Apoptose

<p>Samuraciclib (CT7001) is an oral CDK7 inhibitor with 41 nM IC50, notable for its high selectivity and potency against breast cancer cells.</p>

<p>Ivaltinostat (CG-200745) is an oral panHDAC inhibitor, inducing apoptosis and enhancing cancer drug sensitivity.</p>

<p>GGTI298 is a potent GGTase I inhibitor; IC50 3μM for Rap1A, &gt;20μM for Ha-Ras.</p>

<p>MTDH-SND1 blocker 2 (compound C19) is an effective MTDH-SND1 inhibitor with an IC50 value of 487 nM. It binds to the SND1 protein with a Kd of 279 nM and can degrade the SND1 protein. Additionally, MTDH-SND1 blocker 2 exhibits antiproliferative activity and induces apoptosis, showing potential for breast cancer research.</p>

<p>Spicamycin can be used as a potent inducer of differentiation of human myeloid leukemia cells (HL-60) and murine myeloid leukemia cells (M1).</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>Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.</p>

<p>vacuolar H+-ATPases (V-ATPases) inhibitor</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>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>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>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 28 is a nonsteroidal VDR agonist with 690 nM potency, inducing cell cycle arrest and apoptosis in MCF-7 cells.</p>

<p>LQB-118, an orally active compound sourced from sandalwood, demonstrates multiple therapeutic capabilities. It has shown proficiency in inhibiting glioblastoma cell migration and inducing apoptosis. Additionally, LQB-118 can curtail both migration and invasion of prostate cancer cells by modulating the AKT/GSK3β pathway and regulating MMP-9/reck gene expression. The compound is also effective against yeast polysaccharide-induced inflammation in both in vivo and in vitro settings. Notably, LQB-118 specifically triggers ROS-mediated and mitochondrial-dependent apoptosis in Leishmania amazonensis, highlighting its potential in studies focusing on inflammation, infections, and various cancers.</p>

<p>Ferroptosis-IN-6 is an efficient ferroptosis inhibitor, protecting cells from cell death induced by ferroptosis inducers, and inhibiting STY-BODIPY oxidation.</p>

<p>CDK2/9-IN-1 (compound 20a) is an orally active dual inhibitor of CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM for CDK2 and CDK9, respectively. It induces apoptosis by regulating G2/M cell cycle arrest and exhibits antitumor activity.</p>

<p>EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of the L858R/T790M/C797S mutant EGFR kinase, with an IC50 value of 0.87 nM. EGFR-IN-161 effectively inhibits tumor cell apoptosis, G1 phase arrest, and migration.</p>

<p>Topoisomerase I/II inhibitor 4 halts cell growth and spread, induces apoptosis, and is used in liver cancer research.</p>

<p>MI-888 (TFA) is an orally active inhibitor of the MDM2-p53 interaction with a Ki of 0.44 nM. It can induce rapid, complete, and durable tumor regression in xenograft mouse models.</p>

<p>PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual inhibitor targeting PD-L1 and VISTA. It effectively hinders the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), leading to the reactivation of T cells. Additionally, PD-L1/VISTA-IN-1 exhibits antitumor activity.</p>

<p>SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. It effectively suppresses the expression of SIRT1, SIRT2, and SIRT3, leading to increased acetylation and activation of p53. Additionally, SIRT-IN-7 inhibits the proliferation of breast cancer cells and induces apoptosis and autophagy, demonstrating antitumor activity.</p>

<p>Rezatapopt (PC14586) is a p53 reactivator with antitumor activity for the study of locally advanced or metastatic solid tumors.</p>

<p>CLM3, a pyrazolopyrimidine derivative, functions as a multitargeted tyrosine kinase inhibitor. It exhibits antiproliferative and proapoptotic activities on endothelial and cancer cells, activities that are synergistically enhanced by SN38. The primary mechanism of action for CLM3 involves the inhibition of phosphorylation in tyrosine kinases such as VEGFR-2, EGFR, and RET, along with their associated signaling pathways.</p>

<p>FGFR4-IN-7 is a covalent, reversible FGFR4 inhibitor (IC50: 0.42 μM) that blocks the FGFR4 signaling pathway, thereby inducing apoptosis.</p>

<p>VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor (IC50: 3.4 nM). vEGFR-2-IN-13 arrests the HepG2 cell cycle in G2/M phase and induces apoptosis.</p>

<p>Caspase-3 Activator 4 (compound 4o) is an effective caspase-3 activator that can cross the blood-brain barrier. This compound exhibits antiproliferative activity and can induce cell apoptosis (apoptosis). Additionally, Caspase-3 Activator 4 enhances the gene expression of TNF-α and reduces the expression of cleaved caspase-3/caspases 3.</p>

<p>WK88-1, an inhibitor of Hsp90, effectively induces the degradation of various oncogenic signaling molecules, including EGFR, ErbB2, and ErbB3, in the gefitinib-resistant H1975 cell line. This leads to subsequent growth arrest and apoptosis.</p>

<p>LA-CB1 is a derivative of Abemaciclib that targets CDK4/6 and promotes their degradation via the ubiquitin-proteasome pathway, thereby blocking the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis (Apoptosis). It demonstrates antiproliferative activity against MDA-MB-231 cells with an IC50 of 0.27 µM and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In highly invasive models like triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth, showing robust dose-dependent antitumor activity. This compound can be utilized in breast cancer research.</p>

<p>PI3K-IN-58 (Compound 17f) is an inhibitor of PI3Kα with an IC50 value of 0.039 μM. It shows significant antiproliferative effects on PC-3, 22RV1, MDA-MB-231, and MDA-MB-453 cell lines with IC50 values of 3.48 μM, 1.06 μM, 2.21 μM, and 0.93 μM, respectively. PI3K-IN-58 induces apoptosis by downregulating the expression of anti-apoptotic proteins Bcl-XL and Bcl-2 while upregulating the expression of the pro-apoptotic protein BAX. This compound is applicable for research in cancer targeting through PI3K pathways.</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>Antitumor agent-37: strong anti-growth, anti-spread, induces DNA damage, apoptosis via Bcl-2/Bax/caspase3, boosts immune response.</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>Mcl-1 inhibitor21 (Example 1-36) is an Mcl-1 inhibitor with an IC50 of 328 nM. It exhibits pro-apoptotic and anti-proliferative activity against SUDHL5 and SUDHL10 cell lines, making it applicable for cancer research.</p>

<p>Top/HDAC-IN-1: Dual Top/HDAC inhibitor, potent against HDAC1-3,6,8 and HCT116 cells; blocks G2 phase, induces apoptosis.</p>

<p>PI3K-IN-35 (6l) selectively inhibits PI3K-α, β, δ (IC50: 13.98, 7.22, 10.94 μM), blocks G2/M phase, induces apoptosis, and is useful in leukemia research.</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>Samuraciclib (CT7001) is a potent oral CDK7 inhibitor (IC50: 41 nM) with anti-breast cancer properties.</p>

<p>Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.</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>Antiproliferative agent-4 suppresses cancer cell growth with low toxicity, inhibits tumors in mice, and induces apoptosis in EC109 cells.</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>Minnelide is a prodrug of triptolide,and shows potent antitumor activity in a number of tumor types.</p>

<p>Tandutinib (MLN518) sulfate is an effective and selective inhibitor of FLT3, with an IC50 value of 0.22 μM. It also inhibits c-Kit and PDGFR, displaying IC50 values of 0.17 μM and 0.20 μM respectively. This compound can be utilized in the treatment of acute myeloid leukemia and has the capability to cross the blood-brain barrier.</p>

<p>ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2 that promotes the accumulation of DSBs and the degradation of ERK1/2 expression. This compound decreases BCL-2 levels and induces DNA damage by inhibiting PARP and ERK1/2. Additionally, ERK1/2 inhibitor 11 activates caspase 3 to induce apoptosis.</p>

<p>MLS-0053105, a chloromaleimide, functions as a selective inhibitor of BFL-1, exhibiting an IC50 of 0.4 µM against Bfl-1/F-Bid. Its inhibitory potency is over tenfold lower for Bcl-W, Bcl-2, and Bcl-XL, and it shows no activity against Bcl-B and Mcl-1.</p>

<p>TRPM7-IN-1 (compound SUD) is a benzamide-urea derivative and an effective inhibitor of TRPM7. This compound induces cell cycle arrest and apoptosis in MCF-7 and BGC-823 cells, reducing their migration capabilities. It decreases vimentin expression while increasing E-cadherin expression. TRPM7-IN-1 reduces TRPM7-like currents and inhibits TRPM7 expression by activating the PI3K/Akt signaling pathway. This compound shows potential as a therapeutic agent for reducing breast and gastric cancer metastasis by targeting TRPM7 expression and activity.</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>TI17 is a selective TRIP13 inhibitor with anticancer activity and inhibits proliferation of multiple myeloma (MM) cells</p>

<p>Casuarinin, an ellagitannin found in pomegranates and certain Casuarina/Stachyurus plants, is a carbonic anhydrase inhibitor and astringent.</p>

<p>GP130-IN-1 (compound 49) is an effective inhibitor of GP130, demonstrating significant in vitro anti-tumor activity and higher selectivity compared to Bazedoxifene. It induces ultrastructural changes in cells, leading to a time-dependent arrest of the cell cycle at the G0/G1 phase, and triggers both apoptosis and autophagy. GP130-IN-1 is useful for research on triple-negative breast cancer.</p>

<p>PD-L1-IN-1, potent PD-L1 inhibitor with 115 nM IC50, suppresses tumors, boosts immune response, and spares healthy cells.</p>

<p>TopoisomeraseI/II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI/II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.</p>

<p>Lysosomal P-gp targeted agent 1 (Compound 14) is an antitumor drug that targets lysosomal P-glycoprotein (Pgp). It is selectively transported to lysosomes via overexpressed Pgp, releasing nitric oxide that generates reactive oxygen species (ROS), causing lysosomal membrane permeabilization (LMP) and inducing apoptosis. This compound can overcome resistance mediated by P-glycoprotein, leading to cell cycle arrest while maintaining relatively low toxicity to normal cells. It exhibits antitumor activity by significantly inhibiting tumor growth.</p>

<p>Antitumor agent-72 (compound 6w) is a potent anticancer agent that exhibits its anticancer activity by inducing apoptosis via caspase-3 activation and PARP</p>

<p>EGFR-IN-3 is an EGFR inhibitor with antitumor activity.EGFR-IN-3 inhibits EGFRwt-TK, induces apoptosis (cell death), and can block cells in the G2/M phase.</p>

<p>T0080 is an FPR-1 antagonist. It reduces apoptosis (Apoptosis) and inhibits the production of reactive oxygen species (ROS) and pro-inflammatory cytokines (TNF-α and IL-1β) in plaque macrophages within ApoE−/− mouse models, thereby slowing the progression of atherosclerosis.</p>

<p>FTO-IN-13 (compound 8t) is a potent FTO inhibitor with antiproliferative properties. It induces apoptosis (cell apoptosis) and reduces the expression of Bcl-2 and Caspase 3 active proteins. Additionally, FTO-IN-13 lowers the expression of MYC and CEBPA genes and demonstrates anticancer activity.</p>

<p>L-threo-Sphingosine C-18 is a protein kinase C inhibitor.</p>

<p>β-Carotene-13C10 (Provitamin A-13C10) is a form of β-Carotene labeled with 13C. It is a carotenoid compound and serves as a natural precursor to vitamin A. This compound acts as a regulator of reactive oxygen species (ROS), exhibiting both antioxidant and anti-inflammatory properties. Depending on its intrinsic characteristics and the redox potential of the biological environment, β-Carotene can function either as an antioxidant or a pro-oxidant. It also possesses anticancer activity, inducing apoptosis in breast cancer cells.</p>

<p>DL-Buthionine-(S,R)-sulfoximine hydrochloride (Buthionine sulfoximine hydrochloride) is a potent and specific glutamylcysteine synthetase biosynthesis inhibitor</p>

<p>MB710 is an amino-benzothiazole derivative that tightly binds to the Y220C pocket and stabilizes p53-Y220C in vitro.</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>GPX4-IN-3 (26a) is a potent GPX4 inhibitor, inducing selective ferroptosis with 71.7% inhibition at 1 μM.</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>inhibitor of Akt, protein kinase C, PDK1 and cyclin-dependent kinases</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>

ASCT2-IN-1 (compound 20k) is an inhibitor of ASCT2, demonstrating IC50 values of 5.6 μM in A549 cells and 3.5 μM in HEK293 cells. It induces apoptosis and inhibits tumor growth.

A signal-specific JNK/p38 pathway and TAK 1 inhibitor

<p>tDHU, acid is a dihydropyrimidine cereblon ligand consisting of an E3 ligase ligand and a benzoic acid linker. It serves as an E3 ubiquitin ligase ligand-linker conjugate in the development of PROTACs.</p>

<p>RIPK1-IN-23 (compound 19) is an RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC50 = 1.7 nM). Additionally, RIPK1-IN-23 exhibits anti-inflammatory properties.</p>

<p>STAT3-IN-9 hinders STAT3 at Tyr705, doesn't affect STAT1 Tyr701, induces apoptosis, and arrests cells in G2/M phase.</p>

<p>Compound B6, also known as TOPOI/PARP-1-IN-1, is a dual inhibitor targeting TOPOI and PARP, exhibiting low cytotoxicity and oral activity with a PARP1 IC 50 of 0.09 μM. This compound effectively inhibits cancer cell proliferation and migration, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. In murine models, TOPOI/PARP-1-IN-1 demonstrated a tumor growth inhibition rate (TGI) of 75.4% [1].</p>

<p>LMP7-IN-1 may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer, is an inhibitor of</p>

<p>EGFR-IN-134 (compound 3f) is a triazolo[3,4-a]quinoline derivative and functions as a potent EGFR inhibitor with an IC50 of 0.023 µM. It induces apoptosis and necrosis in cells, and causes cell cycle arrest in the G2/M and pre-G1 phases. EGFR-IN-134 modulates the expression of apoptosis-regulating proteins by downregulating anti-apoptotic protein Bcl2 and upregulating pro-apoptotic proteins p53, Bax, and caspases 3, 8, and 9, demonstrating significant antiproliferative and anticancer activities.</p>

<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>

Z-VA-DL-D-FMK (Z-VA-DL-D(OH)-FMK) acts as an inhibitor of caspases. It irreversibly binds to caspases, enhancing the sensitivity to TNF-α and stimulating HIV replication in infected T cells ACH-2.

<p>ASP9831 is an orally active PDE4 inhibitor. It suppresses LPS-induced TNF-α production and exhibits anti-inflammatory properties. ASP9831 is useful in the study of steatohepatitis.</p>

<p>BMI-135, a selective estrogen mimic, demonstrates agonist activity for the estrogen receptor and induces a rapid endoplasmic reticulum stress response (UPR) alongside apoptosis in breast cancer cells.</p>

<p>KIM-161 is a PIK3CA inhibitor. It demonstrates significant antiproliferative activity, with IC50 values of 1.428 and 1.562 µM against PI3KCA-mutant breast cancer cell lines MCF7 and T47D, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway, leading to ROS production. It is applicable for research on breast cancer and its PI3KCA-mutant subtypes.</p>

<p>WB436B, a highly selective STAT3 inhibitor, effectively targets and inhibits STAT3-Tyr705 phosphorylation along with the expression of STAT3 target genes. It exhibits cytotoxic effects on pancreatic cancer cells by inducing apoptosis. Furthermore, WB436B suppresses tumor growth and metastasis in pancreatic cancer mouse models, thereby prolonging the survival of tumor-bearing mice.</p>

<p>Spliceostatin A is an anticancer agent and splicing inhibitor that induces apoptosis by inducing cell cycle arrest in the G1 and G2/M phases.</p>

<p>Topoisomerase inhibitor4 (compound 45) acts as an effective inhibitor of Topoisomerase1/2, arresting the cell cycle at the G2/M phase and inducing Apoptosis. This compound exhibits potent antitumor activity.</p>

NDs-IN-1 (Compound 3g) is a novel non-covalent multi-target inhibitor that inhibits the activities of key enzymes such as hBACE-1, hAChE, and hMAO-B, and is primarily used in the study of neurodegenerative diseases [1].

<p>ADH-6, a tripyridylamide, disrupts mutant p53 aggregates in cancer cells, reviving its function and inducing apoptosis.</p>

<p>PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.</p>

<p>SLCB050 is a compound with anticancer activity that inhibits the interaction between DX2 and p14/ARF. It decreases the viability of human lung cancer cells, particularly small cell lung cancer cells, in a p14/ARF-dependent manner, and induces cell apoptosis (apoptosis) and senescence.</p>

<p>MJC13 is an FKBP52-targeting agent with antitumor activity, suitable for prostate cancer research.</p>

<p>Sampangine, an alkaloid, induces apoptosis by causing cell cycle arrest at the G0/G1 phase and inhibits the biosynthesis of heme.</p>

<p>Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and exhibits low oral bioavailability. By inhibiting cGAMP degradation, it effectively activates the intracellular STING pathway. Enpp-1-IN-25 can enhance immune cell infiltration and type I interferon response in the tumor microenvironment, thereby increasing the antitumor efficacy of anti-PD-L1 antibodies. It is applicable for research in cancer immunotherapy.</p>

<p>17-Demethoxy-reblastatin (17-DR) acts as an inhibitor of heat shock protein 90 (Hsp90). It suppresses the proliferation of HepG2 and SMMC7721 cancer cells, diminishes colony formation, and triggers apoptosis via a mitochondria and caspase-mediated pathway.</p>

<p>Apoptosisinducer 25 (Compound 4H) demonstrates potent anticancer capabilities by inhibiting the proliferation of BGC-823 cancer cells with an IC50 of 0.37 μM. It induces apoptosis in BGC-823 cells, causes mitochondrial dysfunction, and arrests the cell cycle at the G2/M phase. Additionally, Apoptosisinducer 25 exhibits favorable pharmacokinetic properties in rats.</p>

<p>TfR-1-IN-1 is a TfR-1 inhibitor, also a Fe(III) salivary phenol complex, inducing apoptosis and inhibiting tumor and normal cell growth.</p>

<p>3′-Hydroxyflavanone is a cyclized flavonoid with anti-tumor properties that induces apoptosis in HeLa cells.</p>

<p>CRI9 effectively inhibits the c-MET/PI3K/Akt/mTOR axis, suppressing the proliferation of hepatocellular carcinoma (HCC) cells. This compound exhibits potent cytotoxicity against HCC cells and induces apoptosis.</p>

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

<p>PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).</p>

<p>CB-184 is a selective ligand for sigma-2 (σ2) receptors, with Ki values of 7436 nM for sigma-1 (σ1) and 13.4 nM for sigma-2 (σ2), and it promotes apoptosis with antitumor activity.</p>

<p>Microtubule inhibitor 2: potent, selective, oral, induces ferroptosis, strong antitumor effect.</p>

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

<p>SL-176, a WIP1 inhibitor, when combined with GSK-J4, can induce cell cycle arrest and apoptosis (apoptosis), thereby inhibiting tumor growth both in vitro and in vivo.</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>06:0 PE (PE(6:0/6:0)) is a water-soluble phospholipid characterized by its short acyl chains. It possesses notable antitumor activity and can inhibit tumor progression in the body. Additionally, it exhibits antiproliferative and pro-apoptotic properties, and serves as a precursor for phosphatidylcholine and phosphatidylethanolamine.</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>RIPK1-IN-28 (compound 13) is an orally active inhibitor of RIPK1. It exhibits inhibitory effects on human I2.1 and Hepa1-6 cells, with IC50 values of 0.4 and 1.2 nM, respectively.</p>

<p>VEGFR-2-IN-18 is a potent VEGFR-2 inhibitor with a 60 nM IC50, promoting cell apoptosis and anticancer effects.</p>

<p>VEGFR-2-IN-15 (Compound 14b) is a potent inhibitor of VEGFR-2. VEGFR-2-IN-15 inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.</p>