Apoptose

<p>SRE-II, an amide derivative, serves as an activatable photosensitizer tailored for photodynamic cancer research, exhibiting diminished fluorescence and</p>

<p>FLT3/HDAC-IN-1 is a dual inhibitor targeting FLT3 and HDAC, with IC50 values of 30.4 nM for FLT3 and 52.4, 14.7 nM for HDAC1/3, respectively. It induces apoptosis in MV-4-11 cells and exhibits antiproliferative effects against BaF3 cells transformed by FLT3 mutations. FLT3/HDAC-IN-1 is useful for research on refractory solid tumors and hematological malignancies.</p>

<p>PTP1B-IN-30 (Compound 3j) is an inhibitor of PTP1B with an IC50 of 0.51 µM. It suppresses the proliferation of T47D cancer cells with an IC50 of 21.21 µM, induces cell cycle arrest at the S phase, and triggers apoptosis in T47D cells.</p>

<p>Fuscin, a quinonoid from O. fuscum, inhibits ADP/ATP translocase, depletes glutathione, disrupts NADH oxidation, and blocks MIP-1α/CCR5 binding (IC50: 21µM).</p>

<p>TV 3279 is a ChE-MAI inhibitor with neuroprotection via anti-apoptotic protein induction and blocks pro-apoptotic enzymes in cells.</p>

<p>VEGFR-2-IN-53 (Compound 15w) is an inhibitor of VEGFR-2 with an IC50 value of 4.34 μM. It induces cell apoptosis (Apoptosis) and inhibits angiogenesis by blocking VEGFR-2 activity and preventing cell migration. Additionally, it shows an IC50 of 3.87 μM in inhibiting the growth of MCF-7 cells, making it pertinent for research in cancer therapeutics.</p>

<p>Aspidin BB, a phloroglucinol from Dryopteris, inhibits cancer by causing cell cycle arrest and apoptosis in HO-8910 cells.</p>

<p>SDH-IN-26 (Compound C3) is a succinate dehydrogenase (SDH) inhibitor with significant inhibitory activity against various plant pathogenic fungi, including solanrhizoctonia and Botrytis cinerea. It exhibits an EC50 value of 0.270 μg/mL against solanrhizoctonia. SDH-IN-26 compromises fungal cell membrane integrity, increases membrane permeability, disrupts cell structure, reduces mitochondrial count, and affects normal hyphal growth. It also decreases mitochondrial membrane potential, inducing apoptosis. SDH-IN-26 holds potential for studying plant diseases caused by fungi.</p>

<p>RIP1 kinase inhibitor 9 (compound SY-1) is a selective inhibitor of RIP kinase. It effectively reduces central inflammatory responses caused by seizures. RIP1 kinase inhibitor 9 also obstructs Z-VAD-FMK-induced necroptosis in HT-29 cells, with an EC50 of 7.04 nM.</p>

<p>CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.</p>

<p>Garivulimab (BGB-A333), a humanized IgG1 monoclonal antibody, binds to PD-L1, blocking PD-1 interaction and exhibiting antitumor activity.</p>

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

Bornyl acetate (Isobornyl acetate) has an anti-inflammatory effect. It is the volatile ingredient in some Chinese traditional herbs and numerous conifer oils.

<p>HDSI-18 is an orally active selective inhibitor of HDAC6 with an IC50 of 1.6 nM. It exhibits cytotoxic effects against K562, MV4-11, MOLM-13, THP-1, and Jurkat cells with IC50 values of 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively. HDSI-18 can activate Caspase-3, induce mitochondrial depolarization, and trigger apoptosis (Apoptosis), demonstrating antitumor activity.</p>

<p>Lisaftoclax, an oral Bcl-2/Bcl-xl inhibitor (IC50: 2 nM &amp; 5.9 nM), treats CLL by promoting leukemia cell death.</p>

<p>HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.</p>

<p>Anti-Mouse TNF alpha Antibody is a rat-derived IgG inhibitor targeting mouse TNF alpha.</p>

<p>Thalidomide-O-C8-NH2 is a synthetic cereblon ligand &amp; PROTAC linker, serving as an E3 ligase ligand-linker.</p>

<p>Anticancer agent 130 (compound 8d) significantly induces apoptosis in A549 cells [1].</p>

<p>GDCNF-11, an HSP90-based HIM-PROTACGPX4 degrader, facilitates the ubiquitination and degradation of GPX4 through the HSP90 chaperone complex. This reduction in endogenous GPX4 induces ferroptosis in HT-1080 cells, with a DC50 value of 0.08 μM.</p>

<p>"Antitumor agent-96 (Compound D34) is a potent MRE11 inhibitor that down-regulates the homologous recombination (HR) pathway by binding to and suppressing the</p>

<p>Ferroptosisinducer 6 (6d) is an inducer of ferroptosis (ferroptosis) that exhibits potent potential for Type I/II photodynamic therapy by inducing ROS production, oxidative stress, and mitochondrial damage. Additionally, it demonstrates antitumor activity.</p>

<p>Apoptosisinducer 33 (compound H2) is a hydrazone derivative. It exhibits antioxidant and antimicrobial properties, capable of inhibiting the growth of Staphylococcus aureus, Escherichia coli, and Candida albicans. Additionally, Apoptosisinducer 33 can suppress tumor cell proliferation and induce apoptosis (apoptosis), making it useful for tumor research.</p>

<p>TS-24 is a cysteine protease histone S (CTSS) inhibitor that promotes BRCA1-mediated apoptosis.</p>

<p>PAA5, a polynuclear Au(I) cluster, triggers ferroptosis and has anticancer effects by increasing pH2AX over time.</p>

<p>F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.</p>

<p>FR900359 is a macrocyclic Gq protein inhibitor that inhibits melanoma cell proliferation and can be used to study asthma, inflammation and cancer.</p>

<p>GPX4-IN-7 (Compound 31), an indirubin derivative, serves as a ferroptosis inducer in colon cancer treatment.</p>

<p>Ferumoxytol is an iron oxide nanoparticle with anti-leukemia properties, specifically against acute myeloid leukemia (AML) cells with low ferroportin (FPN) expression. By increasing intracellular iron levels, Ferumoxytol induces the Fenton reaction to produce reactive oxygen species (ROS), resulting in oxidative stress and ferroptosis. It selectively kills leukemia cells with low FPN expression while sparing normal cells, making it useful for studying leukemia targeting iron metabolism abnormalities.</p>

<p>FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.</p>

<p>MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.</p>

Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .

<p>Moflerafusp alfa is a fusion protein that targets the human signal-regulatory protein alpha (SIRPα) variant V2 D1 domain and human programmed death-ligand 1 (PD-L1). It shows potential for research in various cancer treatments.</p>

<p>PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC) and an Mcl-1 inhibitor, useful in cancer research.</p>

<p>EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. It effectively suppresses the proliferation of various lung cancer cells, with IC50 values of 11.7, 5.19, 7.32, and 1.53 μM for NCI-H1781, HCC827, NCI-H3255, and NCI-H1975, respectively. Additionally, EGFR-IN-151 hinders colony formation and cell migration in H1975, induces G1 phase cell cycle arrest, and triggers apoptosis in H1975 cells.</p>

<p>USP7-IN-9 is a potent USP7 inhibitor (IC50 = 40.8 nM), induces apoptosis, arrests RS4;11 cells, and modulates key oncoproteins.</p>

<p>Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex.</p>

<p>Antitumor Photosensitizer-4 (compound 10b), a conjugate of dasatinib and imatinib, serves as a potent tyrosine kinase inhibitor (TKI) targeting ABCG2.</p>

<p>Apoptosis inducer37 (Derivative 10) is an agent that induces apoptosis and exhibits anticancer properties by causing cell cycle arrest at the S-G2/M phase and promoting cell apoptosis. It significantly inhibits HCT116, SKOV3, and HepG2 cancer cells with IC50 values of 24.98 μM, 26.15 μM, and 23.09 μM, respectively. Apoptosis inducer37 demonstrates antitumor activity and can be utilized in ovarian cancer research.</p>

<p>d-(KLAKLAK)2 is an antimicrobial and antitumor peptide, notable within the group of antimicrobial peptides, and exhibits strong anticancer properties. It kills bacteria by disrupting their cell membranes, causing leakage of cell contents. Additionally, d-(KLAKLAK)2 inhibits tumor cell proliferation by inducing apoptosis through mitochondrial swelling and membrane damage.</p>

<p>Maceneolignan A, a natural product isolated from the aril of Myristica fragrans (Myristicaceae), inhibits β-hexosaminidase release in RBL-2H3 cells, exhibiting</p>

<p>Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].</p>

<p>Volrustomig is a bi-engineered fragment crystallizable (Fc) domain, a monovalent bispecific IgG1 monoclonal antibody targeting the key immune checkpoint receptors PD-1 and CTLA-4. It boosts T-cell activation and antitumor immunity, making it a promising immunotherapy for various cancers. Molecular weight: 146.77 kDa.</p>

<p>Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.</p>

<p>N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP</p>

<p>Conglobatin is a natural product for research related to life sciences. The catalog number is T36494 and the CAS number is 72263-05-9.</p>

<p>Oligomycin B is an antibiotic isolated from marine Streptomyces, is an eukaryotic ATP synthase inhibitor, induces apoptosis.</p>

<p>MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP.</p>

<p>JNK-1-IN-3 (Compound 9e) downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity.</p>

<p>BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)</p>

<p>PROTACPD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with significant PD-L1 protein degradation capacity. It demonstrates strong PD-L1 degradation activity in 4T1 cells, with a DC50 of 0.609 μM. This compound is applicable to breast cancer research.</p>

<p>QZ2135 (compound 20) is a PROTAC degrader that specifically targets RET and exhibits antitumor activity in vivo within a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The compound demonstrates degradation activity with DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C) when targeting KIF5B-RET. QZ2135 is composed of the target protein ligand (red part) RETligand-3, the E3 ligase ligand (blue part) Lenalidomide-F, and the PROTAC Linker (black part) 7-Iodohept-1-yne, wherein the target protein ligand combined with the linker forms the conjugate RETLigand-Linker Conjugate-1.</p>

<p>Human PD-L1 inhibitor III is a human PD-L1 inhibitor.</p>

<p>PBE-AMF is a prodrug that activates H2O2 and exhibits anticancer activity. It impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing cell death (apoptosis), and blocking the cell cycle. PBE-AMF effectively and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells.</p>

<p>KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.</p>

<p>CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).</p>

<p>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>ChoKα Inhibitor-5, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoKα1 with an IC50 value of 0.64 μM and induces apoptosis.</p>

<p>Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].</p>

<p>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

<p>Thalidomide-PEG conjugate for E3 ligase in PROTACs; has cereblon ligand and 3-unit PEG linker.</p>

<p>TNF-α (31-45), human is a peptide of tumor necrosis factor-α.</p>

<p>ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.</p>

<p>Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin &gt; R837 [1].</p>

<p>TRAP1-IN-1 is a selective TRAP1 inhibitor, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.</p>

<p>YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.</p>

<p>Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.</p>

<p>Targaprimir-96 TFA is a selective inhibitor of miR-96 in cancer, inducing apoptosis with high affinity for pri-miR-96 but not affecting healthy cells.</p>

<p>Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium-labeled form of Oxybenzone. Commonly used as a UV filter in tanning and skin protection products, Oxybenzone (Benzophenone 3) acts as an endocrine-disrupting chemical (EDC) that can cross both the placental and blood-brain barriers. It impairs autophagy, alters epigenetic states, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.</p>

<p>Tengonermin (ARENEGYR), a vascular agent, is TNF-α fused with CNGRCG peptide, enhancing chemo and T-cell access in tumors.</p>

<p>PD-L1inhibitory peptide is an inhibitor peptide that targets the programmed cell death ligand 1 (PD-L1). By binding to PD-L1, it lifts immune suppression and restores the anti-tumor activity of T cells. PD-L1inhibitory peptide holds promise for use in tumor research.</p>

<p>β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer employed in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-</p>

<p>Thalidomide-NH-C8-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand and a specific linker.</p>

<p>S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.</p>

<p>IRF1-IN-2 is a small molecule IRF1 inhibitor that suppresses pyroptosis, protecting against radiation-induced skin damage.</p>

<p>Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.</p>

<p>Sincalide ammonium, a CCK analog, stimulates bile release, gallbladder contraction, and sphincter relaxation, aiding in diagnoses.</p>

<p>Akt/NF-κB/MAPK-IN-1 (compound 2m) serves as a potent, orally active inhibitor targeting NO with an IC50 of 7.70 μM and demonstrates low toxicity.</p>

<p>BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3, and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM, and 0.009 μM, respectively. It also inhibits the phosphorylation of MEK1/2 and ERK1/2. Additionally, BRAFV600E/JNK-IN-1 suppresses tumor cell proliferation, NO release, and PGE2 production, exhibiting both antitumor and anti-inflammatory activities.</p>

<p>Tubulin/AKT1-IN-1 (Compound D1-1) serves as an inhibitor of both tubulin polymerization and AKT pathway activation, effectively suppressing proliferation and</p>

<p>Ac-LEVD-CHO, a caspase-4 inhibitor, is a peptide with the sequence Ac-Leu-Glu-Val-Asp-al [1].</p>

<p>Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.</p>

<p>Ferroptosis-IN-12 (Cpd-A1) is an inhibitor of ferroptosis. It effectively suppresses ferroptosis in mouse renal tubular epithelial cells (mTECs) treated with Erastin and improves renal function in dose-dependent manners in mouse models of acute kidney injury (AKI) induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). This compound also reduces renal tubular damage and eliminates inflammation. Exhibiting good plasma stability and high distribution in renal tissues during pharmacokinetic studies in mice, Ferroptosis-IN-12 shows promising potential for research in the field of AKI.</p>

<p>ARD-61: potent PROTAC, degrades AR/PR in AR+ cancers, triggers apoptosis, inhibits tumor growth in mice.</p>

<p>CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor that targets CRM1, localizing it to the nuclear periphery, depleting its nuclear presence, and inhibiting</p>

<p>L-threo-PPMP blocks GlcT, curbs glycosphingolipid creation, and triggers cell death, showing anti-cancer effects.</p>

<p>PB28: A potent σ2 agonist (Ki 0.68 nM), σ1 antagonist (Ki 0.38 nM), with anti-tumor properties and inhibits SARS-CoV-2 interactions.</p>

<p>Antiproliferative Agent-25 (Compound 3s4) is a selective PRMT5 inhibitor displaying an IC50 of 0.11 μM.</p>

<p>AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA</p>

<p>NA-Ir is a ferroptosis (Ferroptosis) inducer that targets mitochondrial DNA (mtDNA) and activates the cGAS-STING pathway to stimulate ferritin autophagy (). It also induces the production of reactive oxygen species (ROS) through photodynamic therapy (PDT), depletes glutathione (GSH), and downregulates glutathione peroxidase 4 (GPX4), thereby triggering lipid peroxidation and ferroptosis. NA-Ir exhibits enhanced anticancer activity under light exposure and selectively inhibits cancer cells with high H2S content.</p>

<p>FL118 is a novel survivin inhibitor that inhibits cancer stem cell-like properties.FL118 is a novel camptothecin analog with anticancer activity that inhibits</p>

<p>HDAC-IN-79 (compound 4) is an orally active dual inhibitor of xanthine oxidase and HDAC, exhibiting potent anti-hyperuricemia and antitumor activities in vivo (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM). Among leukemia cells, it is most effective in inhibiting the growth of HL60 cells (IC50=0.706 μM) and induces both apoptosis and autophagy. HDAC-IN-79 also modulates the expression levels of biomarkers associated with intracellular HDAC inhibition.</p>

LZFPN-90 (LZ90) is a dual-target compound aimed at NAMPT and PD-L1. It inhibits the interaction between PD-1/PD-L1 and NAMPT activity. LZFPN-90 suppresses cell growth in a NAMPT-dependent manner, blocking the cell cycle and subsequently inducing apoptosis. Additionally, LZFPN-90 exhibits target-dependent antitumor activity, impacting metabolic processes and the immune system.

<p>Photosensitizer-6 (Compound 4) is a metal ion complex that inhibits TrxR. It induces apoptosis in 4T1 cells, targeting cancer cells and eliminating tumors through chemophototherapy and immunogenic cell death under illumination. Additionally, Photosensitizer-6 can be utilized for tumor imaging.</p>

<p>Thalidomide 4'-oxyacetamide-alkyl-C2-amine HCl is an E3 ligase ligand-linker conjugate containing the E3 ubiquitin ligase cereblon (CRBN) and linker.</p>

<p>Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region.</p>

<p>8-Aminoadenosine reduces ATP, blocks mRNA synthesis, and Akt/mTOR signaling, triggering autophagy and apoptosis independently of p53, with antitumor effects.</p>

<p>Trichostatin C, a natural glycosylated hydroxamate, is a histone deacetylase inhibitor with antifungal properties and can induce cell differentiation.</p>

<p>GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM.</p>

<p>ZS3-046 is a TAF1 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of TAF1. It can activate p53 and induce apoptosis in acute myeloid leukemia (AML) cells. Additionally, ZS3-046 demonstrates anti-tumor efficacy in AML xenograft mouse models.</p>