Apoptose

<p>NLRP3-IN-26 (compound 15Z), with an IC50 of 0.13 μM, functions as an inhibitor of NLRP3. It is applicable in studies involving the DSS-induced colitis model [1].</p>

<p>Compound 28 is a nonsteroidal VDR agonist with 690 nM potency, inducing cell cycle arrest and apoptosis in MCF-7 cells.</p>

<p>TAI-95 is an inhibitor of highly expressed cancer protein 1 (Hec1).</p>

<p>VEGFR-2-IN-11 is a potent inhibitor of VEGFR-2 (IC50: 60.27 nM) with an IC50 value of 60.27 nM, which induces apoptosis and has anticancer activity.</p>

<p>ASTX295 is a selective mouse double minute 2 (MDM2) antagonist with an IC50 value of less than 1 nM. It specifically inhibits the interaction between MDM2 and p53, reactivating wild-type (WT) TP53, which subsequently induces the expression of related transcriptional targets, leading to cell death and cell cycle arrest. ASTX295 holds potential for research in lymphoid malignancies such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and T-cell lymphoma.</p>

<p>HAC-Y6 exerts its anticancer effects by inducing cell cycle arrest. It prompts apoptosis in COLO 205 cells with an IC50 of 0.52 µM.</p>

<p>WF-47-JS03: RET kinase inhibitor, crosses blood-brain barrier, 500x more selective for KDR, IC50: 1.7 nM in Ba/F3 cells, 5.3 nM in LC-2/ad lung cancer cells.</p>

<p>Claturafenib is a brain-permeable, selective, all-mutant BRAF inhibitor.PF-07799933 has shown antitumor activity, used in combination with MEK inhibitors.</p>

<p>RIPK1-IN-24 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an IC50 of 1.3 μM. It is utilized in research on inflammatory diseases.</p>

<p>Compound 3 (DOR agonist 2) acts as a Delta Opioid Receptor agonist. It inhibits the expression of TNF-α, obstructs NF-κB transportation to the nucleus, and activates the G protein-mediated ERK1/2 pathway. This compound is useful for research into neurodegenerative diseases.</p>

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

<p>Fosizensertib is an inhibitor of RIP-1 kinase and is used in research related to ulcerative colitis.</p>

<p>Sabialimon P (compound 16), with an IC50 of 18.12 μM, functions as a NO release inhibitor and exhibits anti-inflammatory properties. It effectively diminishes the secretion of TNF-α, iNOS, IL-6, and NF-κB, and suppresses the expression of COX-2 and NF-κB/p65 in LPS-induced RAW264.7 cells.</p>

<p>RSK-IN-2 (Compound 3e) is an inhibitor of RSK, showing IC50 values of 37.89 nM for RSK2, 30.78 nM for RSK1, 20.51 nM for RSK3, and 91.28 nM for RSK4. It suppresses tumor cell proliferation, induces apoptosis, and causes cell cycle arrest at the G2/M phase.</p>

<p>N-ω-chloroacetyl-L-ornithine (NCAO) serves as a powerful reversible competitive inhibitor of ornithine decarboxylase (ODC), displaying cytotoxic and antiproliferative properties against various tumor cell lines, with EC50 values spanning from 1 to 50.6 µM. In vitro studies reveal that NCAO promotes Apoptosis and restricts tumor cell migration. Additionally, it demonstrates significant antitumor efficacy in a mouse model, targeting both solid and ascitic tumors using the myeloma (Ag8) cell line. NCAO holds promise in the development of antitumor agents.</p>

<p>Antitumor Agent-184 (compound 12aa) triggers apoptosis in various cell lines, exhibiting IC50 values of 2.35 μM in B16-F10 cells, 7.32 μM in 4T1 cells, and 10.31 μM in CT26 cells.</p>

<p>AB8939 is a potent small-molecule inhibitor of microtubule/tubulin polymerization, exhibiting antitumor activity (with tumor cell proliferation inhibition IC50≤10 nM). It effectively circumvents resistance mechanisms mediated by P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis.</p>

<p>Belotecan (CKD-602) inhibits DNA topoisomerase I, blocks cell cycle, induces apoptosis, and is a camptothecin-derived anticancer agent.</p>

<p>MDK-3345 is a reversible covalent inhibitor for Mcl-1.</p>

<p>TNF-α-IN-14, a potent TNFα inhibitor, exhibits a selective inhibition profile with an IC50 of 1.1 µM and demonstrates antiinflammatory properties (WO2001072735A2; compound 12) [1].</p>

<p>vacuolar H+-ATPases (V-ATPases) inhibitor</p>

<p>NLRP3-IN-28 (compound N77) serves as a potent inhibitor of NLRP3, effectively blocking Nigericin-induced pyroptosis with an EC50 of 0.07μM. Additionally, it mitigates inflammatory reactions in vivo [1].</p>

<p>YCW-E11 is an antiapoptotic Bcl-2 family proteins inhibitor.</p>

<p>inhibitor of Akt, protein kinase C, PDK1 and cyclin-dependent kinases</p>

<p>WYJ-2, a selective agonist for toll-like receptor 2/1 (TLR2/1), demonstrates an EC50 of 18.57 nM in HEK 293T cells transiently co-transfected with human TLR2 and TLR1. It induces pyroptosis and has shown anticancer activity against non-small cell lung cancer (NSCLC) [1].</p>

<p>NTU281 inhibits transglutaminase-2, lowers creatinine in diabetic rats, reduces proteinuria, and fights glomerulosclerosis.</p>

<p>BMS 310705, an Epothilone B analog, targets ovarian/renal/bladder/lung cancer, inducing apoptosis via mitochondria.</p>

<p>Apoptosis Inducer 5, a lignan enantiomer extracted from Crataegus pinnatifida, demonstrates cytotoxic properties through inducing apoptosis and autophagy in</p>

<p>PD-1/PD-L1-IN-55 (compound D6) is a potent PD-1/PD-L1 inhibitor with an IC50 of 4.8 nM. It enhances IFN-γ secretion and decreases the proportion of late apoptosis due to PD-L1.</p>

<p>Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.</p>

<p>Antitumor agent-77 suppresses cancer cell growth, migration, induces apoptosis, and hinders EMT.</p>

<p>CIL-102 is an apoptosis inducer that functions as an MMP-2/MMP-9 inhibitor, effectively reducing both the protein expression and mRNA levels of MMP-2/MMP-9. CIL-102 also demonstrates anticancer activity.</p>

<p>Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value</p>

<p>Compound 3b inhibits tubulin polymerization, IC50 12.38 µM, with anticancer properties and promotes cell apoptosis.</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>FLT3/TrKA-IN-1: Potent dual kinase inhibitor for FLT3 &amp; TrKA, promising for AML research.</p>

<p>HSP90-IN-10 is a potent HSP90 inhibitor, targeting HCC1954 cells (IC50: 6 μM) and inducing apoptosis, sparing normal cells.</p>

<p>Lometrexol (LY 264618) is an antifolate that inhibits GARFT, blocks purine synthesis, induces apoptosis, and has anticancer properties.</p>

<p>Vatalanib hydrochloride (PTK787 hydrochloride) is an orally available and highly potent tyrosine kinase (VEGF) inhibitor that reduces the number and size of Aβ plaques in the cortex of 5xFAD mice, which may be useful in the study of Alzheimer's disease and cancer.</p>

<p>SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor, with weak inhibitory activity against CDK2, CDK9 and CDK12.Cost-effective and quality-assured.</p>

<p>UH15-38 is a potent and selective RIPK3 inhibitor that blocks necroptosis in alveolar epithelial cells triggered by IAV, useful for studying lung inflammation.</p>

<p>Milademetan (DS-3032), an MDM2 inhibitor, exhibits antitumor activity, induces G1 cell cycle arrest and apoptosis, and can be used to study solid tumors.</p>

<p>Tuvusertib (M1774), an oral ATR inhibitor (Ki&lt;1µM), selectively blocks CHK1 phosphorylation, disrupts DNA repair, and induces tumor cell apoptosis.</p>

<p>Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and antitumor properties, inhibiting Sox4 translation and inducing apoptosis.</p>

<p>PF-07328948 is a branched-chain keto-acid dehydrogenase kinase (BDK) inhibitor, useful for studying CVD metabolic disorders.</p>

<p>BCL6-IN-3: potent BCL6 inhibitor, 70 nM GI50 in SU-DHL4, affects cell functions, antitumor.</p>

<p>HC-5404 is a potent and selective PERK inhibitor, blocking the activation of the PERK pathway, anti-tumor effects, advanced solid tumors and renal cell Cancer.</p>

<p>CP-4126, a lipophilic pro-drug of Gemcitabine, converts to active form by esterases, allowing oral administration with dose-dependent effects.</p>

<p>JAK2-IN-7 selectively inhibits JAK2 (IC50: 3 nM), shows 14-fold selectivity over JAK1/3, FLT3, induces G0/G1 arrest, apoptosis, and has antitumor effects.</p>

<p>FX-11: potent LDHA inhibitor (Ki 8 μM), activates PKM2, reduces ATP, induces oxidative stress/ROS, cell death, shows antitumor effects.</p>

<p>WEHI-539 hydrochloride is a selective Bcl-XL inhibitor with an IC50 of 1.1 nM.</p>

<p>Beta-Zearalenol, a derivative of zearalenone (ZEA) capable of conjugating with glucuronic acid[2], is a mycotoxin produced by Fusarium spp. It induces apoptosis and oxidative stress in mammalian reproductive cells[1].</p>

<p>(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an inhibitor of P-Glycoprotein.</p>

<p>PIM-447 dihydrochloride is an orally available and selective inhibitor of pan-PIM kinase(Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively).</p>

<p>AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.</p>

<p>OBAA is a potent inhibitor of phospholipase A2 (PLA2) with an IC 50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC 50 of 0.4 μM [1] [2] [3].</p>

<p>Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. It also induces apoptosis and inhibits aminopeptidase M, aminopeptidase N, and leucine aminopeptidase, as well as MMP-1, MMP-3, MMP-8, MMP-9, and meprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin exhibits antiproliferative and antitumor activities [1][2][3][4][5].</p>

<p>Amiloride hydrochloride dihydrate (Amiloride HCl dihydrate) is a pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride hydrochloride dihydrate is used in conjunction with DIURETICS to spare POTASSIUM loss.</p>

<p>Ciprofloxacin lactate is a useful organic compound for research related to life sciences. The catalog number is T66299 and the CAS number is 97867-33-9.</p>

<p>DB818 is a synthetic Homeobox A9 (HOXA9) inhibitor and can be used for research on the treatment of acute myeloid leukaemia associated with HOXA9 overexpression.</p>

<p>Imifoplatin (PT-112) is a platinum compound with antitumor activity and may be used to study prostate cancer and immune system disorders.</p>

<p>Swainsonine (Tridolgosir) is an alkaloid isolated from Astragalus membranaceus and is a potent and reversible inhibitor of alpha-mannosidase. swainsonine has antitumour activity and induces apoptosis and cell cycle arrest in the G2/M phase.</p>

<p>Thalidomide-5-COOH is a useful organic compound for research related to life sciences. The catalog number is T64600 and the CAS number is 1216805-11-6.</p>

<p>Vatiquinone, also known as EPI 743, is an orally bioavailable para-benzoquinone being developed for inherited mitochondrial diseases. The mechanism of action of EPI-743 involves augmenting the synthesis of glutathione, optimizing metabolic control, enhanc</p>

<p>Yatein inhibits herpes simplex virus type 1 replication by interruption the immediate-early gene expression. Yatein is a lignan isolated from A. chilensis. It also has antiproliferative activity.</p>

<p>A-192621 is a potent, nonpeptide, orally active, and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and elevates both arterial blood pressure and plasma ET-1 levels[1][2][3]. Its selectivity is 636-fold higher for ETB than ETA (IC50 of 4280 nM and Ki of 5600 nM).</p>

<p>Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms that effectively induces the translocation of nPKC-delta, -epsilon, and -theta, as well as PKC-mu, from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].</p>

<p>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</p>

<p>XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.</p>

<p>SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonistwith antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects.</p>

<p>Thalidomide-O-C6-COOH is a synthetic conjugate that combines a Thalidomide-derived cereblon ligand with a PROTAC technology linker (E3 ligase ligand-linker).</p>

<p>Carubicin HCl is an anthracycline antineoplastic antibiotic. Through intercalates into DNA and interacts with topoisomerase II, Carubicin inhibits DNA replication and repair and RNA and protein synthesis.</p>

<p>Mcl-1 inhibitor 6 binds Mcl-1 with KD 0.23 nM and Ki 0.02 μM, shows strong selectivity over Bcl-2 family, and demonstrates antitumor efficacy.</p>

<p>Thalidomide-O-C5-NH2 hydrochloride is a synthetic compound consisting of a ligand-linker conjugate with E3 ligase activity. It combines a cereblon ligand based on Thalidomide and a linker commonly utilized in PROTAC technology.</p>

<p>Thalidomide-O-amido-C4-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, combines the cereblon ligand derived from Thalidomide with a linker and is commonly used in the synthesis of PROTACs[1].</p>

<p>Ac-IETD-CHO TFA is a granzyme B and caspase-8 inhibitor that inhibits caspase8 activity by blocking caspase3 precursor cleavage.Ac-IETD-CHO TFA inhibits Fas-mediated apoptosis.</p>

<p>MI-773 is a potent inhibitor of the MDM2-p53 protein interaction (PPI) with a high affinity for MDM2 and a Kd value of 8.2 nM. MI-773 exhibits antitumour effects.</p>

<p>PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity.[1] At a 25 uM concentration, PGA2 blocks the cell cycle progression of NIH 3T3 cells at the G1 and G2/M phase .[2] It has also been shown to act as a vasodilator with natriuretic properties.[3]</p>

<p>RRD-251 is an Rb-Raf-1 interaction inhibitor that induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine[1].</p>

<p>PDK1-IN-RS2, a PIFtide mimic, selectively inhibits PDK1, blocking S6K1 activation (Kd: 9 μM).</p>

<p>CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.</p>

<p>Anti-TNBC agent-2 (3j), a purine derivative, acts as an anti-triple negative breast cancer (TNBC) therapeutic.</p>

<p>SMIP34 is an inhibitor of PELP1 that demonstrates the capability to reduce cell viability and colony formation. Additionally, SMIP34 induces cell apoptosis (apoptosis) and causes cell cycle arrest in the S phase. It reduces the expression of PELP1 and exhibits anti-tumor activity. SMIP34 also has potential for research in triple-negative breast cancer (TNBC).</p>

<p>IHMT-MST1-39 is an orally effective MST kinase inhibitor with IC50 values of 42 nM for MST1 and 109 nM for MST2. It activates the AMPK signaling pathway in hepatocytes and inhibits apoptosis in pancreatic β cells. Additionally, IHMT-MST1-39 improves type 1 diabetes in mice induced by Streptozotocin.</p>

<p>DETD-35 is a promising chemical compound in anti-melanoma therapy, functioning as an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways. It enhances cancer cell apoptosis (Apoptosis) and diminishes resistance to Vemurafenib in cancer cells. The compound exhibits IC 50 values of 2.7, 6.0, 3.9, 3.1, and 2.5 μM against melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c, respectively. DETD-35 offers significant potential for advancing research in melanoma treatment strategies.</p>

<p>Taltobulin (HTI-286) is a synthetic analog of the tripeptide cysteine, a microtubule protein inhibitor that inhibits liver tumor cell proliferation in vitro and tumor growth in vivo.Taltobulin is cytotoxic, induces mitotic arrest and apoptosis, and may be used in the study of breast cancer and microtubule tissue-related diseases.</p>

<p>ZSQ836 is a dual covalent inhibitor of CDK12/CDK13 with oral bioactivity, displaying an EC50 value of 32 nM against CDK12. This compound can induce cell apoptosis (apoptosis) and demonstrates in vivo anticancer properties. ZSQ836 is applicable for research in ovarian cancer.</p>

<p>Cyy-272 is an orally active JNK inhibitor with IC50 values of 1.25, 1.07, and 1.24 μM against JNK1, JNK2, and JNK3, respectively. It exerts anti-inflammatory effects by inhibiting the phosphorylation of JNK, thereby alleviating acute lung injury (ALI) induced by lipopolysaccharide (LPS). Moreover, Cyy-272 significantly reduces inflammation in cardiomyocytes and cardiac tissues caused by high lipid concentrations, further mitigating resultant cardiac hypertrophy, fibrosis, and apoptosis. Cyy-272 is utilized in the study of obesity-related myocarditis.</p>

<p>CHMFL-48, an orally active inhibitor of BCR-ABL kinase, demonstrates efficacy against both the wild-type (wt) and various imatinib-resistant mutants. It exhibits potent inhibitory activity, with IC 50 values of 1 nM for the ABL wild-type and 0.8 nM for the ABL T315I mutant. CHMFL-48 operates by inhibiting the autophosphorylation of both wild-type and mutant BCR-ABL, affecting downstream signaling mediators including STAT5 and CRKL. This disruption leads to cell cycle arrest and triggers apoptosis. Given its properties, CHMFL-48 is a promising candidate for research on chronic myeloid leukemia (CML).</p>