Apoptose

<p>A signal-specific JNK/p38 pathway and TAK 1 inhibitor</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>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>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>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>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>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>Casuarinin, an ellagitannin found in pomegranates and certain Casuarina/Stachyurus plants, is a carbonic anhydrase inhibitor and astringent.</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>GPD-1116 is an orally active inhibitor of phosphodiesterase (PDE)4 and PDE1. The compound effectively reduces smoke-induced apoptosis in lung cells. Additionally, GPD-1116 has shown efficacy in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary arterial hypertension.</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>DL-Buthionine-(S,R)-sulfoximine hydrochloride (Buthionine sulfoximine hydrochloride) is a potent and specific glutamylcysteine synthetase biosynthesis inhibitor</p>

<p>CP-31398 stabilizes the active conformation of p53 in cancer cells with either mutated or wild-type p53, enhancing its activity. Additionally, CP-31398 upregulates target genes of p53 such as p21WAF1/Cip1 and KILLER/DR5. This compound possesses tumor-suppressive properties.</p>

<p>MG-B-28, a BTLA-HVEM inhibitor, demonstrates an IC50 value of 906 nM. It promotes T cell activation dose-dependently by inhibiting the interaction between BTLA and HVEM.</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>Tubulin/NRP1-IN-1 (compound TN-2) serves as a dual inhibitor targeting both Tubulin and NRP1, exhibiting IC50 values of 0.71 μM and 0.85 μM, respectively. This compound notably reduces the viability of prostate tumor cell lines and triggers apoptosis [1].</p>

<p>BHA536 is an orally effective inhibitor of PKCα/β and the NF-kB signaling pathway. This compound inhibits the proliferation of ABC DLBCL cells harboring CD79 mutations by causing cell cycle arrest in the G1 phase and induces apoptosis in TMD8 cells. Additionally, BHA536 exhibits antitumor activity in mice.</p>

<p>Z-VAD is an irreversible pan-caspase inhibitor, suppressing multiple caspases including caspase-3, -6, -7, -8, and -9. Z-VAD induces autophagy in tumour cells.</p>

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

<p>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>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>AQIM-I is a survivin inhibitor that reduces survivin expression and colony formation. It promotes reactive oxygen species (ROS) production, apoptosis, cell cycle arrest, DNA damage, and autophagy. Moreover, AQIM-I effectively inhibits nonsmall cell lung cancer cells A549, with an IC 50 value of 9 nM [1].</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>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>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>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>Fluvastatin (XU 62-320) sodium monohydrate, a fully synthetic competitive HMG-CoA reductase inhibitor, features an IC 50 of 8 nM. This compound also safeguards vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway [1] [2].</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>KDM1/CDK1-IN-1 inhibits KDM1 (IC50: 0.096 μM) &amp; CDK1 (IC50: 0.078 μM), blocks HOP-92 G2/M phase, induces apoptosis, toxic to cancer cells.</p>

<p>JAK2/FLT3-IN-1 (TFA), an oral JAK2/FLT3 inhibitor, shows anticancer properties; IC50: JAK2 (0.7 nM), FLT3 (4 nM), JAK1 (26 nM), JAK3 (39 nM).</p>

<p>Antitumor agent-43 (Compound 4B) is a potent antitumor agent that induces cell cycle arrest at G2/M phase.</p>

<p>Compound 14 is a peptidomimetic that significantly lowers TNFα, NO, CD40, and CD86, showcasing strong anti-inflammatory effects.</p>

<p>SphK1-IN-2: SphK1 inhibitor, IC50: 19.81 nM; less effective on SphK2. Induces apoptosis, hinders cancer cell growth.</p>

<p>QTX125 TFA: Potent, selective HDAC6 inhibitor with antitumor effects.</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>Anticancer agent 46, potent and selective, induces apoptosis, is cytotoxic to cancer cells, with low toxicity to human lymphocytes.</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>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>LSD1-IN-21: potent LSD1 inhibitor, crosses blood-brain barrier, IC50 of 0.956 μM; lowers TNF-α, anti-cancer, anti-inflammatory.</p>

<p>EGFR/HER2-IN-6 is a dual inhibitor of EGFR, HER2, and DHFR with IC50s: 0.122, 0.078, and 0.585 μM, showing anticancer potential and selectivity.</p>

<p>4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.</p>

<p>ADH-6, a tripyridylamide, disrupts mutant p53 aggregates in cancer cells, reviving its function and inducing apoptosis.</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>RMS5: hambanine analogue, inhibits P-gp, anti-cancer with cytotoxic, anti-proliferative effects, reduces Bcl-2 proteins, cleaves PARP.</p>

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

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

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

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

<p>eIF4A3-IN-4 is a novel inhibitor of eIF4A (IC50: 8.6 μM).</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>NA-17 is a naphthalimide compound with antitumor activity and exhibits lower toxicity to normal cells such as HL-7702 and WI-38. It demonstrates p53-dependent inhibition selectivity in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of these cells. NA-17 causes cell cycle arrest in the G1 phase and promotes apoptosis and cell death.</p>

<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>

<p>Minnelide is a prodrug of triptolide,and shows potent antitumor activity in a number of tumor types.</p>

<p>AQX-435 activates SHIP1, inhibits PI3K in BCR signaling, induces apoptosis in B cells, and slows lymphoma growth.</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>vacuolar H+-ATPases (V-ATPases) inhibitor</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>SILA-123, an inhibitor of FLT3 (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM), induces cell apoptosis by hindering the cell cycle progression at the G0/G1 phase through the suppression of FLT3 phosphorylation and its downstream signaling pathways. This compound is utilized in the study of acute myeloid leukemia.</p>

<p>Flonoltinib maleate is an orally active dual inhibitor of JAK2/FLT3, with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. It exhibits anticancer properties.</p>

<p>Antiproliferative agent-4 suppresses cancer cell growth with low toxicity, inhibits tumors in mice, and induces apoptosis in EC109 cells.</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>Thalidomide-NH-amido-PEG2-C2-NH2 is a synthetic E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker. It is utilized in the synthesis of PROTACs.</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>Samuraciclib (CT7001) is a potent oral CDK7 inhibitor (IC50: 41 nM) with anti-breast cancer properties.</p>

<p>mTOR/HDAC6-IN-1 inhibits HDAC6 (IC50: 56 nM) &amp; mTOR (IC50: 133.7 nM), may treat TNBC by inducing autophagy and apoptosis.</p>

<p>Flizasertib is a serine/threonine kinase inhibitor that acts by inhibiting RIPK1, which has anti-inflammatory and therapeutic effects on immune disorders.</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>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>KIRA9 inhibits IRE1 with a 4.8 μM IC50, blocking ER-stress-induced mRNA decay and apoptosis by fully binding IRE1's ATP site.</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>Claturafenib is a brain-permeable, selective, all-mutant BRAF inhibitor.PF-07799933 has shown antitumor activity, used in combination with MEK inhibitors.</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-44: potent EGFR kinase inhibitor, orally active, IC50 4.11 nM, 33.57% bioavailability, induces apoptosis, for lung cancer study.</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>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>eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.</p>

<p>(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) sodium is a synthetic derivative of oleic acid (OA) that binds to the plasma membrane, altering lipid composition. This compound exhibits antitumor properties.</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>HER2-IN-11 is a psoralen derivative that induces apoptosis. HER2-IN-11 shows light-activated cytotoxicity and also exhibits anti-breast cancer activity [1].</p>

<p>SMO-IN-5 (Compound 25(B31)) is an effective inhibitor of smoothened (SMO), which suppresses the Hedgehog (Hh) signaling pathway. This compound inhibits cellular proliferation and induces apoptosis, demonstrating antitumor activity.</p>

<p>EGFR/VEGFR2-IN-3 (compound 9) is an effective inhibitor of EGFR and VEGFR-2, demonstrating IC50 values of 0.129 µM for EGFR, 0.142 µM for VEGFR-2, and 3.428 µM for COX-2. This compound exhibits cytotoxic properties and induces cell apoptosis (apoptosis) as well as cell cycle arrest at the G2/M phase.</p>

<p>GLS1 Inhibitor-6: IC50=68nM, 220x more selective for GLS2, has anti-tumor and pro-apoptosis effects.</p>

<p>CK156 inhibits DAPK with high selectivity; IC50: 182 nM (DRAK1), 34 μM (CK2a1), 39 μM (CK2a2); key in autoimmune/inflammation research.</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>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>Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value</p>

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

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

<p>DC-U4106: USP8 inhibitor, Kd 4.7μM, IC50 1.2μM, degrades Erα, low-toxicity tumor suppressor for breast cancer research.</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>HER2-IN-10 is a psoralen derivative that induces apoptosis. HER2-IN-10 shows anti-breast cancer activity and light-activated cytotoxicity [1].</p>

<p>Tubulin polymerization-IN-4: inhibits tubulin (IC50=4.6 μM), blocks G2/M phase, induces apoptosis, hinders cell cloning/migration, damages vasculature.</p>

<p>Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2/M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [1].</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>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>Anticancer agent 64 (5m) induces apoptosis, has IC50 2.4μM in CCRF-CEM, activates caspases, cleaves PARP, affects mitochondria.</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>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>Topoisomerase I/II inhibitor 4 halts cell growth and spread, induces apoptosis, and is used in liver cancer research.</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>PD-1/PD-L1-IN-17 (Compound P20) is a potent PD-1/PD-L1 inhibitor (IC50: 26.8 nM).</p>

<p>NSD2-IN-1: potent, selective NSD2-PWWP1 inhibitor, IC50 0.11 μM, induces gene expression changes, apoptosis, cell cycle arrest.</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>