Apoptosis

<p>Apoptosis Inducer 5, a lignan enantiomer extracted from Crataegus pinnatifida, demonstrates cytotoxic properties through inducing apoptosis and autophagy in</p>

<p>GGTI-2154 hydrochloride: selective GGTase I inhibitor, IC50 21 nM, used in cancer research.</p>

<p>NVP-CGM097 sulfate is a potent and selective inhibitor of MDM2 (hMDM2, IC50 of 1.7±0.1 nM).</p>

<p>MA242 free base is a dual MDM2/NFAT1 inhibitor that triggers apoptosis in pancreatic cancer cells.</p>

<p>PD-L1/HDAC-IN-1 (Compound 14) is an inhibitor of PD-L1 and HDAC, effectively blocking PD-1/PD-L1 interaction as well as HDAC2 and HDAC3 with IC50 values of 88.10, 27.98, and 14.47 nM, respectively. It exhibits mild cytotoxicity in MCF-7 cells (IC50=19.34 μM) and enhances the expression of PD-L1 and CXCL10, promoting antitumor immune responses by recruiting T cell infiltration into the tumor microenvironment (TME).</p>

<p>Autophagyinducer 7 (Compound SSA) serves as an inducer of autophagy (Autophagy) and apoptosis (Apoptosis). It stimulates autophagy by inhibiting Akt/mTOR signaling and the expression of downstream proteins. Additionally, Autophagyinducer 7 suppresses DNA synthesis and causes G0-G1 cell cycle arrest, ultimately inhibiting the growth of tumor cells.</p>

<p>AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.</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>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>Anticancer agent 14: a potent breast cancer inhibitor; induces cell death, disrupts mito. membrane potential (IC50: 0.20-0.65 μM).</p>

<p>BTK-IN-7 is a potent inhibitor for BTK with 4.0 nM IC50, highly selective over ITK and EGFR, showing strong antitumor activity.</p>

<p>EGFR-IN-62: IC50 of 10-242 nM for various EGFR mutations, blocks A549/H1975 cell cycle, induces apoptosis, and inhibits cell motility and proliferation.</p>

<p>Silvestrol is a eukaryotic translation initiation factor 4A inhibitor. Silvestrol causes autophagy and caspase-mediated apoptosis.</p>

<p>TP-030-2 is a RIPK1 inhibitor (human K i =0.43 nM ; mouse IC 50 =100 nM) .</p>

<p>Microtubule stabilizer; halts cancer cell growth (IC50: 3-30 nM); arrests cells in prometaphase; prevents bipolar spindle formation.</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>CDK-IN-9: A potent CDK inhibitor, gels to enhance CDK12/DDB1 binding, targets CDK2/E (IC50: 4 nM), induces apoptosis via dephosphorylation.</p>

<p>MRK003, a γ-secretase inhibitor, induces apoptosis, halts cell growth in myeloma/NHL, and affects notch signaling and PI3K/Akt pathway.</p>

<p>OICR12694 (JNJ-65234637) is an orally active inhibitor of B cell lymphoma 6 (BCL6) .</p>

<p>NF-κB-IN-4 (compound 17) is a potent inhibitor of NF-κB pathway which can cross blood brain barrier (BBB).</p>

<p>Anticancer agent 64 (5m) induces apoptosis, has IC50 2.4μM in CCRF-CEM, activates caspases, cleaves PARP, affects mitochondria.</p>

<p>Microtubulin-IN-1 (Compound 8g) is an inhibitor of microtubulin, targeting the colchicine-binding site to disrupt tubulin integrity and induce upregulation of p53 protein expression. It exhibits antiproliferative activity across various cancer cell lines, including NCI-H460, BxPC-3, and HT-29, with IC50 values of 2.4, 1.6, and 2.07 nM, respectively. Additionally, Microtubulin-IN-1 induces cell cycle arrest at the G2/M phase and apoptosis in NCI-H460 cells.</p>

<p>IMB5046 is a microtubule inhibitor that induces apoptosis (cell death) by obstructing the G2/M phase of the cell cycle. It possesses antitumor properties.</p>

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

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

<p>Ketorolac (RS37619) hydrochloride is a nonsteroidal anti-inflammatory drug and a non-selective COX inhibitor, exhibiting IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This compound is utilized in a 0.5% ophthalmic solution format for the investigation of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and post-operative ocular inflammation pain. Additionally, Ketorolac hydrochloride serves as a DDX3 inhibitor, making it pertinent for research in cancer therapies.</p>

<p>Cetzole (Compound 1) acts as an inducer of ferroptosis (iron-dependent cell death) through the accumulation of ROS, leading to cell death. The compound exhibits varying half-maximal cytotoxic concentrations (CC50) against several cell lines: 2.56 μM in NCI-H522, 10.31 μM in NCI-H522 GFP-SCL7A11 #8, 2.71 μM in NCI-H522 RV-GFP, 3.07 μM in HT-1080, 14.9 μM in NARF2, and 6.28 μM in MDA-MB-231. This highlights Cetzole's potential for research in cancer therapeutics.</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>

<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>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>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>HP590: potent oral STAT3 inhibitor, IC50=27.8 nM, blocks ATP, IC50=24.7 nM, hinders gastric cancer growth, triggers cell death.</p>

<p>MNK1/2-IN-6: Strong, selective MNK1/2 inhibitor; IC50s: MNK1 at 2.3 nM, MNK2 at 3.4 nM; triggers dose-dependent apoptosis.</p>

<p>Antiproliferative agent-4 suppresses cancer cell growth with low toxicity, inhibits tumors in mice, and induces apoptosis in EC109 cells.</p>

<p>PF-3837 is an inhibitor of the Mps1 kinase, with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, thereby reducing genomic stability and leading to cancer cell apoptosis (Apoptosis). PF-3837 is utilized in the study of breast cancer.</p>

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

<p>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>ONC213, an αKGDH inhibitor, functions by hindering αKGDH activity, thus suppressing mitochondrial respiration and elevating α-ketoglutarate levels, ultimately inducing apoptosis (Apoptosis) in AML cells. It is utilized in the study of acute myeloid leukemia.</p>

<p>GNE684 inhibits RIP1; Ki app: 21 nM (human), 189 nM (mouse), 691 nM (rat).</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>p53-MDM2-IN-6, an LSM-83177 hydrazone analog, acts as an efficacious p53-MDM2 inhibitor with an IC50 of 11.08 µg/mL. This compound inhibits the p53-MDM2 interaction leading to an increase in p-53 levels while concurrently decreasing GST enzyme expression. It halts the cell cycle at the S phase and induces early and late apoptosis (Apoptosis), exhibiting antiproliferative activity against the HT29 cell line with an IC50 of 10.44 µg/mL. p53-MDM2-IN-6 holds promise for research in colorectal cancer.</p>

<p>Mps-BAY1, an MPS1 inhibitor, exhibits anticancer activity. It inhibits cell proliferation and induces cell apoptosis by activating mitotic aberrations in cancer cells, leading to overall aneuploidy and polyploidy. Mps-BAY1 is used in research pertaining to colorectal and cervical cancer.</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>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>D18: Dual agonist for TLR7/8, boosts PD-L1, aids tumor sensitivity to PD-1/PD-L1 inhibitors, and is a cytotoxin for ADC HE-S2.</p>

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

<p>RET-IN-1 is a RET kinase inhibitor (IC50s: 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively).</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>HDAC-IN-37 inhibits HDACs 1, 3, 8, &amp; 6, induces histone acetylation, halts G1 to S phase, and triggers early apoptosis.</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>APD-94 is a dual inhibitor targeting tubulin and Bmi-1. It disrupts the normal polymerization of tubulin and suppresses the expression of Bmi-1. This compound induces cell cycle arrest at the G2/M phase and triggers apoptosis, thereby inhibiting cancer cell proliferation. Additionally, APD-94 inhibits the growth of HT29 cell xenograft tumors in NOD/SCID mice and is applicable to colorectal cancer research.</p>

<p>DAPK1-IN-1 (compound 10) is an inhibitor of Death-associated protein kinase 1 (DAPK1), with a dissociation constant (Kd) of 0.63 μM. It is utilized in the study of Alzheimer's disease.</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>Tubulin-IN-9 inhibits tubulin (IC50: 1.82 μM), halts K562 cells in G2/M, induces apoptosis, and has anti-cancer effects.</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>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>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>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>PLK1-IN-13 is a selective, orally active PLK1 inhibitor with an IC50 of 0.27 nM. It also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 induces cell cycle arrest at the G2 phase, promotes apoptosis, and downregulates the transcription of the cancer-associated oncogene c-MYC. This compound inhibits tumor growth and is applicable for research in acute myeloid leukemia (AML).</p>

<p>HSP90-IN-10 is a potent HSP90 inhibitor, targeting HCC1954 cells (IC50: 6 μM) and inducing apoptosis, sparing normal cells.</p>

<p>Compound 3b inhibits tubulin polymerization, IC50 12.38 µM, with anticancer properties and promotes cell apoptosis.</p>

<p>Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.</p>

<p>Cernuumolide J (TMJ-105) functions as a JAK2/STAT3 inhibitor and exhibits potent activity against HEL leukemia cells by inhibiting their growth in both time-dependent and concentration-dependent manners, with an IC 50 value of 1.79 μM. This compound effectively induces G2/M phase arrest and apoptosis by downregulating the phosphorylation of JAK2, STAT3, and Erk, while simultaneously upregulating the phosphorylation of JNK and p38 MAPK. Cernuumolide J holds potential for research applications in anti-cancer therapy.</p>

<p>FLT3/TrKA-IN-1: Potent dual kinase inhibitor for FLT3 &amp; TrKA, promising for AML research.</p>

<p>Tubulin inhibitor 13 (E27), IC50 16.1 μM, blocks tubulin polymerization, cancer cell migration, and invasion, induces apoptosis.</p>

<p>QTX125 TFA: Potent, selective HDAC6 inhibitor with antitumor effects.</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>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>VEGFR-IN-3 inhibits cancer cell growth (OVCAR-4, MDA-MB-468) with IC50s: 0.29, 0.35μM. Used in cancer research.</p>

<p>JAK-2-/3-IN-3 (ST4j) is a potent JAK2/3 inhibitor for leukemia research, with IC50s: JAK2, 13 nM; JAK3, 14.86 nM; induces apoptosis.</p>

<p>Compound 3 (DOR agonist 2) acts as a Delta Opioid Receptor agonist. It inhibits the expression of TNF-α, obstructs NF-κB transportation to the nucleus, and activates the G protein-mediated ERK1/2 pathway. This compound is useful for research into neurodegenerative diseases.</p>

<p>GRP78-IN-1 binds to GRP78 protein, inhibits cell growth, and triggers apoptosis in breast cancer; has -8.07 kcal/mol binding energy.</p>

<p>EGFR-IN-47: strong oral EGFRL858R/T790M/C797S blocker, induces cell death; promising for NSCLC research. IC50: 0.01 μM.</p>

<p>HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.</p>

<p>Compound 5f, a potent tubulin polymerization inhibitor (IC50 = 1.09 μM), blocks cell migration, tube formation, and has anti-angiogenic effects.</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>(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>Ferrostatin-1 diyne (Fer-1 diyne) (compound 2) serves as an inhibitor of ferroptosis, accumulating in cellular lysosomes, mitochondria, and the endoplasmic reticulum. It notably inhibits ferroptosis independently of lysosomal and mitochondrial activity.</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>Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.</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>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>ZSH-512 is a potent inhibitor of RARγ with antiproliferative properties. It induces apoptosis and reduces the expression of CD133, NANOG, SOX2, and EPCAM proteins. ZSH-512 exhibits anticancer activity and shows potential for colorectal cancer research.</p>

<p>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>HBV/HDV-IN-2 (Compd 143) functions as an inhibitor for HBV, HDV, and PD-1/PD-L1, demonstrating an EC 50 of 35 nM in T cell activation.</p>

<p>TNF-α-IN-14, a potent TNFα inhibitor, exhibits a selective inhibition profile with an IC50 of 1.1 µM and demonstrates antiinflammatory properties (WO2001072735A2; compound 12) [1].</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>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>VEGFR-2-IN-18 is a potent VEGFR-2 inhibitor with a 60 nM IC50, promoting cell apoptosis and anticancer effects.</p>

<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>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>

<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>N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride (TLCK hydrochloride) is an irreversible serine protease inhibitor that functions by alkylating the histidine residue at the active site, thus inhibiting trypsin and trypsin-like proteases. It effectively inhibits caspase-3, caspase-6, and caspase-7 with IC50 values of 12.0, 54.5, and 19.3 μM, respectively. Additionally, N-a-Tosyl-L-lysinyl-chloromethylketone hydrochloride induces apoptosis in HL-60 cells and prevents the reduction of mitochondrial transmembrane potential during the apoptosis process.</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>Bcl-2-IN-6 suppresses Bcl-2, upregulates p53/Bax/caspase-7, arrests cell cycle, and induces MCF-7 apoptosis; IC50s: MCF-7 20.91 μM, others &lt;48 μM.</p>

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

<p>HDAC1-IN-5 inhibits HDAC1 (IC50=15 nM) &amp; HDAC6 (IC50=20 nM), promotes apoptosis, damages chromatin, and reduces tumor growth in mice.</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>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>TBC-1 is a chlorophyll-a derivative that acts as a photosensitizer for photodynamic therapy (PDT). It efficiently generates type I ROS and targets the endoplasmic reticulum. TBC-1 demonstrates in vitro biocompatibility and PDT effectiveness under both normoxic and hypoxic conditions.</p>

<p>Autophagy-IN-1 blocks autophagy in cancer cells, hinders tumor growth in mice, and aids in studying colorectal cancer.</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>ZLWT-37: Oral CDK inhibitor, CDK9 IC50=0.002 µM, CDK2 IC50=0.054 µM; halts HCT116 cells at G2/M, induces apoptosis.</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>