Apoptose

<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

<p>Pomstafib-2, a potent and selective inhibitor of STAT5b, reduces pSTAT5b expression and effectively induces apoptosis [1] [2].</p>

<p>H-20 is a PD-1 agonist that reduces the required dosage of morphine for analgesia. It can be used in studies related to chronic pain.</p>

<p>Cardanol (C15:1), found in cashew nut shell liquid, induces mitochondria-associated apoptosis in human melanoma cells.</p>

<p>VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 of 0.509 µM and an IC50 value of 7.48 μM for inhibiting MCF-7 cell proliferation. Its anticancer activity is exerted through cell cycle arrest, induction of apoptosis (Apoptosis), and modulation of gene expression, making it suitable for breast cancer research.</p>

<p>IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug that suppresses IDO expression. It induces apoptosis, reduces mitochondrial membrane potential, and inhibits tumor cell migration and invasion. Additionally, IDOi-Pt(IV) prodrug-1 triggers reactive oxygen species-mediated endoplasmic reticulum stress and the secretion of damage-associated molecular patterns (DAMPs), leading to immunogenic cell death (ICD). Compared to cisplatin, IDOi-Pt(IV) prodrug-1 exhibits relatively high efficiency and low toxicity in its antitumor activity.</p>

<p>Peginterferon beta-1a: first pegylated interferon for cancer, RMS research; induces tumor cell apoptosis.</p>

<p>NecroIr1, an iridium(III) complex, induces necroptosis in Cisplatin-resistant lung cells, targeting mitochondria and disrupting MMP.</p>

<p>Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.</p>

<p>Stem bromelain: cysteine protease from pineapple stem with fibrinolytic, anti-inflammatory, antitumoral properties.</p>

<p>ERK1/2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.</p>

<p>HTH-01-091 TFA: Potent, selective MELK inhibitor (IC50=10.5 nM); also targets PIM1/2/3, RIPK2, DYRK3, smMLCK, CLK2; used in breast cancer research.</p>

<p>SM-164 Hydrochloride: cell-permeable, binds to XIAP (BIR2/3 domains), IC50 of 1.39 nM, potent XIAP antagonist.</p>

<p>AB-3PRGD2 is a radiolabeled agent that targets integrin αvβ3. It enhances tumor uptake and prolongs retention time in tumors, significantly improving the inhibition of tumor growth. AB-3PRGD2 also remodels the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.</p>

<p>Etanercept is a fusion protein consisting of the soluble portion of the p75-tumor necrosis factor receptor (TNFR) and the Fc fragment of human IgG1 and is commonly used to treat patients with rheumatoid arthritis.Cost-effective and quality-assured.</p>

<p>Haemanthamine hydrochloride, an alkaloid from Amaryllidaceae, has anticancer, antioxidant, antiviral, antimalarial, and anticonvulsant properties.</p>

<p>ATPase-IN-3 is an ATPase (ATPase) inhibitor that can be used in the study of metabolism-related diseases.</p>

<p>Lacto-N-fucopentaose I is a milk oligosaccharide.</p>

<p>WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).</p>

<p>Pexelizumab is a humanized antibody targeting C5 to inhibit apoptosis and treat cerebral IR injury and myocardial infarction.</p>

<p>Izuralimab is a bispecific IgG1 antibody that targets both the inducible T-cell costimulator (ICOS/CD278) and PD-1 [1].</p>

<p>Thalidomide-O-C8-COOH, also known as Cereblon ligand 3, is a Thalidomide-derived compound that serves as a Cereblon (CRBN) ligand for the targeted recruitment</p>

<p>Onfekafusp alfa (L19TNF), a trimeric fusion of L19 scFv and human TNF, targets malignant glioma.</p>

<p>Flavopiridol (Alvocidib) blocks CDK1/2/4/6 by competing with ATP (IC50 ~40 nM); 7.5x selectivity over CDK7; also inhibits EGFR, PKA. In Phase 1/2 trials.</p>

<p>AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG</p>

<p>Nemorosone, a PPAP from C. rosea, inhibits neuroblastoma and pancreatic cancer cell growth, induces apoptosis, and reduces mouse xenograft tumors.</p>

<p>Humulone is a natural product and has a wide range of applications in life science related research.</p>

<p>ChoKα Inhibitor-3, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoK α1 with an IC50 value of 0.66 μM and possesses the capability to</p>

<p>AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.</p>

<p>Sterigmatocystine, a G1 phase and DNA synthesis inhibitor, curbs p21 and is a mycotoxin precursor from Aspergillus versicolor.</p>

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

<p>Relfovetmab is an anti- NGF monoclonal antibody (mAb) [1] .</p>

<p>Apoptosisinducer 31 (compound 19) triggers caspase-dependent apoptosis (cell death). It plays a crucial role in cancer research.</p>

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

<p>PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).</p>

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

<p>F1324 acetate is an efficient, high-affinity b-cell lymphoma inhibitor with IC50 of 1 nM.</p>

<p>Episilvestrol is a derivative of silvestrol with eIF4A-targeted antitumor properties, found in Aglaia silvestris fruits and twigs.</p>

<p>mTORinhibitor-27 (Compound 7e) is an inhibitor of mammalian target of rapamycin (mTOR) with an IC50 value of 5.47 μM. It can induce apoptosis in tumor cells and arrest the cell cycle in the S phase, thereby inhibiting cancer cell growth. mTORinhibitor-27 presents potential for research in cancer, including skin cancer.</p>

<p>Deoxynyboquinone is a potent inducer of cancer cell death with IC(50) values between 16 and 210 nM.</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>Tubulysin B: a potent, cytotoxic microtubule-disrupting peptide from Archangium geophyra and Angiococcus disciformis.</p>

<p>Targaprimir-96 TFA is a selective inhibitor of miR-96 in cancer, inducing apoptosis with high affinity for pri-miR-96 but not affecting healthy cells.</p>

<p>PROTACROR1degrader-1 (Compound 11d) serves as a PROTAC degrader targeting the pseudokinase ROR1, with the capability of degrading ROR1 in NSCLC cells at a DC50 of 40-80 nM. It induces PARP cleavage and apoptosis in NCI-H23 cells. [Pink: ligand for target protein ROR1 ligand-1; Black: linker; Blue: ligand for VHL E3 ligase (S,R,S)-AHPC]</p>

<p>Liensinine is the active constituent of plumula nelambinis with anti-hypertension.</p>

<p>Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.</p>

<p>4-hydroperoxy cyclophosphamide (4-OOH-CY) induces hepatotoxicity. It increases ghrelin levels and enhances inflammatory factors and oxidative markers.</p>

<p>STEP-IN-1 (Compound 14b) is a potent and selective inhibitor of STEP, with an IC50 of 5.27 μM. It offers neuroprotective effects by safeguarding neuronal cells from glutamate-induced toxicity, reducing intracellular reactive oxygen species (ROS) accumulation, and inhibiting apoptosis. STEP-IN-1 is applicable in research related to neurodegenerative diseases.</p>

<p>PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.</p>

<p>BC13 is a CDK6/BRD4 inhibitor with IC50 values of 234 nM for CDK6 and 36 nM for BRD4. It exhibits antiproliferative properties, induces apoptosis (cell death) and DNA damage, and elevates ROS levels.</p>