts as a β-catenin/GSK-3β activator, influences Na/K-ATPase, regulates apoptosis.</p>

<p>PROTACGPX4 degrader-4 is a GPX4 PROTAC degrader with a DC50 of 5.32 nM. It inhibits the activity of cancer cell lines RT4, T24, and J82 with IC50 values of 0.09, 2.97, and 7.58 μM, respectively. This compound elevates lipid ROS levels and induces ferroptosis in T24 and RT4 cells. In T24 tumor-bearing BALB/c nude mouse models, PROTACGPX4 degrader-4 demonstrates antitumor activity. It is applicable to bladder cancer research.</p>

<p>Mechercharmycin A, a cytotoxic compound, was isolated from Thermoactinomyces sp. YM3-251, a marine source. It demonstrates potent antitumor activity.</p>

<p>Garivulimab (BGB-A333), a humanized IgG1 monoclonal antibody, binds to PD-L1, blocking PD-1 interaction and exhibiting antitumor activity.</p>

<p>d-(KLAKLAK)2 is an antimicrobial and antitumor peptide, notable within the group of antimicrobial peptides, and exhibits strong anticancer properties. It kills bacteria by disrupting their cell membranes, causing leakage of cell contents. Additionally, d-(KLAKLAK)2 inhibits tumor cell proliferation by inducing apoptosis through mitochondrial swelling and membrane damage.</p>

<p>Pantinin-1 is an antimicrobial peptide found in the venom of the emperor scorpion (Pandinus imperator). This compound exhibits strong antibacterial activity against Gram-positive bacteria and fungi, but has weaker effects on Gram-negative bacteria. Additionally, Pantinin-1 demonstrates very low hemolytic activity on human red blood cells and possesses anticancer properties, specifically inducing apoptosis in tumor cells.</p>

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

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

<p>Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.</p>

<p>Volrustomig is a bi-engineered fragment crystallizable (Fc) domain, a monovalent bispecific IgG1 monoclonal antibody targeting the key immune checkpoint receptors PD-1 and CTLA-4. It boosts T-cell activation and antitumor immunity, making it a promising immunotherapy for various cancers. Molecular weight: 146.77 kDa.</p>

<p>Ac-FEID-CMK: Potent inhibitor for zebrafish GSDMEb, reduces pyroptosis, and lessens septic AKI.</p>

<p>Boc-Asp(OBzl)-CMK, an inhibitor of IL-1 converting enzyme (ICE, caspase1), prevents the death of CHP100 neuroblastoma cells and inhibits IL-1β release induced by the viral coat protein [1].</p>

<p>PBE-AMF is a prodrug that activates H2O2 and exhibits anticancer activity. It impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing cell death (apoptosis), and blocking the cell cycle. PBE-AMF effectively and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells.</p>

<p>Human PD-L1 inhibitor III is a human PD-L1 inhibitor.</p>

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

<p>Chol-CTPP targets the BBB and glioma cells; when combined with Chol-TPP, forms Lip-CTPP, enhancing anti-glioma drug efficacy.</p>

<p>Iparomlimab: anti-PD-1 IgG4κ antibody, targets PSB103 γ4/κ-chains, forms dimers, used in cancer research.</p>

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

<p>Echitamine chloride, an alkaloid in Alstonia scholaris, has anti-cancer properties and inhibits pancreatic lipase (IC50: 10.92 µM).</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>TD52 dihydrochloride, an Erlotinib derivative, inhibits protein phosphatase 2A and induces apoptosis in TNBC by disrupting CIP2A/PP2A/p-Akt signaling.</p>

<p>Ac-YVAD-CHO acetate, potent reversible ICE and caspase-1 inhibitor; K_i: 3.0 nM (mouse), 0.76 nM (human); blocks IL-lβ production.</p>

<p>PD-L1inhibitory peptide is an inhibitor peptide that targets the programmed cell death ligand 1 (PD-L1). By binding to PD-L1, it lifts immune suppression and restores the anti-tumor activity of T cells. PD-L1inhibitory peptide holds promise for use in tumor research.</p>

<p>Fluorescein-diisobutyrate-6-amide, a powerful inducer of ferroptosis, shows promise for cancer research applications [1].</p>

<p>Apoptosis Inducer 12 (Compound 3z) is a compound that promotes cell death via the mitochondrial pathway and is utilized in cancer research [1].</p>

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

<p>4-Nitrothalidomide is a modified form of thalidomide that inhibits the growth and proliferation of HUVEC cells and is commonly used in the synthesis of pomalidomide, which has anticancer potential.</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>MDM2/4-p53-IN-2 (2q) is a dual MDM2/MDM4 inhibitor, p53 activator; IC50: 70.7 nM(MDM2), 81.4 nM(MDM4); tumor suppressor.</p>

<p>Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region.</p>

<p>ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.</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>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>AM-8553 is potent and selective piperidine the MDM2-p53 interaction inhibitor.</p>

<p>FOXO4-DRI: a peptide blocking FOXO4/p53 interaction; induces senescent cells' apoptosis.</p>

<p>CDC20-IN-2 (14c) is an inhibitor of Cdc20 with a KD of 7.65 μM, inducing G2/M phase arrest, promoting DNA damage accumulation, and stabilizing key substrates such as Cyclin B1 and Bim. This leads to enhanced apoptosis, as well as inhibition of tumor cell proliferation and migration.</p>