Apoptosis

<p>CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that impedes the cell cycle by binding to CDK2, leading to cytotoxicity, increased ROS production, and apoptosis (Apoptosis). It exhibits anticancer activity with an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. CDK2-IN-41 is applicable in research related to AML-associated cancers.</p>

<p>NYY-6a is a ferroptosis (Ferroptosis) inhibitor, demonstrating significant suppression of RSL3-induced ferroptosis in 786-O and HT-1080 cells, with EC50 values of 52 nM and 50 nM, respectively. As a radical-trapping antioxidant (RTA), NYY-6a effectively reduces lipid peroxidation, comparable to ferrostatin-1 and liproxstatin-1, making it useful for research into ferroptosis-related pathologies.</p>

<p>FMP is a platinum (IV) complex. It significantly upregulates the expression of γ-H2AX and p53, enhances ROS production, and markedly increases the expression of apoptosis (Apoptosis) related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP exhibits antiproliferative activity against breast cancer.</p>

<p>TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, showing significant antiproliferative activity. It can induce G1 phase cell cycle arrest and apoptosis (with notable increases in early and late apoptosis rates) and is useful for research in cancers such as colon, breast, and liver cancer.</p>

<p>Sasanlimab (PF-06801591), a humanized IgG4-κ antibody, selectively targets PD-1 and is primarily produced in Chinese Hamster Ovary (CHO) cells [1].</p>

<p>Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active inhibitor of tubulin polymerization. It acts at the colchicine binding site to inhibit tubulin polymerization with an IC50 value of 2.505 μM, effectively disrupting the intracellular microtubule network and interfering with mitosis. Tubulin polymerization-IN-76 shows significant inhibitory effects on MGC-803 and HGC-27 cells, with IC50 values of 1.61 and 1.82 nM, respectively. It effectively suppresses colony formation and cell migration activities in these cell lines, inducing G2/M phase cell cycle arrest and apoptosis (Apoptosis). Furthermore, Tubulin polymerization-IN-76 exhibits broad-spectrum antiproliferative activity.</p>

<p>DNMT-IN-4 (Compound 4d) is a DNMT inhibitor with an IC50 value of 5.78 µM. It induces apoptosis and exhibits anticancer activity.</p>

<p>MBC-11 trisodium, a bisphosphonate-Ara-C conjugate, may treat TIBD.</p>

<p>Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.</p>

<p>Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.</p>

<p>CDK9-IN-36 (Compound T7) is a potent, selective, and metabolically stable CDK9 inhibitor with an IC50 value of 1.2 nM. It effectively suppresses the proliferation of Osimertinib-resistant NSCLC cells by downregulating Mcl-1, reducing colony formation, and inducing apoptosis. Additionally, CDK9-IN-36 exhibits antitumor activity in xenograft models.</p>

<p>Tubulin polymerization-IN-73 (Compound 37) is an inhibitor of microtubule polymerization with an IC50 of 1.8 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in A549 cells. The compound inhibits the proliferation of both A549 WT and A549/T resistant cells with IC50 values of 0.023 μM and 0.057 μM, respectively. Additionally, Tubulin polymerization-IN-73 demonstrates antitumor activity in mouse models.</p>

<p>Src Inhibitor4 (Compound 18) is a derivative of KX-01 and functions as a Src inhibitor. It effectively disrupts tumor cells, damages microtubules, and induces cell cycle arrest, apoptosis, and immunogenic cell death. After introducing phenol or aniline functional groups, Src Inhibitor4 serves as a payload conjugation site for antibody-drug conjugates, showcasing antitumor activity.</p>

<p>Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic</p>

<p>Type-I/-II Photosensitizer-1 (compound 8b) is a photosensitizer with anticancer properties. It exhibits significant phototoxicity against A549 and 4T1 tumor cells. Under laser irradiation, Type-I/-II Photosensitizer-1 demonstrates strong oxygen-independent antitumor activity with an IC50 ranging from 1.50 to 1.76 μM.</p>

<p>C188, a naphthol-based STAT3 inhibitor, blocks IL-6-induced STAT3 activity in HepG2 cells, sparing STAT1.</p>

<p>Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.</p>

<p>Thalidomide-O-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].</p>

<p>2-deoxy-D-Glucose-13C6 is an internal standard for GC/LC-MS, a glycolysis inhibitor, and induces apoptosis in certain cells at 2 mg/ml.</p>

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

<p>6-Bromo-4-methoxypyrazolo[1,5-a]pyridine-3-carbonitrile is a PDK1 inhibitor with anticancer and antiproliferative activity that can be used to study</p>

<p>Pro-GA is a cell-permeable γ-glutamylcyclotransferase (γ-GGCT) inhibitor that inhibit proliferation in multiple bladder cancer cell lines. antitumour.</p>

<p>NMC-001 is a human IgG1 monoclonal antibody (mAb) that targets MDM2. It is useful for pancreatic cancer research. The recommended isotype control is HumanIgG1kappa, Isotype Control.</p>

<p>Narasin (sodium salt) (HainanMycin) induces tumor necrosis factor-related apoptosis-induced ligand (TRAIL)-mediated apoptosis by ER stress in glioma cells and</p>

<p>Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic</p>

<p>4-Nitro-3-cresol exhibits ciliate toxicity against Tetrahymena pyriformis and is widely used in biochemical experiments and drug synthesis research.</p>

<p>TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα ( K D = 6.8 nM).</p>

<p>Calcimycin (A-23187) is an antibiotic calcium ionophore that raises intracellular Ca2+ to induce cell death.</p>

<p>AMXT-1501 tetrahydrochloride is an inhibitor of polyamine transport.</p>

<p>Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).</p>

<p>RIP2 Kinase Inhibitor 4, a selective RIPK2 PROTAC, degrades RIPK2 (pIC50=8), inhibits TNF-α release.</p>

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

<p>Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.</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>Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.</p>

<p>Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.</p>

<p>Prolgolimab (BCD-100) is an anti-PD-1 antibody used in melanoma research.</p>

<p>Methylene Violet 3RAX is a cationic dye that is a potential photosensitizer in photodynamic therapy and has antitumor activity.</p>

<p>Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].</p>

<p>Glutathione arsenoxide hydrochloride: anti-cancer, inhibits tumour metabolism, targets ANT, promotes apoptosis, marks cell proteins.</p>

<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>

<p>Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist.</p>

<p>Boanmycin, an antibiotic exhibiting antitumor activity, induces cellular senescence and apoptosis [1] [2] [3].</p>

<p>Nofazinlimab (CS1003) is a human anti-PD-1 IgG4 monoclonal antibody for the study of unresectable hepatocellular carcinoma (uHCC).</p>

<p>Pidilizumab (CT-011), a humanized IgG1κ anti-PD-1 monoclonal antibody, serves as a DLL1 antagonist with potential applications in researching hematologic</p>

<p>Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.</p>

<p>Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.</p>

<p>YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.</p>

<p>Camrelizumab (SHR-1210) is a human IgG4-κ monoclonal antibody with high affinity and directed against PD-1.Camrelizumab binds PD-1 with a binding affinity of up</p>

<p>Thalidomide-NH-amido-C6-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, designed for the synthesis of PROTAC.</p>

<p>CPTH2 is an inhibitor of the HAT activity of Gcn5.</p>

<p>P-gp inhibitor 16 (compound 14) is an inhibitor of p-glycoprotein. It significantly enhances apoptosis induced by doxorubicin and displays anticancer properties.</p>

<p>Cu(I) chelator 1 (Compound LH2) is a chelating agent specifically targeting the Cu(I) redox state. It inhibits the production of ROS.</p>

<p>EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. It exhibits antiproliferative activity, effectively inhibiting the proliferation of H1975 cells and inducing apoptosis (apoptosis). EGFR-IN-107 is applicable in cancer research.</p>

<p>Chlopynostat (Compound 6c) is an HDAC1 inhibitor with an IC50 value of 67 nM. It induces apoptosis by inhibiting HDAC1, thereby reversing STAT4/p66Shc defects.</p>

<p>DB0614 degrades 26 kinases including AAK1 and CDK6, targeting aberrant activity in disease research.</p>

<p>Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate</p>

<p>Enniatin complex: fungal cyclohexadepsipeptides inhibit enzymes, induce cancer cell apoptosis, and have ionophoric, antibiotic, and hypolipidemic effects.</p>

<p>Ferroptosis-IN-13 (compound NY-26) is an inhibitor of ferroptosis. It effectively suppresses RSL3-induced ferroptosis in 786-O cells, with an EC50 value of 62 nM.</p>

<p>WAY-118959-A is a potential microtubule acetylation inhibitor.</p>

<p>Sorafenib D4 is deuterium-labeled Sorafenib, a multi-kinase inhibitor (Raf-1, B-Raf, VEGFR-3) with IC50s: 6, 20, 22 nM.</p>

<p>Se-Aspirin (Se-NSAID-8) has anticancer activity and gastroprotective effects, inhibits activation of proinflammatory and pro-survival NF-ĸB pathways, and inhibits the expression of anti-apoptotic targets downstream of NF-ĸB (e.g., Bcl-xL, Mcl-1, and survivin).Se-Aspirin induces Cell cycle arrest and activation of apoptosis accelerates ulcer healing and can be used to study pancreatic and colorectal cancer.</p>

<p>ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.</p>

<p>Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic.</p>

<p>Eucalyptol, a natural monoterpenoid and cyclic ether found in eucalyptus species, effectively controls excessive airway mucus secretion and asthma by inhibiting pro-inflammatory cytokines. It serves as an efficacious treatment for non-purulent sinusitis, reducing inflammation and pain when applied topically, and demonstrating leukemic cell-killing capabilities in vitro.</p>

<p>CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.</p>

<p>TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.</p>

<p>PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 77 nM. This compound can activate Jurkat T cells and effectively block the PD-1/PD-L1 immune checkpoint.</p>

<p>PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.</p>

<p>VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation.</p>

<p>2-aminobenzo[d]thiazol-6-ol: antimicrobial, antioxidant, anticancer; may trigger cancer cell apoptosis.</p>

<p>(+)-Mcl-1 inhibitor 21 (Example 1-37) is a chemical compound that acts as an Mcl-1 inhibitor with an IC50 value of 172 nM. It demonstrates pro-apoptotic and antiproliferative activities in SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.</p>

<p>BC13 is a CDK6/BRD4 inhibitor with IC50 values of 234 nM for CDK6 and 36 nM for BRD4. It exhibits antiproliferative properties, induces apoptosis (cell death) and DNA damage, and elevates ROS levels.</p>

<p>CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.</p>

<p>DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]</p>

<p>PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.</p>

<p>STEP-IN-1 (Compound 14b) is a potent and selective inhibitor of STEP, with an IC50 of 5.27 μM. It offers neuroprotective effects by safeguarding neuronal cells from glutamate-induced toxicity, reducing intracellular reactive oxygen species (ROS) accumulation, and inhibiting apoptosis. STEP-IN-1 is applicable in research related to neurodegenerative diseases.</p>

<p>GPLGIAGQ acetate: MMP2-cleavable peptide; stimulus-sensitive linker for MMP2-targeted liposomal/micellar carriers in photodynamic therapy.</p>

<p>The compound is a negative control peptide for the Bax inhibitor peptides V5 and P5.</p>

<p>Mangafodipir trisodium can enhance contrast in magnetic resonance imaging (MRI) of the liver, is a contrast agent delivered intravenously.</p>

<p>Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, acts as a competitive and reversible FXR antagonist (IC 50 = 40 μM) and exhibits antiapoptotic</p>

<p>8-Bromo-cAMP is a cell-permeable cAMP analogue and activator of CAMP-dependent protein kinase A that induces cell death and reduces proliferation.</p>

<p>AMPK-IN-6 (compound 13a) is a potent AMPK inhibitor with an IC50 value of 0.093 µM. It induces apoptosis and suppresses autophagy. Additionally, AMPK-IN-6 exhibits antiproliferative activity and holds potential for research into pulmonary arterial hypertension.</p>

<p>2,4,6-trichloroanisole inhibits the cell viability of CHO and C32 cell lines and apoptosis, antibacterial activity against Plasmodium falciparum.</p>

<p>PROTACROR1degrader-1 (Compound 11d) serves as a PROTAC degrader targeting the pseudokinase ROR1, with the capability of degrading ROR1 in NSCLC cells at a DC50 of 40-80 nM. It induces PARP cleavage and apoptosis in NCI-H23 cells. [Pink: ligand for target protein ROR1 ligand-1; Black: linker; Blue: ligand for VHL E3 ligase (S,R,S)-AHPC]</p>

<p>Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer properties, exhibiting an IC50 of 90 nM against MCF-7 breast cancer cells. This compound induces apoptosis by modulating the Bax-caspase 3 signaling pathway and triggers ferroptosis by regulating key signaling molecules (including GPX4). Antitumor agent-196 shows potential for cancer research applications.</p>

<p>Bcl-2-IN-5: BCL-2 inhibitor, IC50: 0.12 nM (wt), 0.14 nM (D103Y), 0.22 nM (G101V); Cell growth IC50: 0.2 nM, 0.44 nM (RS4;11).</p>

<p>Apoptosisinducer 31 (compound 19) triggers caspase-dependent apoptosis (cell death). It plays a crucial role in cancer research.</p>

<p>STAT3-IN-40 (Compound 8b) is an anticancer agent. It initiates immune responses in CD4+ and CD8+ T lymphocytes by inhibiting the expression and phosphorylation of STAT3, and induces ferroptosis and apoptosis in tumor cells. STAT3-IN-40 is valuable for research into cancer chemoimmunotherapy drugs.</p>

<p>Thalidomide-derived cereblon ligand linked to a PROTAC technology linker, Thalidomide-O-amido-C3-NH2, is a synthetic E3 ligase ligand-linker.</p>

<p>Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and</p>

<p>DPH: antihistamine for cough, nausea, itching, allergy, Parkinson's, sleep aid, cold remedy.</p>

<p>WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).</p>

<p>Bcl-2-IN-15 (Compound 13d) is a Bcl-2 inhibitor with an IC50 of 363 nM, which impedes the proliferation of the NCI leukemia cancer cell line [1].</p>

<p>Raptinal activates caspase-3 directly and initiates intrinsic caspase-dependent apoptosis pathway in multiple cell lines.</p>

<p>NSD-IN-4 (Compound A8) is a potent and orally active inhibitor of NSD3, inducing apoptosis in a dose-dependent manner. It demonstrates significant antitumor activity against lung squamous cell carcinoma.</p>

<p>Anticanceragent 267 (Compound 5q) serves as an activator of RIPK3 and MLKL. It effectively inhibits the proliferation of several cancer cell lines, with IC50 values of 9.79, 10.77, and 5.94 μM for MDA-MB-231, MDA-MB-486, and MCF-7, respectively. The compound induces cell cycle arrest at the subG1 phase and triggers necroptosis in MDA-MB-231 cells. Additionally, Anticanceragent 267 demonstrates antitumor activity in mouse xenograft models.</p>

<p>Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells.</p>

<p>Zalypsis, a transcription factor inhibitor, is used potentially for the treatment of lymphoma, and cervical carcinoma.</p>

<p>Tubulin/MMP-IN-3 (Compound 15j) is a dual inhibitor of tubulin polymerization and MMP, effectively inhibiting MMP-2 and MMP-9 with IC50 values of 21.13 μM and 19.24 μM, respectively. It disrupts the NF-κB signaling pathway, leading to mitochondrial dysfunction and mitochondrial-dependent apoptosis. Tubulin/MMP-IN-3 shows antiproliferative activity in various cancer cells by causing cell cycle arrest at the G2/M phase and demonstrates antitumor effects in mouse models.</p>