Apoptosis

<p>HPCR exhibits antiproliferative activity against various cancer cells and is involved in apoptosis (apoptosis).</p>

<p>KT-253 is a p53 stabilizer and a PROTAC degrader of MDM2 (DC50=0.4 nM). It inhibits the proliferation of cancer cells RS4;11 with an IC50 of 0.3 nM, induces cell cycle arrest in the G2/M phase, and triggers apoptosis. In mouse models, KT-253 demonstrates antitumor activity. (Pink: ligand for target protein MDM2 ligand 4; Black: linker; Blue: ligand for E3 ligase cereblon)</p>

<p>FF2049 is a selective HDAC PROTAC degrader with a DC50 of 257 nM for HDAC1. It facilitates the ubiquitination and degradation of HDAC and promotes apoptosis (Apoptosis). FF2049 is applicable in research involving hematological and solid tumors.</p>

<p>FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.</p>

<p>Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+</p>

<p>15-acetoxyscirpenol: ASM that induces apoptosis, inhibits Jurkat T cell growth dose-dependently, and activates caspases other than caspase-3.</p>

<p>SZU-B6, a PROTAC degrader, targets and degrades SIRT6 with DC50 values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells. It inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cell lines. Additionally, SZU-B6 induces apoptosis in SK-HEP-1 cells and causes cell cycle arrest at the G2/M phase. It demonstrates anti-tumor activity in murine models.</p>

<p>STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.</p>

<p>CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. It exhibits cytotoxicity towards Vero cells with an IC50 of 28.52 μM.</p>

<p>Quercetin-d3 hydrate, a deuterated form of Quercetin hydrate, acts as a flavonoid that stimulates recombinant SIRT1 and serves as a PI3K inhibitor. The compound specifically exhibits IC50 values of 2.4 μM, 3.0 μM, and 5.4 μM against PI3Kγ, PI3Kδ, and PI3Kβ, respectively.</p>

<p>Apoptosisinducer 30 (Compound 15a) acts as an anticancer agent. It induces apoptosis in MCF-7 cells through the mitochondrial pathway. This compound elevates intracellular levels of reactive oxygen species (ROS), decreases mitochondrial membrane potential, and arrests the cell cycle at the G0/G1 phase. Apoptosisinducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and suppresses tumor growth in a mouse breast cancer model.</p>

<p>Tubulin polymerization-IN-70 (compound Q19) is an effective inhibitor of tubulin polymerization. This compound exerts antiproliferative properties by targeting the colchicine binding site on tubulin, thereby inhibiting its polymerization. Tubulin polymerization-IN-70 also induces apoptosis and cell cycle arrest at the G2/M phase. Additionally, it triggers a decrease in mitochondrial membrane potential and elevates levels of reactive oxygen species (ROS). Moreover, Tubulin polymerization-IN-70 possesses anti-angiogenic and anticancer activities.</p>

<p>ECDD-S18 (compound ECDD-S18) induces apoptosis in a dose-dependent manner, effectively targeting the vacuolar ATPase (V-ATPase) and impairing lysosomal acidification.</p>

<p>[Au(L4)(CyJohnPhos)]SbF6 is a gold-containing compound that exhibits inhibitory effects on cyclooxygenase-1/2 (COX-1/2), suppresses the proliferation of colon cancer cells Caco2-/TC7 with an IC50 of 0.98 μM, and induces cell apoptosis (apoptosis). Additionally, [Au(L4)(CyJohnPhos)]SbF6 acts as an inhibitor of thioredoxin reductase (TrxR) and demonstrates antioxidative activity by modulating ROS levels.</p>

<p>Salinomycin sodium salt (Sodium salinomycin), an antibiotic potassium ionophore, is an effective inhibitor of Wnt/β-catenin signaling.</p>

<p>CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS</p>

<p>UM4118 (N-quinolin-8-ylpyridine-2-carboxamide) is a copper ion carrier used in the study of acute myeloid leukemia.</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>Gliotoxin, a mycotoxin, inhibits Wnt pathway, causing apoptosis in mutated colorectal cancer cells and blocks NF-κB by preserving IκB.</p>

<p>SPOP-IN-6lc is a SPOP inhibitor with oncogenic effects in renal cancer cells.SPOP-IN-6lc can be used to study apoptosis.</p>

<p>Borrelidin (Treponemycin) is an inhibitor of trehalose-6-phosphate synthase, a nitrogen-containing macrolide antibiotic isolated from Streptomyces rochei.</p>

<p>POV-PC is an oxidized phospholipid that inhibits VSMC growth under high serum conditions and induces cell apoptosis under low serum conditions.</p>

<p>HFY-4A is a novel HDAC inhibitor.HFY-4A has antitumour activity and has shown antiproliferative activity in breast cancer cells.</p>

<p>FA4-Cu is a compound formed from the effective pancreatic cancer inhibitor FA4 and Cu(II), which can induce apoptosis by triggering ER and mitochondrial stress.</p>

<p>BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein</p>

<p>Compound 2v (Anti-inflammatory agent 45) demonstrates anticancer properties with direct inhibitory impacts on the proliferation of various blood malignancies,</p>

<p>Anticancer Agent 141 (Compound AE), an antimycin alkaloid, exhibits inhibitory potential against HPV-infected cervical cancer.</p>

<p>Compound Rh2 (Anticancer agent 133) is a cytotoxic and antimetastatic agent that induces cell cycle arrest, apoptosis, and autophagy.</p>

<p>Compound 6, fac-[Re(CO)3(L6)(H2O)][NO3], a rhenium(I) tricarbonyl aqua complex, serves as an anticancer agent by disrupting mitochondrial function.</p>

<p>Pyridinium bisretinoid A2E (A2E) TFA, a fluorophore derived from retinal pigment epithelium (RPE) lipofuscin, initiates blue-light-induced apoptosis, mediates</p>

<p>Antitumor agent-112 (compound 3a) is a potent antitumor agent that induces apoptosis and exhibits cytotoxic activity on A549 cells, with an IC50 value of 91.35</p>

<p>Compound 106 (compound 10ic) induces apoptosis in B16-F10 melanoma cells and potently inhibits metastatic nodules in mouse models of lung metastatic melanoma,</p>

<p>FD2157, a photosensitive PI3K inhibitor, exhibits inhibitory IC50 values of 43 nM for PI3Kα, 83 nM for PI3Kβ, 84 nM for PI3Kγ, and 14 nM for PI3Kδ.</p>

<p>CPM-1285 induces apoptosis by effectively inhibiting the function of intracellular Bcl-2 and associated death antagonists.</p>

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

<p>(E/Z)-Squalene modulates ROS, triggers apoptosis/necrosis, reduces liver cholesterol and triglycerides.</p>

<p>A947 is a potent and selective SMARCA2 PROTAC that induces the degradation of SMARCA2, with significant antitumor activity in SMARCA4-mutant NSCLC cells.</p>

<p>VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively.</p>

<p>Cannflavin A, isolated from Cannabis sativa L., exhibits anti-cancer, neuroprotective, and anti-inflammatory activities by inhibiting Aβ1-42 aggregation and</p>

<p>Hexapeptide-11 is a novel proteostasis network modulator in human diploid fibroblasts.</p>

<p>Monensin, from Streptomyces cinnamonensis, inhibits Wnt/β-catenin. Potential anticancer agent.</p>

<p>TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.</p>

<p>PROTAC HIF-1α degrader-1 (compound V2) is an effective proteolysis-targeting chimeric (PROTAC) degrader of hypoxia-inducible factor-1α (HIF-1α), with an IC50 value of 7.54 µM. This compound exhibits anti-proliferative activity, reduces HIF-1α protein expression, and induces apoptosis.</p>

<p>NDI-Lyso is an anticancer agent targeting lysosomes, functioning through an enzyme-induced self-assembly (EISA) mechanism catalyzed by Cathepsin B. In cancer cell lysosomes, it forms rigid long fibers, promoting lysosomal swelling, lysosomal membrane permeabilization (LMP), and membrane disruption. This leads to non-classical caspase-independent apoptosis (Apoptosis). NDI-Lyso demonstrates significant selective anticancer activity across various cancer cell lines and drug-resistant cancer cells (IC50 approximately 10 μM), while exhibiting low toxicity to normal cells (IC50 &gt; 60 μM).</p>

<p>P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).</p>

<p>Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.</p>

<p>MEK/PI3K-IN-2 is a potent dual inhibitor (MEK1 IC50: 352 nM, PI3Kα: 107 nM, PI3Kδ: 137 nM) that reduces pAKT, pERK1/2, and hinders tumor cell growth.</p>

<p>Prodigiosin is a secondary metabolite of Symbiotic bacteria. It also has anti-fungal and anti-cancer activity.</p>

<p>SCR7, a specific DNA Ligase IV inhibitor, blocks nonhomologous end-joining (NHEJ).</p>

<p>BMH-7 HCl is a p53 activator, showing anti-cancer activity by activating the p53 pathway.</p>

<p>Galloflavin Potassium is an inhibitor of lactate dehydrogenase.</p>

<p>Antitumor agent-100 hydrochloride (compound A6), serving as both an apoptosis inducer and molecular glue, exhibits superior anti-tumor activity [1].</p>

<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>CRP protein and its fragment (174-185, RS-83277) boost human monocyte and macrophage cancer-killing effects in vitro.</p>

<p>RMC-7977 is a inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.</p>

<p>Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.</p>

<p>Thalidomide-O-amido-C8-NH2 is a thalidomide-based ligand-linker for PROTAC synthesis.</p>

<p>EGFR-IN-153 (Compound 5l) is an EGFR inhibitor that suppresses the proliferation of MDA-MB-231 cells with an IC50 of 0.73 μM and induces apoptosis. It is applicable for research in breast cancer.</p>

<p>α-Tubulin polymerization-IN-1 (Compound 8l) functions as an inhibitor of α-tubulin polymerization. This compound modulates the NRF2/KEAP-1 signaling pathway and induces ROS production in PC-3 cells, leading to apoptosis. It inhibits the proliferation of PC-3 cells with a GI50 of 0.17 µM, causing cell cycle arrest in the G2/M phase. Additionally, α-Tubulin polymerization-IN-1 demonstrates antitumor activity in mouse models.</p>

<p>NSC 295642: phosphatase inhibitor, boosts phospho-Erk in cells, aids cancer research.</p>

<p>PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal</p>

<p>Kdo2-Lipid A ammonium (KLA) is a selective and potent TLR4 agonist, a lipopolysaccharide.Kdo2-Lipid A ammonium induces the release of TNF and PGE2.</p>

<p>Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.</p>

<p>Acetyl coenzyme A (Acetyl-CoA) is a pivotal molecule connecting multiple cellular metabolic pathways in the tricarboxylic acid cycle, fatty acid synthesis</p>

<p>D-Trimannuronic acid from seaweed induces TNF-α in mouse macrophages; useful in pain, dementia studies.</p>

<p>Macrophage-activating lipopeptide 2 TFA (MALP-2 TFA) is a diacylglycerol lipopeptide and TLR-2/TLR-6 agonist activates immune cell responses macrophages,</p>

<p>Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.</p>

<p>RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.</p>

<p>Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific</p>

<p>ADPM06: nonporphyrin PDT agent; leads in apoptosis, strong IC50 in µM against human tumors.</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>Sterigmatocystine, a G1 phase and DNA synthesis inhibitor, curbs p21 and is a mycotoxin precursor from Aspergillus versicolor.</p>

<p>Cyanoacetamide has inhibitory activity against the myeloid leukaemia cell differentiation protein Mcl-1</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>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>Rasagiline (AGN1135) is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons</p>

<p>Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.</p>

<p>Psalmotoxin 1 is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker.</p>

<p>SP3N hydrochloride is a specific degrader of the prolyl isomerase (FKBP12). Its alkylamine moiety is metabolized into an active aldehyde (SP3CHO), which recruits the SCFFBXO22 ligase for the degradation of FKBP12. SP3N hydrochloride is applicable in cancer research.</p>

<p>Suramin is an RdRp and PTPase inhibitor with anti-parasitic, anti-tumor, and anti-angiogenic activities, inhibiting sirtuins and DNA topoisomerase II.</p>

<p>Barakol, a primary compound found in Cassia siamea, inhibits MMP-3 activity and enhances the anti-metastatic effects of doxorubicin. Additionally, Barakol induces apoptosis (Apoptosis), generates reactive oxygen species, increases the Bax/Bcl-2 expression ratio, and activates caspase-9. This compound also exhibits laxative, anti-anxiety, central nervous system depressant, antioxidant, and anticancer properties.</p>

<p>YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.</p>

<p>HSP90-IN-33 (compound 24e) is an effective Hsp90 inhibitor, demonstrating dissociation constants (Kd) of ≥200 µM for Hsp90α and 7.3 µM for Hsp90β. This compound induces cellular apoptosis (apoptosis) and arrests the cell cycle at the G0/G1 phase. Additionally, HSP90-IN-33 reduces the protein expression of ERα, CDK4, and Akt.</p>

<p>TOPOI/PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI/PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.</p>

<p>FGFR1/VEGFR2-IN-3 (Compound 8m) acts as a dual inhibitor of FGFR1 and VEGFR2. This compound exhibits both anti-cancer cell proliferation and anti-migration activities, and it also has the capability to induce cell apoptosis (apoptosis).</p>

<p>Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with anticancer properties.</p>

<p>ROS inducer 5 (compound 6e) induces intracellular ROS accumulation and subsequent nuclear fragmentation. It can provoke apoptosis in MCF-7 cells with an IC50 of 3.85 μM. ROS inducer 5 is useful for cancer research applications.</p>

<p>Z-VEID-FMK is a selective caspase-6 peptide inhibitor that irreversibly covalently binds to the enzyme, thereby inhibiting apoptosis and DNA breakage.</p>

<p>PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.</p>

<p>EGFR-IN-131 (compound 3a) is an efficacious EGFR inhibitor capable of crossing the blood-brain barrier, with an IC50 value of 272.9 nM. This compound exhibits anti-proliferative activity, induces cellular apoptosis (apoptosis), and causes cell cycle arrest in the G0/G1 phase. Additionally, EGFR-IN-131 reduces the protein expression of p-EGFR.</p>

<p>Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.</p>

<p>MSU-42011: oral RXR-like agonist, inhibits iNOS &amp; p-ERK, antitumor in lung cancer model, effective preclinical treatment.</p>

<p>MAO-B-IN-30 is a selective and potent MAO-B inhibitor that crosses the blood-brain barrier with antiproliferative activity and inhibits both MAO-A and MAO-B.MAO-B-IN-30 reduces the levels of TNF-alpha, IL-6, and NF-kB in organisms, and can be used to study Parkinson's-type neurological disorders.</p>

<p>CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target inhibitor of CYP51/PD-L1, displaying IC50 values of 0.17 and 0.021 μM, respectively.</p>

<p>PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.</p>

<p>β-Apopicropodophyllin, a natural product isolated from Hyptis wticillata, promotes apoptosis through mechanisms including microtubule disruption, DNA damage,</p>

<p>ARV-393 HCl is an orally active and potent PROTAC targeting BCL6 with antitumor activity for the study of non-Hodgkin's lymphoma.</p>