Apoptose

<p>TZEP7 functions as an EGFR kinase inhibitor in cancer cells. It exhibits cytotoxicity and induces apoptosis within these cells. TZEP7 downregulates the anti-apoptotic protein Bcl-2, upregulates the pro-apoptotic protein Bax, and increases caspase levels. This compound holds potential for research in anticancer drug development.</p>

<p>EMT inhibitor-3 (compound 11i) is an epithelial-mesenchymal transition (EMT) inhibitor that effectively suppresses the proliferation, migration, and invasion of SK-N-SH neuroblastoma cells, with an IC50 value of 2.5 μM. It induces mitochondrial-mediated intrinsic apoptosis in tumor cells by enhancing the Bax/Bcl-2 protein expression ratio, promoting the release of cytochrome C from mitochondria, and activating caspase 9 and caspase 3. EMT inhibitor-3 is applicable for cancer research.</p>

<p>MA242 is a nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy and dual inhibitor of murine double minute 2 (MDM2).</p>

<p>PROTAC FKBP Degrader-3, with FKBP and VHL binding groups linked, is a potent FKBP degrader.</p>

<p>ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. This compound is potentially applicable in research involving ASK1 signaling pathways, including studies on cellular stress response, inflammatory response, neurodegenerative diseases, and cardiovascular diseases.</p>

<p>Ferroptosis-IN-18 (51) is a phenothiazine derivative known for its potent anti-ferroptotic and antioxidant properties. It is useful for research related to intracerebral hemorrhage (ICH).</p>

<p>Apoptosisinducer 36 (Compound 42) exhibits anti-leukemic activity by reducing leukemia stem cells (LSC) and inducing differentiation. It inhibits proliferation of AML cells by causing cell cycle arrest in the G1 phase, and induces PANoptosis, which includes apoptosis, pyroptosis, and necrosis.</p>

<p>WEHI-539 is a selective Bcl-XL inhibitor (IC50: 1.1 nM).</p>

<p>MD102, with an IC50 value of 0.35 μM, is a potent TG2 inhibitor that stabilizes p53 by inhibiting TG2. This results in a decrease in p-AKT and p-mTOR downstream signaling, ultimately inducing tumor cell apoptosis [1].</p>

<p>Scytonemin, a cyanobacterial pigment, inhibits cancer cell growth by decreasing Plk1 activity, especially effective on U266 myeloma cells.</p>

<p>PD-L1/HDAC6-IN-1 (Compound HP29) is an inhibitor targeting both PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction and inhibiting HDAC6 activity, with IC50 values of 26.8 nM and 69 nM, respectively. This compound enhances the cytotoxicity of Jurkat T cells against HepG2 cells, exhibiting an IC50 of 3.4 μM. In rats, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics, showing a drug exposure level of 871.62 ng·h/mL, and displays antitumor activity in a B16-F10 xenograft mouse model.</p>

<p>MG28 exhibits significant cytotoxic effects, likely stemming from its direct and potent DNA-damaging activity. The compound is utilized in cancer research.</p>

<p>Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.</p>

<p>RIPK1-IN-14 inhibits RIPK1 with 92 nM IC50 and reduces necrotic apoptosis in U937 cells.</p>

<p>Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. It induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, while decreasing GPX4 protein expression. Nur77 agonist-1 binds with affinity to the ligand binding domain of Nur77, with a KD of 13.80 μM. It demonstrates significant antiproliferative activity against various breast cancer cells (IC50: 2.15-3.26 μM) and exhibits low cytotoxicity towards normal cells. This compound is useful for breast cancer research.</p>

<p>SSB-2548 is a CXCR-4 inhibitor that suppresses the proliferation and migration of acute myeloid leukemia cells and induces apoptosis (apoptosis). It is well absorbed in the gastrointestinal tract and can be used for leukemia research.</p>

<p>KMUP-1 is a xanthine derivative known for its vasodilatory properties. It functions as a phosphodiesterase (PDE) inhibitor and an activator of soluble guanylate cyclase (sGC), engaging the NO/sGC/cyclic guanosine monophosphate pathway. Additionally, KMUP-1 can open K+ channels and has the potential to alleviate ischemia-induced cardiac myocyte apoptosis (apoptosis). This compound is useful in cardiovascular and anti-inflammatory research.</p>

<p>Fluvastatin (XU 62-320) sodium monohydrate, a fully synthetic competitive HMG-CoA reductase inhibitor, features an IC 50 of 8 nM. This compound also safeguards vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway [1] [2].</p>

<p>Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2/M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [1].</p>

<p>Isoforretin A is a potent inhibitor of thioredoxin-1 (Trx1) with significant biological activity, inducing anti-tumor effects mediated by reactive oxygen species (ROS). The compound inhibits Trx1 activity by covalently binding to the activation site residues Cys32/Cys35, which triggers ROS accumulation, leading to DNA damage and apoptosis (Apoptosis) in cancer cells. Additionally, Isoforretin A has demonstrated the ability to suppress the growth of HepG2 tumors in a mouse hepatic cell carcinoma xenograft model.</p>