Apoptose

<p>CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LD). It exhibits phototoxicity against breast cancer cells with an IC50 of 0.01-0.02 μM and demonstrates antitumor efficacy in a 4T1 xenograft mouse model.</p>

<p>Soquelitinib (CPI-818) is a selective ITK inhibitor， inhibits tumor growth,T-cell, up-regulatCXCR3, IFNγ, TNFα, and CD107a expression in normal CD8 cells.</p>

<p>Thalidomide-NH-C5-NH2 is a synthetic E3 ligase ligand-linker conjugate, consisting of a Thalidomide-based cereblon ligand and a linker, used in the synthesis of PROTACs.</p>

<p>VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, which inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.</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>ZLHQ-5f inhibits CDK2/Topo I, with IC50 of 0.145μM for CDK2/CycA2, and promotes apoptosis by arresting HCT116 cells in S phase.</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>HDAC-IN-9, a dual tubulin/HDAC inhibitor, impedes A549 cell invasion/migration and shows strong anti-tumor/angiogenic effects.</p>

<p>Compound C11 inhibits 14-3-3η protein (KD: 35 μM), targets liver cancer cells, blocks G1-S phase, and induces apoptosis.</p>

<p>Pan-Trk-IN-3: potent Trk inhibitor (IC50: 2-26 nM), effective against drug-resistant mutants, induces apoptosis, anti-tumor effects.</p>

<p>DNMT1-IN-5 (Compound 55) is an inhibitor of DNMT, specifically targeting DNMT1 and DNMT3A, with IC50 values of 2.42 μM and 14.4 μM, respectively. It demonstrates antiproliferative effects across various cancer cell lines (TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226, and HCT116) with IC50 values ranging from 0.19 to 2.37 μM. The compound induces G2/M phase cell cycle arrest and apoptosis in TMD-8 and DOHH2 cells. Additionally, DNMT1-IN-5 exhibits antitumor efficacy in a TMD-8 xenograft mouse model.</p>

<p>Ferroptosis-IN-15 (compound 12) serves as an effective inhibitor of ferroptosis, exhibiting EC50 values of 0.76 μM and 0.67 μM in A375 cells and 786-O cells, respectively. It acts as a potential iron chelator and radical-scavenging antioxidant.</p>

<p>SMIP34 is an inhibitor of PELP1, binding to this target with a dissociation constant (Kd) of 37.4 μM. It demonstrates efficacy in inhibiting the proliferation of cancer cells and tumor progression. Specifically, SMIP34 is effective in breast cancer research, showing activity against wild-type (WT), mutant (MT) estrogen receptor-positive (ER+), and treatment-resistant (TR)-ER+ breast cancers.</p>

<p>ZIF-8 is an anticancer agent that can inherently trigger pyroptosis through a caspase-1/gasdermin D (GSDMD)-dependent pathway.</p>

<p>4-Hydroxyresveratrol (3,4,5,4'-Tetrahydroxystibene) is a resveratrol analog that variably induces the expression of pro-apoptotic genes such as p53 and Bax. It triggers apoptosis in SV40 virus-transformed WI38 cells (WI38VA), but not in WI38 cells. Additionally, 4-Hydroxyresveratrol significantly increases the expression of p53, GADD45, and Bax genes in WI38VA cells, while suppressing the expression of the bcl-2 gene.</p>

Etalocib (LY293111) sodium is an orally active leukotriene B4 (LTB4) receptor antagonist with a Ki value of 25 nM for inhibiting [3H]LTB4 binding. It exhibits an IC50 of 20 nM against LTB4-induced calcium mobilization. Additionally, Etalocib sodium can induce apoptosis.

<p>NLRP3-IN-72 (Compound 2) is a benzimidazole derivative. It exhibits anti-inflammatory and antioxidant properties, with an IC50 of 0.3 μM for NLRP3 IL-1β, a PD50 of 0.4 μM for protection against cell pyroptosis, and an EC50 of 0.6 μM for inducing HO-1.</p>

<p>Isoforretin A is a potent inhibitor of thioredoxin-1 (Trx1) with significant biological activity, inducing anti-tumor effects mediated by reactive oxygen species (ROS). The compound inhibits Trx1 activity by covalently binding to the activation site residues Cys32/Cys35, which triggers ROS accumulation, leading to DNA damage and apoptosis (Apoptosis) in cancer cells. Additionally, Isoforretin A has demonstrated the ability to suppress the growth of HepG2 tumors in a mouse hepatic cell carcinoma xenograft model.</p>

<p>GNE684 inhibits RIP1; Ki app: 21 nM (human), 189 nM (mouse), 691 nM (rat).</p>

<p>BRD-K44839765 selectively targets Bcl-2, exhibiting an IC50 of 5.6 μM in IMR-90 cells. This compound is also orally active.</p>

<p>BRD-K20733377 is a Bcl-2 inhibitor that exhibits selective cytotoxicity toward senescent cells, specifically inhibiting the activity of etoposide-induced senescent IMR-90 cells with an IC50 of 10.7 μM. Additionally, BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21, and KI67 in aged mouse models.</p>

<p>HDAC-IN-81 (Compound 11g) is an HDAC inhibitor capable of effectively inhibiting HDAC1 with an IC50 value of 4.5 nM. Additionally, it exhibits anticancer activity by inhibiting cell proliferation and can induce cell apoptosis (apoptosis).</p>

<p>Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.</p>

<p>Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.</p>

<p>BRD-K56819078, a Bcl-2 inhibitor, significantly reduces the burden of senescent cells and the mRNA expression of aging-related genes in the kidneys. It exerts its anti-aging effects by inhibiting cell apoptosis (apoptosis).</p>

<p>HR-19011 (Compound 40) is an inducer of eIF2α phosphorylation that increases expression levels of downstream proteins ATF and CHOP,antiproliferative.</p>

<p>TLBC, a borane-chalcone derivative, exhibits dose-dependent inhibitory effects across various glioma cell lines with IC50 values ranging from 5.5 to 25.5 μM. TLBC induces apoptosis independently of alterations in the tumor suppressor factor p53.</p>

<p>Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate, comprised of a cereblon ligand based on Thalidomide and a linker, utilized in the synthesis of PROTACs.</p>

<p>Antiproliferative agent-63 (compound 4d) is a cyclic analog of cannabidiol that acts as an anticancer agent. It demonstrates favorable activity against breast and colorectal cancer. Moreover, this compound can arrest the cell cycle in the G1 phase and induce apoptosis through the mitochondrial pathway in breast cancer cell lines.</p>

<p>Compound 2c is a potent p38α MAPK inhibitor with antitumor effects, enhancing apoptosis and ROS.</p>

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

<p>Nitrovin is an antimicrobial growth promoter that induces ROS-mediated non-apoptotic and quasi-apoptotic cell death by targeting TrxR1. It exhibits anticancer activity with IC50 values ranging from 1.31 to 6.60 μM for both tumor and normal cells.</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>PD-1/PD-L1-IN-30: Cancer research inhibitor with 0.018 μM IC50.</p>

<p>hCAIX/XII-IN-1: potent CAIX inhibitor (KI=0.48μM), CAXII (KI=0.83μM), antiproliferative, induces apoptosis in MCF-7 cells.</p>

<p>PARP/NAMPT-IN-1 (Compound 13j) is a dual-target inhibitor of PARP and NAMPT, with IC50 values of 0.8 nM for PARP1 and 18 nM for NAMPT. It suppresses breast cancer cell proliferation and migration, inducing apoptosis. PARP/NAMPT-IN-1 is applicable for research on triple-negative breast cancer.</p>

<p>SC428 acts as an inhibitor of the androgen receptor (AR), specifically targeting the N-terminal domain of AR. This compound effectively diminishes the transactivation of various AR forms, including AR-V7, ARv567es, full-length AR (AR-FL), and its LBD mutants. Additionally, SC428 significantly inhibits AR-FL nuclear translocation, chromatin binding, and AR-regulated gene transcription under androgen stimulation. In vitro, SC428 suppresses the proliferation of tumor cells. In vivo, it inhibits tumor growth in mice transplanted with 22Rv1 cells by inducing apoptosis.</p>

<p>PARP1-IN-12: potent PARP1 inhibitor, IC50 2.99 nM, triggers cell apoptosis, G2/M arrest, induces DSBs in BRCA-deficient cells.</p>

<p>SIJ1777, a derivative of GNF-7, exhibits potent anticancer effects against melanoma cells harboring BRAFI/II/III mutations. The compound significantly inhibits the activation of MEK, ERK, and AKT. Furthermore, SIJ1777 notably induces apoptosis (cell death) and effectively prevents migration, invasion, and anchorage-independent growth of melanoma cells with BRAFI/II/III mutations.</p>

<p>Antitumor agent-37: strong anti-growth, anti-spread, induces DNA damage, apoptosis via Bcl-2/Bax/caspase3, boosts immune response.</p>

<p>Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.</p>

<p>Compound 12, an anticancer agent, halts G2/M phase, triggers cell death, and activates p53 &amp; PTEN for tumor suppression.</p>

<p>RMS5: hambanine analogue, inhibits P-gp, anti-cancer with cytotoxic, anti-proliferative effects, reduces Bcl-2 proteins, cleaves PARP.</p>

<p>HDAC-IN-34 inhibits HDAC1 (IC50: 0.022 μM) &amp; HDAC6 (IC50: 0.45 μM), binds DNA causing damage, and halts HCT-116 cell growth (IC50: 1.41 μM).</p>

<p>GLI1-IN-1 (CBC-1), a GLI-1 inhibitor, exhibits superior water solubility and anticancer properties. It effectively induces apoptosis and inhibits colorectal cancer growth by targeting the Hedgehog (HH) pathway (IC 50 = 1.3 μM) [1].</p>

<p>ZB-R-55 is an oral and highly potent bimodal RIPK1 inhibitor with excellent kinase selectivity in lps-induced sepsis models for the study of SIRS and sepsis.</p>

<p>c-Myc inhibitor16 iodide (Compound W11) is a selective inhibitor of the c-MycG-quadruplex (c-MycG4). It suppresses the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle by halting growth at the G0/G1 phase, and activates mitochondrial apoptotic pathways, leading to early apoptosis in cancer cells. This compound shows potential for research in breast cancer.</p>

<p>GI-Y2 is a GSDMD inhibitor that suppresses macrophage pyroptosis induced by oxidized low-density lipoprotein (ox-LDL). In vivo, GI-Y2 dose-dependently reduces atherosclerotic plaques and decreases lesion size and fibrosis in the aortic root of ApoE-/- mice. GI-Y2 holds potential for research in pyroptosis and cardiovascular diseases, such as atherosclerosis.</p>

HC-5404-Fu is an inhibitor of PERK with anti-tumor activity. This compound inhibits the signaling pathway of the endoplasmic reticulum stress response. Additionally, HC-5404-Fu increases the sensitivity of renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). It holds potential for research into renal cell carcinoma, stomach cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.

<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>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>GPX4 Activator 2 (Compound C3) serves as an activator of GPX4 and exhibits cardioprotective effects by inhibiting cellular iron death (ferroptosis) with an efficacy concentration (EC50) of 7.8 μM. It is used in the study of myocardial damage.</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>

<p>PF-7006, an Mps1 kinase inhibitor, exhibits a Ki value of 0.27 nM and an IC50 value of 2.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reduces histone H3 levels, and shortens the duration of mitosis, thereby inducing apoptosis (Apoptosis) in cancer cells. When used in combination with Palbociclib, the tolerance of cancer cells to PF-7006 is enhanced. PF-7006 is applicable for research on breast cancer.</p>

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

<p>Mcl-1 inhibitor22 (Example 36) is an MCL-1 inhibitor that suppresses its anti-apoptotic function by blocking the interaction between MCL-1 and pro-apoptotic proteins. It exhibits antiproliferative activity against various cancer cell lines and can be utilized for cancer research.</p>

<p>TNF-α-IN-2 is orally active TNFα inhibitor that distorts the TNFα trimer, causing abnormal signal transduction when it binds to TNFR1, rheumatoid arthritis.</p>

<p>MC3629, an inhibitor of the histone methyltransferase (EZH2), exhibits antitumor activity. This compound effectively inhibits the proliferation and self-renewal of SHH MB cancer cells while inducing cell apoptosis (apoptosis). MC3629 is also useful in research on tumor aggressiveness and resistance.</p>

<p>Decarbamoylmitomycin C, an analog of Mitomycin C (MC), functions as a DNA alkylating agent. It is capable of activating chromatin relaxation by the ataxia-telangiectasia and Rad3-related protein (ATR) in a p53-independent manner.</p>

<p>Coumarin 9a: Selective inhibitor of hCA IX/XII (Ki 93.3/85.7 nM), blocks cancer cell growth, and induces apoptosis.</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>Gallium 8-Hydroxyquinolinate is an inducer of apoptosis that initiates both p53-dependent and independent cell death in cancer cells through the induction of Ca2+ signaling transduction. In addition to its apoptotic properties, this compound's nanostructures exhibit excellent optical performance, making it suitable for use in tumor research.</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>SPI-001 is a selective inhibitor of PPM1D (IC50=0.48 µM) that exhibits anticancer activity. The compound inhibits the phosphatase activity of PPM1D in human breast cancer cells overexpressing PPM1D and enhances the phosphorylation of p53. Additionally, SPI-001 suppresses cell proliferation by inducing apoptosis.</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>TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.</p>

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

<p>TZEP7 functions as an EGFR kinase inhibitor in cancer cells. It exhibits cytotoxicity and induces apoptosis within these cells. TZEP7 downregulates the anti-apoptotic protein Bcl-2, upregulates the pro-apoptotic protein Bax, and increases caspase levels. This compound holds potential for research in anticancer drug development.</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>XSJ05, a derivative of camptothecin (CPT), exhibits anti-cancer activity by inhibiting topoisomerase I (Topo I). This compound induces DNA double-strand breaks, leading to DNA damage. Furthermore, XSJ05 stifles the growth of colorectal cancer (CRC), halts the cell cycle in the G2/M phase, and induces apoptosis.</p>

<p>Nenocorilant (Relacorilant) is an orally active glucocorticoid receptor (GR) antagonist (Ki: 0.15 nM). Nenocorilant can be used to study tumours.</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>GPX4-IN-13 (compound 16), a GPX4 inhibitor, exhibits anticancer properties by diminishing the expression of GPX4, thereby reducing thyroid cell proliferation and inducing ferroptosis. Additionally, this compound effectively inhibits the growth of three distinct thyroid cancer cell lines: N-thy-ori-3-1 (IC 50 =8.39 μM), MDA-T32 (IC 50 =10.28 μM), and MDA-T41 (IC 50 =8.18 μM).</p>

<p>ERK-MYD88 Interaction Inhibitor 1, an agent that disrupts the interaction between ERK and MYD88, has demonstrated the ability to trigger an HRI-mediated integrated stress response (ISR) that specifically promotes immunogenic cell apoptosis (apoptosis) in cancer cells. Additionally, in models using Lewis lung cancer mice, this compound has been shown to stimulate anti-tumor T cell responses, thereby exhibiting significant anti-tumor activity.</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>Top/HDAC-IN-1: Dual Top/HDAC inhibitor, potent against HDAC1-3,6,8 and HCT116 cells; blocks G2 phase, induces apoptosis.</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>Ac-DMLD-CMK is a peptide designed to target the caspase3-Gsdme signaling pathway in mice. It specifically inhibits the activation of caspase 3 and Gsdme, preventing the cleavage of Gsdme by caspase 3, which reduces pyroptosis. This process helps alleviate damage to renal tubular epithelial cells and decrease the secretion of inflammatory cytokines. Ac-DMLD-CMK can lower serum creatinine and blood urea nitrogen levels in mice induced by Cisplatin, thereby mitigating the progression of renal dysfunction. It holds potential for research into chemotherapy-induced nephrotoxicity.</p>

<p>JND4135, a type II TRK inhibitor, exhibits IC50 values targeting TRKA, TRKB, and TRKC at 2.79, 3.19, and 3.01 nM, respectively. It can overcome resistance due to TRKxDFG and other mutations in the BaF3 stable model, inhibiting the phosphorylation of TRKs WT, xDFG mutations, and their downstream signaling molecules. Additionally, JND4135 induces G0/G1 phase arrest and cell apoptosis (apoptosis) in BaF3–CD74-TRKA-G667C cells. This compound also demonstrates antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model by suppressing tumor growth.</p>

<p>PD-L1/HDAC6-IN-1 (Compound HP29) is an inhibitor targeting both PD-L1 and HDAC6, effectively disrupting the PD-L1/PD-1 interaction and inhibiting HDAC6 activity, with IC50 values of 26.8 nM and 69 nM, respectively. This compound enhances the cytotoxicity of Jurkat T cells against HepG2 cells, exhibiting an IC50 of 3.4 μM. In rats, PD-L1/HDAC6-IN-1 demonstrates favorable pharmacokinetics, showing a drug exposure level of 871.62 ng·h/mL, and displays antitumor activity in a B16-F10 xenograft mouse model.</p>

<p>Siphonaxanthin is a carotenoid found in green algae, known for targeting the death receptor 5 (DR5) on cancer cells to induce apoptosis. In human leukemia HL-60 cells, it increases DR5 expression, reduces Bcl-2 levels, and activates caspase-3. It also inhibits fibroblast growth factor receptor-1 (FGFR-1) signaling in endothelial cells. Siphonaxanthin suppresses the proliferation, migration, and tubular formation of human umbilical vein endothelial cells (HUVECs), as well as the growth of microvessels in rat aorta rings. Additionally, it has anti-inflammatory properties by blocking the translocation of high-affinity IgE receptors (FcεRI) to lipid rafts in mast cells. Siphonaxanthin shows potential for research into diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.</p>

<p>Topo II/HDAC-IN-2 (8d) demonstrates remarkable dual inhibitory effects on Topo II and HDAC, and also induces apoptosis [1].</p>

[D-Leu-4]-OB3 suppresses the expression of genes associated with inflammation, proliferation, and metastasis, as well as the expression of PD-L1.

<p>XJTU-L453, a PI3Kα inhibitor, exhibits an IC50 of 0.4 nM. It inhibits the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM respectively. Additionally, XJTU-L453 disrupts the PI3K pathway, leading to cell cycle arrest and cell apoptosis (apoptosis). It also demonstrates antitumor activity in MCF7 xenograft mice.</p>

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

<p>RET-IN-10: Potent RET inhibitor, may treat congenital megacolon and tumors (Patent WO2021135938A1, compound 18).</p>

<p>RIPK1-IN-14 inhibits RIPK1 with 92 nM IC50 and reduces necrotic apoptosis in U937 cells.</p>

<p>Scytonemin, a cyanobacterial pigment, inhibits cancer cell growth by decreasing Plk1 activity, especially effective on U266 myeloma cells.</p>

<p>GA001 is a potent G9a antagonist with an IC50 of 1.32 μM. It can induce autophagy and apoptosis, and is applicable in the treatment of breast cancer.</p>

<p>MG28 exhibits significant cytotoxic effects, likely stemming from its direct and potent DNA-damaging activity. The compound is utilized in cancer research.</p>

<p>YLL545 is an inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2). It inhibits VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling mediators (such as phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). Additionally, YLL545 suppresses HUVEC proliferation, migration, invasion, and angiogenesis. It also induces apoptosis and inhibits tumor growth in a mouse model of breast cancer.</p>

<p>DX3-234 is a OXPHOS inhibitor that acts by inhibiting complex I in the mitochondrial ETC,for cancers dependent on aerobic metabolism, such as pancreatic cancer.</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>

<p>Tubulin-IN-9 inhibits tubulin (IC50: 1.82 μM), halts K562 cells in G2/M, induces apoptosis, and has anti-cancer effects.</p>

<p>WEHI-539 is a selective Bcl-XL inhibitor (IC50: 1.1 nM).</p>

<p>DDO-8958 is an orally active and selective BET BD1 inhibitor, exhibiting a KD of 5.6 nM for BRD4 BD1. It shows low nanomolar inhibitory activity across all BET BD1 bromodomains except for BRDT BD1. DDO-8958 inhibits tumor cell proliferation and migration, induces apoptosis and cell cycle arrest, and demonstrates antitumor activity.</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>(S)-JDQ-443, an isomer of JDQ-443, is a selective, potent oral KRAS G12C inhibitor with antitumor properties.</p>

<p>(S)-Purvalanol B is the S enantiomer of Purvalanol B. Purvalanol B is an inhibitor of cyclin-dependent kinase(CDK) .</p>

<p>Multi-kinase-IN-1, a powerful kinase inhibitor, exhibits antitumor properties by inducing cell apoptosis.</p>

<p>PSF-IN-2 (Compound (C)-30) is a PSF inhibitor with an IC50 value of 0.005 pM. It exhibits anticancer properties, inhibiting the proliferation of 22Rv1 cells with an IC50 value of 0.5 μM. PSF-IN-2 activates the p53 signaling pathway by disrupting PSF-RNA binding, inducing expression of related genes, promoting apoptosis, and inhibiting the cell cycle. This compound is applicable in cancer research.</p>

<p>PKM2 modulator 2 (compound C599) is a potent inhibitor of PKM2, displaying antiproliferative activity and inducing apoptosis. This compound holds potential for research in glioblastoma.</p>

<p>Tubulin polymerization-IN-61 (Compound 9a), a tubulin polymerization inhibitor, disrupts the microtubule skeleton, arrests the cell cycle at the G2/M phase, induces Apoptosis, and impedes cancer cell migration and colony formation. This compound demonstrates antitumor efficacy in vivo within the 4T1 xenograft model [1].</p>

<p>Kahweol Acetate, a semi-synthetic coffee bean derivative, inhibits osteoclasts, cancer cells, DNA damage, and oxidative stress.</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>