Apoptosis

<p>Calcimycin hemimagnesium is an antibiotic, ionophore, and ATPase inhibitor that boosts intracellular Ca2+, causing cell death and apoptosis.</p>

<p>Thalidomide-NH-PEG4-COOH is a E3 ligase ligand-linker for synthesizing the selective degrader dCBP-1 targeting p300/CBP.</p>

<p>MI-1061 TFA: potent MDM2 inhibitor, orally bioavailable, stable (IC50=4.4 nM, Ki=0.16 nM), activates p53, induces apoptosis in mice tumors.</p>

<p>PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.</p>

<p>CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).</p>

<p>Sarglaroids F (compound 6), an anti-inflammatory agent extracted from the roots of Grass Coral, suppresses LPS/ATP-induced IL-1β secretion by modulating K+</p>

<p>PROTAC EGFR degrader 5 effectively breaks down EGFR Del19 in HCC827 cells at 34.8 nM, inducing apoptosis and G1 arrest.</p>

<p>MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].</p>

<p>Vallesiachotamine, a recognized monoterpene indole alkaloid, exhibits anti-tumor activity [1].</p>

<p>Tomuzotuximab: fully human, glycoengineered IgG1 anti-EGFR monoclonal antibody with anticancer properties.</p>

<p>EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. It induces apoptosis by arresting the cell cycle at the G2/M phase and exhibits antitumor activity.</p>

<p>TrxR-IN-7 (14f) is a potent inhibitor of thioredoxin reductase (TrxR), with an IC50 value of 3.5 µM. It exhibits antiproliferative activity and can induce apoptosis and the production of reactive oxygen species (ROS).</p>

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

<p>TS-IN-5 (Compound 15) is an inhibitor of thymidylate synthase (TS). It induces apoptosis by modulating the proteins Bax, BCL-2, PI3K, and STAT1. TS-IN-5 exhibits antitumor activity against liver cancer, breast cancer, and colon cancer.</p>

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

<p>PNT100: 24-base DNA oligo targeting BCL-2 regulatory region; halts tumor cell growth, induces death.</p>

<p>Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar</p>

<p>DefNEtTrp is an iron bis-chelating ligand composed of Def and Trp groups. It demonstrates potent broad-spectrum antiproliferative and cytotoxic effects in cancer cell lines. DefNEtTrp induces apoptosis and ferroptosis, exhibiting cytotoxicity with an IC50 value of 0.77 μM.</p>

<p>CQ627 is a molecular glue that targets the degradation of RIOK2. It effectively recruits the E3 ubiquitin ligase RNF126, inducing the proteasomal degradation of RIOK2 via the ubiquitin-proteasome system (UPS) in MOLT4 leukemia cell lines, with a DC50 value of 410 nM. Additionally, CQ627 induces apoptosis in a dose-dependent manner in these cells, blocking the cell cycle at the G2/M phase, and exhibits antiproliferative activity across various cancer cell lines. It also demonstrates in vivo anticancer activity in MOLT4 xenograft mouse models.</p>

<p>JAK-IN-40 (Compound 46) is an inhibitor of JAK, effectively targeting JAK1, JAK2, and JAK3 with IC50 values of 0.022, 0.759, and 1.601 μM, respectively. It reduces the phosphorylation of STAT3 and inhibits the proliferation of cancer cells Ba/F3 and JAK1-TEL Ba/F3 with GI50 values of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle progression at the G2/M phase in H1975 and H2087 cells, leading to apoptosis. Additionally, JAK-IN-40 exhibits a synergistic anti-tumor effect when used in combination with Osimertinib.</p>

<p>Nargenicin: a macrolide antibiotic effective against S. aureus, MRSA, M. luteus; inhibits bacterial DnaE and reduces inflammation and leukemia cell growth.</p>

<p>Thalidomide-PEG4-NH2 HCl, a cereblon ligand-linker for PROTAC.</p>

<p>Thalidomide-derived cereblon ligand with PROTAC linker as an E3 ligase ligand-linker conjugate, in hydrochloride form.</p>

<p>Relfovetmab is an anti- NGF monoclonal antibody (mAb) [1] .</p>

<p>Satratoxin G, from Stachybotrys chartarum, triggers apoptosis in nasal and brain OSNs.</p>

<p>EMB-02 is a bispecific antibody targeting both PD-1 and LAG-3. It inhibits the downregulation of T cell activation and proliferation mediated by PD-1 and LAG-3, showing potent anti-cancer properties.</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>Dimeric Smac mimetic inhibits XIAP, cIAP1/2 (IC50: 15/15/21 nM); binds BIR3 domain; degrades cIAPs; induces apoptosis in cancer cells; shrinks tumors in mice.</p>

<p>Antitumor Agent-41 (Compound N-12) exhibits potent antitumor properties, demonstrating significant antimigration and anti-invasion activities.</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>Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.</p>

<p>Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linked E3 ligase used in PROTAC with a 2-unit PEG.</p>

<p>Sudubrilimab (HS636) is an IgG1-κ monoclonal antibody targeting PDL1, fused with TGFBR2-ECD to block PD-1/PDL1 and TGF-β in tumors.</p>

<p>ERK1/2 inhibitor 13 (Compound 21y) is an orally bioavailable ERK inhibitor that targets ERK1 and ERK2, with IC50 values of 91.71 nM and 97.87 nM, respectively. It effectively suppresses the proliferation of cancer cell lines MCF-7, 4T1, MDA-MB-468, and HCC1970 with IC50 values of 0.67 μM, 2.76 μM, 2.15 μM, and 1.68 μM, respectively. Additionally, it inhibits cancer cell migration, induces apoptosis and autophagy in MCF-7 cells, and demonstrates anti-tumor and anti-metastatic effects in a 4T1 xenograft mouse model.</p>

<p>Holothurin A is a triterpene glycoside.</p>

<p>5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory properties. It suppresses IL-6, IL-1β, TNF-α, and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. Additionally, 5-LOX-IN-8 decreases the disease activity index in DSS colitis models. This compound is applicable for research in inflammatory bowel disease (IBD).</p>

<p>YTHDF2-IN-1 (Compound CK-75) is an inhibitor of YT521-B homology domain family 2 (YTHDF2) with a dissociation constant (Kd) of 26.2 μM, and it effectively blocks the interaction between YTHDF2 and m6A RNA. It suppresses colony formation in JAR cells and exhibits antiproliferative activity in various cancer cell lines, with an IC50 in the micromolar range. Additionally, YTHDF2-IN-1 induces apoptosis in K562 cells and causes cell cycle arrest at the G0/G1 phase.</p>

<p>Thymidine 3',5'-diphosphate tetrasodium inhibits staphylococcal nuclease, SND1 &amp; tyrosyl nuclease; has anti-tumor properties &amp; catalyzes biochemical reactions.</p>

<p>Human membrane-bound PD-L1 polypeptide serves as an antigen for inducing the production of PD-L1 antibodies [1].</p>

<p>Z-LEHD-FMK is a selective and potent caspase-9 inhibitor that protects against reperfusion injury and slows apoptosis.Z-LEHD-FMK exhibits antitumor and</p>

<p>Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and</p>

<p>Pomstafib-2, a potent and selective inhibitor of STAT5b, reduces pSTAT5b expression and effectively induces apoptosis [1] [2].</p>

<p>Boc-D-FMK is an irreversible, cell-permeable, and broad-spectrum caspase inhibitor and inhibits apoptosis stimulated by TNF-α (IC50: 39 μM).</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>CPM-1285 induces apoptosis by effectively inhibiting the function of intracellular Bcl-2 and associated death antagonists.</p>

<p>Pacmilimab (CX-072) is a Probody immune checkpoint inhibitor targeting programmed death ligand 1 (PD-L1) with anti-tumor activity for the study of solid tumors.</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>Anticanceragent 178 (compound C2) is a potent anticancer compound. It effectively inhibits the proliferation and metabolic activity of MDA-MB 231 cells, with IC50 values of 1.1 and 4.2 μM, respectively. Additionally, Anticanceragent 178 induces ferroptosis and necroptosis in cells.</p>

<p>Fludarabine triphosphate inhibits key enzymes, causing cell death.</p>

<p>DJ4 induces a dose-dependent pro-apoptotic effect in the micromolar range.</p>

<p>Antitumor Agent-113 exhibits cytotoxicity in A549 cells, with an IC50 of 46.60 μM, and induces apoptosis, making it applicable for research in non-small cell</p>

<p>Necrosis inhibitor 2 hydrochloride (Compound B19) is an agent that inhibits cellular necrosis. It is useful for researching diseases associated with necrotic pathways, including inflammation, cancer, metabolic disorders, and neurodegenerative diseases.</p>

<p>Anticanceragent 204 (Compound 6) is a fluorinated derivative of cinnamamides with anticancer activity. It can arrest the cell cycle of HepG2 cells in the G1 phase and induces apoptosis by reducing mitochondrial membrane polarization (MMP) levels.</p>

<p>MX106-4C is a survivin inhibitor that selectively targets ABCB1-positive colorectal cancer cells. It can work synergistically with Doxorubicin for enhanced anticancer effects or restore Doxorubicin sensitivity in drug-resistant ABCB1 cells.</p>

<p>PROTACGPX4 degrader-2 (compound 18a) is a proteolysis-targeting chimera (PROTAC) that targets the degradation of glutathione peroxidase 4 (GPX4), with a DC50, 48h value of 1.68 μM. It induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. Additionally, PROTACGPX4 degrader-2 exhibits antiproliferative activity.</p>

<p>OPBP-1 is a D-peptide developed through phage display screening, molecular docking, and molecular dynamics simulations. It exhibits high stability, strong antitumor activity, and oral bioavailability. OPBP-1 selectively binds to the PD-L1 protein, significantly blocking the interaction between PD-1 and PD-L1, which helps restore and enhance T lymphocyte function while reducing the proportion of myeloid-derived suppressor cells (MDSCs), counteracting tumor-induced immune evasion. OPBP-1 is applicable for research in cancer immunotherapy.</p>

<p>Cytostatin: Natural antitumor, inhibits cell adhesion, blocks B16 melanoma, induces apoptosis, selectively targets PP2A (IC50 = 29 nM).</p>

<p>Antimycobacterial agent-5 (compound 27) is an imidazopyridine amide compound that targets the Mycobacterium electron transport chain (ETC) respiratory CIII2CIV2 supercomplex. It acts on Mycobacterium smegmatis CIII2CIV2 with an IC50 of 441 nM.</p>

<p>WK369 is an innovative small molecule inhibitor of BCL6, demonstrating remarkable bioactivity against ovarian cancer by inducing cell cycle arrest and triggering apoptosis. It binds directly to the BCL6-BTB domain, obstructing the interaction between BCL6 and SMRT, which results in the reactivation of p53, ATR, and CDKN1A.</p>

<p>PROTACEGFRdegrader 9 (Compound C6) is an orally active, CRBN-based PROTAC EGFR degrader. It has a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTACEGFRdegrader 9 demonstrates effective degradation activity against various EGFR mutants while not affecting EGFRWT.</p>

<p>MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.</p>

<p>TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide that exhibits inhibition of various gram-positive and negative bacterial</p>

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

<p>Mcl-1 Inhibitor 15 (Compound (Ra)-15), with a K i of 0.02 nM, is utilized in cancer research [1].</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>Boc-Asp(OBzl)-CMK, an inhibitor of IL-1 converting enzyme (ICE, caspase1), prevents the death of CHP100 neuroblastoma cells and inhibits IL-1β release induced by the viral coat protein [1].</p>

<p>TAT-NEP1-40 TFA, a blood-brain barrier-permeable peptide, safeguards PC12 cells against oxygen and glucose deprivation (OGD) and fosters neurite outgrowth.</p>

<p>Pep19-2.5: Synthetic antitoxin peptide inhibits LP/LPS signals via PRRs, preventing inflammation and pyroptosis.</p>

<p>PD-1/PD-L1-IN-48 (compound HD10) is an effective inhibitor of the PD-1/PD-L1 interaction, exhibiting an IC50 of 3.1 nM. It plays a vital role in cancer research.</p>

<p>PROTACNCOA4 degrader-1 (Compound V3) is a PROTAC-based degrader of NCOA4, exhibiting a DC50 of 3 nM in HeLa cells. Besides acting as a ferroptosis inhibitor, this compound effectively reduces the levels of NCOA4 and decreases intracellular ferrous (Fe2+) levels. Moreover, PROTACNCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model.</p>

<p>Thalidomide-PEG conjugate for E3 ligase in PROTACs; has cereblon ligand and 3-unit PEG linker.</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>Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.</p>

<p>Human PD-L1 inhibitor I, a peptide, blocks PD-L1/PD-1 interaction with 3.39 μM affinity.</p>

<p>CDC20-IN-2 (14c) is an inhibitor of Cdc20 with a KD of 7.65 μM, inducing G2/M phase arrest, promoting DNA damage accumulation, and stabilizing key substrates such as Cyclin B1 and Bim. This leads to enhanced apoptosis, as well as inhibition of tumor cell proliferation and migration.</p>

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

<p>Zamzetoclax (compound 1) acts as a potential inhibitor of Mcl-1.</p>

<p>MMRi62, a MDM2-MDM4 inhibitor, induces ferroptosis and autophagy in PDAC, degrades FTH1 and mutant p53, and inhibits KRAS/TP53 mutant PDAC in mice.</p>

<p>Emfizatamab (GNC-038) is a tetravalent antibody that activates CD3 and 4-1BB on T cells while targeting CD19 or PD-L1 on tumor cells, resulting in T-cell-mediated cytotoxicity against human leukemia and lymphoma cells.</p>

<p>SACLAC is a cysteine asparaginase activation inhibitor with antitumor activity used in the study of acute myeloid leukemia and cancer.</p>

<p>Ptd-p65-p1 Peptide TFA inhibits NF-kappaB, has a cell-penetrating antennapedia sequence, and selectively blocks NF-kappaB activation.</p>

<p>Tubulin Inhibitor 34 (compound b5), a potent anticancer agent, inhibits tubulin polymerization and induces G2/M arrest and apoptosis.</p>

<p>XIAP BIR2/BIR2-3 Inhibitor-3 functions as a dual inhibitor targeting both BIR2 and BIR2-3 domains, exhibiting potent activity with IC50 values below 1 nM. This compound is utilized in cancer research [1].</p>

<p>ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.</p>

<p>Carnitine palmitoyltransferase 2 (CPT2), an enzyme involved in fatty acid oxidation, serves as a prognostic biomarker for colorectal cancer (CRC).</p>

<p>PUMA BH3 activates Bak, binds Bcl-2; triggers apoptosis via cytochrome C release; Kd 26 nM.</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>TAT-NEP1-40, a blood-brain barrier (BBB) permeable peptide, confers protection to PC12 cells against oxygen and glucose deprivation (OGD) while promoting</p>

<p>Flaccidoside II, an active triterpenoid saponin from Anemone flaccida rhizome, both inhibits proliferation and induces apoptosis in Malignant Peripheral Nerve</p>

<p>Thalidomide-based cereblon ligand with 2-unit PEG linker for PROTAC, in hydrochloride form.</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>JPS014 TFA, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC</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>ZC0109 inhibits IDO1 (50 nM) &amp; TrxR1 (3.0 μM), induces ROS, arrests G1/S phase, causing cancer cell apoptosis.</p>

<p>Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].</p>

<p>Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM), exhibits an IC50 value of 3.38 μM against human dermal fibroblasts (HDF) and</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>WEHI-3773 is an inhibitor of the interaction between VDAC2 and either BAK or BAX. It prevents BAX-mediated apoptosis (Apoptosis) by blocking the recruitment of BAX to the mitochondria through VDAC2. Conversely, WEHI-3773 promotes BAK-mediated apoptosis (Apoptosis) by limiting VDAC2's inhibitory sequestration of BAK. This compound shows promise for research in the field of cancer therapy.</p>

<p>5-LOX-in-2: a 5-lipoxygenase inhibitor with IC50 of 0.33 μM, reduces kidney cancer cell activity, induces apoptosis.</p>

<p>Peptide from c-Jun (33-57) blocks JNK binding, inhibits phosphorylation, upregulates p21, and induces HeLa cell apoptosis.</p>