Apoptose

<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>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>SB 699551 is a selective 5-HT5A antagonist (Ki=6.31 nM) that enhances 5-HT neuronal function. It inhibits SERT (Ki=25.12 nM),inhibit breast cancer.</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>Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.</p>

<p>BRD4 Inhibitor-39 (compound 12m) is an orally active inhibitor of BRD4 with an IC50 of 0.02 μM. It can induce apoptosis and demonstrates antitumor activity.</p>

<p>Cholesteryl Hemisuccinate Tris Salt is a cholesteryl ester with anticancer activity.Cholesteryl hemisuccinate has antitumor activity and inhibits tumor growth.</p>

<p>Besufetamig is a bispecific antibody targeting programmed cell death protein 1 (PD-1) and the CD3ε chain. It modulates immune cell activity, exerting both immunosuppressive and antitumor effects. Besufetamig holds promise for cancer research.</p>

<p>Z-WEHD-FMK is a cell-permeable and irreversible inhibitor of caspase-1/5. It also shows a robust inhibitory effect on cathepsin B activity (IC50: 6 μM).</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>Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.</p>

<p>IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor, demonstrating an IC50 of 8.7 nM.</p>

<p>c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.</p>

<p>Thalidomide-PEG4-NH2 HCl, a cereblon ligand-linker for PROTAC.</p>

<p>Thalidomide-derived cereblon ligand with PROTAC linker as an E3 ligase ligand-linker conjugate, in hydrochloride form.</p>

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

<p>Nargenicin: a macrolide antibiotic effective against S. aureus, MRSA, M. luteus; inhibits bacterial DnaE and reduces inflammation and leukemia cell growth.</p>

<p>Relfovetmab is an anti- NGF monoclonal antibody (mAb) [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>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>PROTAC FGFR2 degrader 1 (compound N5) is a potent PROTAC that efficiently targets FGFR2, boasting a DC 50 value of 6.46 nM and an FGFR2 IC 50 of 0.08 nM. This compound exhibits significant anti-proliferative effects and high selectivity. It induces G0/G1 arrest in the cell cycles of KATOIII and SNU16 and inhibits apoptosis by diminishing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. Additionally, PROTAC FGFR2 degrader 1 maintains over 50% inhibition of gastric cancer cells at a concentration of 0.17 nM and effectively suppresses the growth of SNU16 xenograft tumors in a mouse model.</p>

<p>S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.</p>

<p>Albanol B, from mulberries, combats Alzheimer's, bacteria, and oxidation, hinders cancer growth, and triggers cell arrest and apoptosis.</p>

<p>Satratoxin G, from Stachybotrys chartarum, triggers apoptosis in nasal and brain OSNs.</p>

<p>Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].</p>

<p>Didocosahexaenoin, omega-3 diglyceride, disrupts mitochondria, induces ROS, apoptosis, and is cytotoxic to prostate cancer cells.</p>

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

<p>SBP-0636457: SMAC mimetic, IAP inhibitor, binds BIR-domains (Ki=0.27μM), potential in tumor/cancer research.</p>

<p>Nrf2 activator-11 (compound M11) is a Nrf2 activator that possesses blood-brain barrier permeability and offers anti-oxidation, anti-inflammation, anti-ferroptosis, and anti-apoptosis properties. It is applicable for use in studying cerebral ischemia-reperfusion (CI/R) injury models.</p>

<p>CS4 is a selective HDAC inhibitor, with IC50 values for HDAC1, HDAC6, HDAC8, HDAC4, and HDAC11 reported as 38 nM, 12 nM, 5.8 μM, 19 μM, and 61 μM, respectively. It enhances the acetylation of α-tubulin and histone 3 (histone 3). Additionally, CS4 activates PPARγ and blocks glycolysis (glycolysis). It induces cell cycle arrest at the G2 phase and triggers apoptosis (apoptosis), exhibiting anticancer effects both in vitro and in vivo.</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>AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.</p>

<p>Vallesiachotamine, a recognized monoterpene indole alkaloid, exhibits anti-tumor activity [1].</p>

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

<p>Tomuzotuximab: fully human, glycoengineered IgG1 anti-EGFR monoclonal antibody with anticancer properties.</p>

<p>dTAG-47 targets FKBP12 F36V for protein degradation, useful in basal-like breast cancer research.</p>

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

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

<p>p53-HDM2-IN-1 is a potent inhibitor of the p53-HDM2 protein-protein interaction, demonstrating an inhibitory concentration (IC 50) of 0.103 μM.</p>

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

<p>Ac-LEVD-CHO, a caspase-4 inhibitor, is a peptide with the sequence Ac-Leu-Glu-Val-Asp-al [1].</p>

<p>MI-1061 TFA: potent MDM2 inhibitor, orally bioavailable, stable (IC50=4.4 nM, Ki=0.16 nM), activates p53, induces apoptosis in mice tumors.</p>

<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>CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).</p>

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

<p>PARP1-IN-27 (Compound 9B) serves as an inhibitor of both PARP1 and PARP2, exhibiting IC 50 values of 2.53 nM and 6.45 nM, respectively, in SUM149PT cells. This compound effectively suppresses the proliferation of BRCA-mutated cancer cell lines such as SUM149PT, HCC1937, and Capan-1, with respective IC 50 values of 0.62, 1.91, and 4.26 μM. Additionally, PARP1-IN-27 exacerbates DNA double-strand breaks, enhances ROS production, causes G2/M phase cell cycle arrest, and triggers apoptosis in SUM149PT cells.</p>

<p>HJC0416 hydrochloride: potent oral STAT3 inhibitor, better anticancer effects than Stattic, promising for breast cancer research.</p>

<p>YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.</p>