Apoptose

<p>LYG-202 is a novel flavonoid with piperazine substitution and antitumor effects in vivo and in vitro.LYG-202 induced apoptosis in MCF-7, MDA-MB-231, and MDA-MB-</p>

<p>Patamostat (E-3123) mesylate is an HDAC inhibitor that promotes cell cycle termination and apoptosis.</p>

<p>Zileuton (A 64077) inhibits 5-lipoxygenase, reduces leukotrienes, aids bronchodilation, lessens mucus/edema, and helps manage asthma symptoms.</p>

<p>Fluvastatin sodium (Fluvastatin sodium salt), a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol</p>

<p>Azilsartan (TAK-536) is an Angiotensin II Type 1 receptor antagonist that lowers blood pressure.</p>

<p>Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM).</p>

<p>Ciprofloxacin monohydrochloride (Bay-09867 hydrochloride) is a broad-spectrum antimicrobial carboxyfluoroquinoline.</p>

<p>Lenalidomide (CC-5013) is an orally immunomodulator. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN). Cost-effective and quality-assured.</p>

<p>ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β.</p>

<p>"Spartalizumab (PDR001), a humanized IgG4 monoclonal antibody, targets PD-1 to inhibit PD-L1/L2 interactions, useful in ATC research."</p>

<p>D-(-)-3-Phosphoglyceric acid disodium: a key glycolysis/gluconeogenesis intermediate, inhibits yeast enolase, crucial in serine, glycine, threonine synthesis.</p>

<p>Benzethonium chloride (Quatrachlor) is a synthetic quaternary ammonium salt with surfactant, antiseptic, and broad spectrum antimicrobial properties.</p>

<p>Ceftiofur sodium (Naxcel), an antibiotic of the cephalosporin type (third generation), is used as veterinary medicine.</p>

<p>SLU-PP-1072: inverse agonist for ERRα/γ, disrupts PCa metabolism, induces apoptosis, studies prostate cancer.</p>

<p>Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR.</p>

<p>Roxithromycin (RU-28965) is a semi-synthetic derivative of the macrolide antibiotic erythromycin with antibacterial and anti-malarial activities.</p>

<p>Carbaryl is a carbamate insecticide/parasiticide with low dermal toxicity used against head lice.</p>

<p>Nifuratel (SAP 113) is a local antiprotozoal and antifungal agent that may also be given orally.</p>

<p>Amcinonide (CL-34699) is a Corticosteroid. The mechanism of action of amcinonide is as a Corticosteroid Hormone Receptor Agonist.</p>

<p>Chlorhexidine is a biguanide antiseptic targeting bacteria, damaging cell membranes and causing cell death, more effective against gram-positive types.</p>

<p>Benazepril hydrochloride (CGS 14824A HCl) is an angiotensin-converting enzyme (ACE) inhibitor widely used in the therapy of hypertension.</p>

<p>Dantrolene sodium treats spasticity by disrupting muscle contraction; not central in action, grouped with central relaxants.</p>

<p>Tasisulam triggers apoptosis, halts mitosis, and normalizes blood vessels to combat cancer.</p>

<p>FAK-IN-24 (Compound 9f) is a potent FAK inhibitor with an IC50 of 0.815 nM. It induces DNA damage and apoptosis, and exhibits activity against glioblastoma. FAK-IN-24 effectively inhibits proliferation of glioblastoma cell lines U87-MG (IC50= 15 nM) and U251 (IC50= 20 nM), and suppresses tumor growth in U87-MG xenograft models.</p>

<p>TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin that induces apoptosis. This compound enhances the expression of p53, caspase-3, caspase-8, caspase-9, and Bax proteins, while reducing Bcl-2 protein levels. TCF4/β-catenin-IN-1 also inhibits CYP3A4, CYP1A2, and CYP2C19, demonstrating significant cytotoxic activity in cancer cells.</p>

<p>GD3 Ganglioside sodium is a crucial ganglioside in human melanoma and functions as an inducer of mitochondrial permeability. It targets mitochondria directly in a manner controlled by bcl-2. Following the aggregation of death-inducing receptors, ceramide accumulates rapidly, synthesizes GD3 ganglioside, and triggers apoptosis.</p>

<p>HYS-072 is an orally active derivative of chrysin with antitumor properties. It induces apoptosis (Apoptosis) and autophagy (Autophagy) by inhibiting the PI3K/AKT/mTOR signaling pathway, and suppresses tumor growth in xenograft models in vivo by modulating autophagy-related pathways. HYS-072 is applicable for research in treating triple-negative breast cancer.</p>

<p>FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.</p>

<p>SHP1 activator 1 (Compound 3n) is an activator of protein tyrosine phosphatase 1 containing the src homology-2 domain (SHP1), with an EC50 of 17.66 μM. It inhibits the proliferation of ABC-DLBCL cells and induces apoptosis by suppressing the STAT3 signaling pathway. In MDA-MB-231 cells, SHP1 activator 1 emits blue and green fluorescent signals, making it suitable as a cellular imaging agent.</p>

<p>HDAC-IN-88 (Compound HJ-9) is a potent inhibitor of HDAC, effectively targeting HDAC6, HDAC1, HDAC2, HDAC8, and HDAC3 with IC50 values of 0.226, 1.103, 2.308, 3.255, and 3.864 μM, respectively. This compound suppresses the proliferation of cancer cells HepG2, HCT116, and MV4-11 with IC50 values of 5.47, 9.78, and 0.38 μM, respectively. Additionally, it inhibits the migration of HCT116 cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis and autophagy in MV4-11 cells. HDAC-IN-88 reduces ROS levels and mitochondrial membrane potential and demonstrates antimalarial activity by inhibiting Plasmodium falciparum 3D7 with an EC50 of 165 nM. Furthermore, HDAC-IN-88 exhibits anti-angiogenic properties.</p>

<p>UAMC-4821 is a ferroptosis inhibitor with an IC50 of 5.2 nM. It effectively scavenges free radicals, inhibits lipid peroxidation, and prevents ML162-induced ferroptosis, providing protective effects on HT-1080 cells. With favorable pharmacokinetic properties in mice, UAMC-4821 presents an oral bioavailability of 63% and demonstrates blood-brain barrier permeability.</p>

<p>OA-Br-1 is an orally active, selective inhibitor of PTP1B with an IC50 value of 7.08 μM. It induces apoptosis and exhibits broad-spectrum anti-cancer cell proliferation activity. OA-Br-1 exerts anti-breast cancer effects both in vitro and in vivo through the PTP1B/PI3K/AKT signaling pathway.</p>

<p>CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that impedes the cell cycle by binding to CDK2, leading to cytotoxicity, increased ROS production, and apoptosis (Apoptosis). It exhibits anticancer activity with an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. CDK2-IN-41 is applicable in research related to AML-associated cancers.</p>

<p>DNMT-IN-4 (Compound 4d) is a DNMT inhibitor with an IC50 value of 5.78 µM. It induces apoptosis and exhibits anticancer activity.</p>

<p>Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.</p>

<p>Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.</p>

<p>CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.</p>

<p>Tubulin polymerization-IN-73 (Compound 37) is an inhibitor of microtubule polymerization with an IC50 of 1.8 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in A549 cells. The compound inhibits the proliferation of both A549 WT and A549/T resistant cells with IC50 values of 0.023 μM and 0.057 μM, respectively. Additionally, Tubulin polymerization-IN-73 demonstrates antitumor activity in mouse models.</p>

<p>Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.</p>

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

<p>Boanmycin, an antibiotic exhibiting antitumor activity, induces cellular senescence and apoptosis [1] [2] [3].</p>

<p>Aloeresin G, a chromone glycoside isolated from Aloe, exhibits a moderate inhibitory effect on TNFα-induced NF-κB transcriptional activity, evidenced by an IC50</p>

<p>Rat form of the beta-Amyloid (1-40) peptide</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

<p>JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.</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>Ferroptosis-IN-17 (Compound 18) is an inhibitor of ferroptosis with an EC50 value of 0.57 μM. It effectively reduces the accumulation of intracellular ferrous ions and lipid peroxidation while restoring levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). In rat plasma, Ferroptosis-IN-17 demonstrates good solubility and notable metabolic stability. This compound holds potential for research in tumor suppression, neurodegenerative diseases, and cardiovascular disorders.</p>