Apoptosis

<p>Antitumor agent-78 blocks GPx-4, raises COX2, triggers apoptosis, halts EMT, and stifles cancer cell growth and migration.</p>

<p>PD-1/PD-L1-IN-30: Cancer research inhibitor with 0.018 μM IC50.</p>

<p>Anticancer agent 65: Effective on A549 cells, IC50 1.07 μM, halts S phase, triggers apoptosis, elevates p53/p21, causes ROS and MMP collapse.</p>

<p>CCT369260 (compound 1), an orally active inhibitor targeting B-cell lymphoma 6 (BCL6), demonstrates anti-tumor efficacy with an IC50 value of 520 nM [1].</p>

<p>GLUT-1-IN-4 (Compound 13) is an inhibitor of the GLUT-1 glucose transporter that depends on the p53 protein. It suppresses the proliferation of various cancer cells at submicromolar IC50 levels. Additionally, GLUT-1-IN-4 can halt the cell cycle, induce oxidative stress, and promote apoptosis (cell death).</p>

<p>Verrucarin A, a mycotoxin from Myrothecium verrucaria, inhibits protein synthesis, leukemia growth, and triggers apoptosis.</p>

<p>DPP-21 is an inhibitor of microtubule protein polymerization (IC50: 2.4 μM). It exhibits antiproliferative activity against various cancer cell lines, with IC50 values of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23), and 9.37 nM (HepG2). DPP-21 induces cell cycle arrest at the G2/M phase of mitosis and subsequently triggers apoptosis in tumor cells by decreasing Bcl-2 while increasing pro-apoptotic protein Bax levels.</p>

<p>JR5-26B is an orally active apoptosis (apoptosis) inducer. It induces cell death via copper-mediated apoptosis and necroptosis (necroptosis). JR5-26B exhibits antiproliferative activity against MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells, with IC50 values of 0.6, 4.4, 8.0, 1.1, and 3.4 μM, respectively.</p>

<p>BRD4/CK2-IN-1 is a small-molecule inhibitor targeting BRD4 and CK2, inducing apoptosis and autophagy-related cell death.</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>Top/HDAC-IN-3 (Compound 31) is a dual inhibitor of Topoisomerase and HDAC with oral activity. It induces DNA damage by elevating reactive oxygen species (ROS) levels, consequently inhibiting the clonal formation and migration of cancer cells, and triggering apoptosis (Apoptosis) and cell cycle arrest. Top/HDAC-IN-3 demonstrates a significant antitumor effect in NSCLC models, exhibiting a tumor growth inhibition (TGI = 77.5%, 100 mg/kg) superior to that of the HDAC inhibitor SAHA and the combination of SAHA with the topoisomerase inhibitor Irinotecan.</p>

<p>VDX-111, an analog of vitamin D, exhibits cytotoxicity in ovarian cancer cells by upregulating the RIPK1/RIPK3 pathway and inducing necroptosis. It also promotes the expression of cytokines and demonstrates antitumor activity in a mouse model [1].</p>

<p>PD-1/PD-L1-IN-16 is a potent inhibitor of PD-1/PD-L1 (IC50: 53.2 nM) and has shown research potential for tumour immunotherapy.</p>

<p>Antitumor agent-58 suppresses tumor growth, colony formation, cell migration, and induces mitochondrial dysfunction in MGC-803 cells.</p>

<p>RET-IN-11 selectively inhibits RET (IC50: 6.20 nM), promotes apoptosis, and hinders cell proliferation and migration.</p>

<p>ER covalent antagonist-1 (Compound 39D) acts as an antagonist of the estrogen receptor α (ERα). This compound inhibits the proliferation of ERα-positive MCF-7 cells with an IC50 of 0.98 μM, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. Additionally, ER covalent antagonist-1 demonstrates antitumor activity in mouse models.</p>

<p>Antitumor agent-76 is a water-soluble, orally active, rapid-release prodrug of Triptolide that exhibits anticancer effects.</p>

<p>Bomedemstat (IMG-7289) hydrochloride, an oral LSD1 inhibitor, has anticancer properties, blocking cell growth and triggering apoptosis.</p>

<p>Bayer-18 is an inhibitor of TYK2. It inhibits the viability of anaplastic large cell lymphoma cells, including K299, SR786, Mac1, and Mac2a, with an IC50 ranging from 2-3 µM. Additionally, Bayer-18 induces apoptosis in K299 and SR786 cells.</p>

<p>Mcl-1 Inhibitor 9 (Example 2) is a potent inhibitor of myeloid cell leukemia 1 (Mcl-1), demonstrating anti-tumor activity with an IC50 value of 0.21889 nM.</p>

<p>Samuraciclib (CT7001) is a potent oral CDK7 inhibitor (IC50: 41 nM) with anti-breast cancer properties.</p>

<p>ZSH-512 is a potent inhibitor of RARγ with antiproliferative properties. It induces apoptosis and reduces the expression of CD133, NANOG, SOX2, and EPCAM proteins. ZSH-512 exhibits anticancer activity and shows potential for colorectal cancer research.</p>

<p>VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.</p>

<p>TH-6, a potent HDAC inhibitor (IC50: HDAC1-0.115, 2-0.135, 3-0.242, 6-0.138, 8-2.120 μM), blocks cell migration, invasion, and has anti-tumor properties.</p>

<p>3-AP-Me is the dimethyl derivative of the ribonucleotide reductase inhibitor 3-AP (SML0568). It activates the endoplasmic reticulum (ER) stress pathway by promoting eIF2α phosphorylation and upregulating gene expression of transcription factors ATF4 and ATF6, thereby inducing apoptosis. Additionally, 3-AP-Me activates cellular stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase, leading to the upregulation of spliced mRNA variant XBP1. It is applicable in cancer research.</p>

<p>AZD0424: oral Src/Abl kinase inhibitor; potential anticancer; induces apoptosis, cell cycle arrest in lymphoma.</p>

<p>TopoisomeraseII Inhibitor 20 TFA is a potent inhibitor of topoisomerase II with an IC50 of 0.98 µM. It can induce cell apoptosis and exhibits broad-spectrum anticancer activity.</p>

<p>Anticancer agent 54 blocks cell cycle in G0/G1, induces apoptosis, and fights cancer via DNA embedding and ROS.</p>

<p>p53 Activator 14 (Compound 7A) is a derivative of Neratinib that can induce DNA damage and activate p53, thereby inhibiting the proliferation of various cancer cells, with an IC50 of 7.21 μM for HCT116 cells. This compound hinders adhesion, migration, and invasion of HCT116 cells, disrupts the cell cycle, and triggers apoptosis. In addition, p53 Activator 14 exhibits anti-tumor properties and inhibits angiogenesis in the chick embryo chorioallantoic membrane (CAM) model.</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>MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor that specifically targets the Mixed Lineage Kinase domain-like (MLKL) protein.</p>

<p>CHI-KAT8i5 is a selective inhibitor of KAT8 with a KD of 19.72 μM. It induces apoptosis (Apoptosis) in a dose-dependent manner. CHI-KAT8i5 can inhibit tumor growth in esophageal squamous cell carcinoma, colon cancer, melanoma, gastric cancer, non-small cell adenocarcinoma, and liver cancer.</p>

<p>RET-IN-9 is a potent RET kinase inhibitor, potentially useful for studying RET-related diseases, including lung and thyroid cancer.</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>Compound W10 is a dual inhibitor of Topo I (IC50: 0.90μM) and COX-2 (IC50: 2.31μM), inducing cancer cell apoptosis via mitochondria.</p>

<p>PI3K/AKT-IN-1 is a dual inhibitor of PI3K and AKT with anti-cancer activity, inhibiting the PI3K/AKT pathway and inducing caspase 3-dependent apoptosis.</p>

<p>AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.</p>

<p>FAK-IN-4 (Compound 7d) has anticancer activities that can induce cell apoptosis. FAK-IN-4 is potential inhibitor of FAK [1].</p>

<p>L5-DA, a G-quadruplex ligand, stabilizes G4s in HeLa cells, induces apoptosis, and is cytotoxic with an IC50 of 4.3 μM.</p>

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

<p>PF-07328948 is a branched-chain keto-acid dehydrogenase kinase (BDK) inhibitor, useful for studying CVD metabolic disorders.</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>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>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>BCL6-IN-3: potent BCL6 inhibitor, 70 nM GI50 in SU-DHL4, affects cell functions, antitumor.</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>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>Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and antitumor properties, inhibiting Sox4 translation and inducing apoptosis.</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>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>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>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>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>AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.</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>WEHI-539 hydrochloride is a selective Bcl-XL inhibitor with an IC50 of 1.1 nM.</p>

<p>(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an inhibitor of P-Glycoprotein.</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>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>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>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>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>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>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>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>SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonistwith antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects.</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>Imifoplatin (PT-112) is a platinum compound with antitumor activity and may be used to study prostate cancer and immune system disorders.</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>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>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</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>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>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>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>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>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>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>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>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>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>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>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>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>

<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>