Apoptose

<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>Albicanol is a biochemical.</p>

<p>Bromoiodoacetamide (I-HAcAm): cytotoxic, induces ROS &amp; apoptosis in HepG-2 cells.</p>

<p>Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified derivative of Thalidomide serving as a Cereblon ligand to recruit CRBN proteins and a pivotal intermediate in</p>

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

<p>Ceftiofur hydrochloride (U-67279A) is a stable, broad-spectrum 3rd-gen cephalosporin with antibacterial properties.</p>

<p>Xylopine: an aporphine alkaloid, cytotoxic to cancer cells, induces oxidative stress, G2/M arrest, and apoptosis.</p>

<p>Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.</p>

<p>Siomycin A: thiopeptide antibiotic, selectively inhibits FOXM1, anti-tumor, induces apoptosis.</p>

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

<p>Carubicin, an anthracycline antibiotic from Actinomadura carminata, disrupts DNA replication and repair by intercalating DNA and inhibiting topoisomerase II.</p>

<p>Fisetin quarterhydrate, a natural flavonol present in numerous fruits and vegetables, exhibits benefits including antioxidant, anticancer, and neuroprotective</p>

<p>Verproside is a useful organic compound for research related to life sciences. The catalog number is T124745 and the CAS number is 50932-20-2.</p>

<p>dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.</p>

<p>Pantinin-1 is an antimicrobial peptide found in the venom of the emperor scorpion (Pandinus imperator). This compound exhibits strong antibacterial activity against Gram-positive bacteria and fungi, but has weaker effects on Gram-negative bacteria. Additionally, Pantinin-1 demonstrates very low hemolytic activity on human red blood cells and possesses anticancer properties, specifically inducing apoptosis in tumor cells.</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>TAS-117, a PKB/Akt inhibitor, is used potentially for the treatment of solid tumors.</p>

<p>ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.</p>

<p>Anticancer agent 104 has anticancer activity, and induces cancer cell apoptosis [1] .</p>

<p>Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.</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>Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.</p>

<p>Sandalore boosts hair growth, reduces cell death, and raises IGF-1, acting on olfactory receptor OR2AT4.</p>

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

<p>Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.</p>

<p>PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.</p>

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

<p>TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.</p>

<p>Thalidomide-based E3 ligase ligand for PROTAC degrader MI-389 synthesis, linked to cereblon and Boc.</p>

<p>Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linker for PROTACs with a 3-unit PEG.</p>

<p>Vonlerolizumab (MOXR 0916) is a humanized IgG OX40 agonist monoclonal antibody with potential in cancer and immune disease research.</p>

<p>Conophylline, an alkaloid from Ervatamia microphylla, induces pancreatic cell differentiation and apoptosis, and suppresses HSC.</p>

<p>KWCN-41, a RIPK1 inhibitor with 88 nM IC50, blocks necrosis, spares apoptosis, and is anti-inflammatory.</p>

<p>(R)-JAK2/STAT3-IN-10a is the R-isomer of JAK2/STAT3-IN-1.JAK2/STAT3-IN-1 is a structural domain inhibitor of GP130 D1 with antitumor activity.</p>

<p>JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.</p>

<p>WKYMVM is a N-formyl peptide receptor (FPR1) agonist.</p>

<p>Betifisolimab (MSB-2311) is a humanized antibody targeting PD-L1 for solid tumors and blood cancer research.</p>

<p>GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-</p>

<p>KC01 selectively inhibits ABHD16A (IC50: 0.2-0.5 μM), much more potent than KC02 (&gt;10 μM); human ABHD16A IC50: 90±20 nM.</p>

<p>Spexin TFA: GAL2/GAL3 agonist (EC50: 45.7/112.2 nM), no activity at GAL1, reduces appetite, fatty acid uptake, and LH secretion; anxiolytic.</p>

<p>Z-Ala-Ala-Asp-CMK (Z-AAD-CMK) is a selective granzyme B inhibitor that blocks granzyme B protease activity, for inflammatory diseases and tumours.</p>

<p>Potent PROTAC degrader for FLT3/CDK9, induces apoptosis, and shows promise for FLT3-ITD mutated AML research.</p>

<p>SB 699551 is a selective 5-HT5A antagonist (Ki=6.31 nM) that enhances 5-HT neuronal function. It inhibits SERT (Ki=25.12 nM),inhibit breast cancer.</p>

<p>Mcl1-IN-26 is an effective and selective myeloid cell leukemia 1 inhibitor.</p>

<p>RMC-9805(Zoldonrasib) is a KRAS G12D inhibitor with anti-tumor and anti-proliferative activity for the study of pancreatic cancer.</p>

<p>ChoKα Inhibitor-4 is a bioisosteric agent that effectively inhibits human choline kinase α1 (HChoK α1) with an IC50 of 0.66 μM.</p>

<p>S-(5'-Adenosyl)-L-methionine iodide, also known as S-Adenosyl-L-methionine iodide, is a vital methyl donor present in all living organisms [1].</p>

<p>BLU-222 is a potent, selective and orally active CDK2 inhibitor. BLU-222 shows robust antitumor activity.</p>

<p>Syringolin A is a useful organic compound for research related to life sciences. The catalog number is T125354 and the CAS number is 212115-96-3.</p>

<p>PCC0208017 is an inhibitor of MARK3 and MARK4 with IC50s of 1.8 and 2.01 nM. PCC0208017 disrupts microtubule dynamics and displays potent antitumor activity.</p>

<p>Lodapolimab (LY3300054) is an IgGλ anti- PD-1 monoclonal antibody [1] .</p>

<p>Ganoderic acid T1, a derivative of Ganoderic acid T, triggers cancer cell apoptosis by boosting ROS and activating caspases.</p>

<p>Thailanstatin D blocks AR-V7 splicing, disrupts U2AF65/SAP155 binding, and induces apoptosis in CRPC xenografts.</p>

<p>Potent GAL2/GAL3 agonist (EC50 = 45.7, 112.2 nM), inactive at GAL1. Reduces appetite, fatty acid uptake in adipocytes, and LH in goldfish; anxiolytic in vivo.</p>

<p>Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.</p>

<p>Sotigalimab (APX 005) is a monoclonal antibody targeting CD40 with anticancer activity for the study of metastatic pancreatic cancer.</p>

<p>Antiproliferative agent-23: destabilizes microtubules, induces apoptosis in cancer cells via mitochondrial path, and triggers ER stress.</p>

<p>Topoisomerase II inhibitor 14: powerful anticancer agent that induces apoptosis, halts S phase, and lowers GSH, MDA, and NO levels.</p>

<p>Platycoside G3 is a useful organic compound for research related to life sciences. The catalog number is T124100 and the CAS number is 849758-44-7.</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>Apoptosis Inducer 13 (Compound Ru4) promotes apoptosis in cancer cells while also suppressing their migration and invasion.</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>TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.</p>

<p>hMcl-1-IN-1 (Compound 9) is an hMcl-1 inhibitor based on a His224 arylsulfonyl fluoride, displaying an IC50 value of 5.8 nM.</p>

<p>PROTAC HIF-1α degrader-1 (compound V2) is an effective proteolysis-targeting chimeric (PROTAC) degrader of hypoxia-inducible factor-1α (HIF-1α), with an IC50 value of 7.54 µM. This compound exhibits anti-proliferative activity, reduces HIF-1α protein expression, and induces apoptosis.</p>

<p>RWJ-56110 dihydrochloride is a potent PAR-1 inhibitor (IC50=0.44μM), blocking platelet aggregation, angiogenesis, and induces apoptosis. No PAR-2/3/4 effect.</p>

<p>NDI-Lyso is an anticancer agent targeting lysosomes, functioning through an enzyme-induced self-assembly (EISA) mechanism catalyzed by Cathepsin B. In cancer cell lysosomes, it forms rigid long fibers, promoting lysosomal swelling, lysosomal membrane permeabilization (LMP), and membrane disruption. This leads to non-classical caspase-independent apoptosis (Apoptosis). NDI-Lyso demonstrates significant selective anticancer activity across various cancer cell lines and drug-resistant cancer cells (IC50 approximately 10 μM), while exhibiting low toxicity to normal cells (IC50 &gt; 60 μM).</p>

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

<p>EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.</p>

<p>DiPT-4, a dual TOP1/PARP1 inhibitor, effectively induces DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells, with potential to</p>

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

<p>SCR7, a specific DNA Ligase IV inhibitor, blocks nonhomologous end-joining (NHEJ).</p>

<p>Antitumor agent-36: potent anti-cancer; causes DNA damage, triggers apoptosis, enhances immune response by upregulating T cells.</p>

<p>Ledostomig is an immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody that targets human neurotensin receptor type 5 (NTS5) and programmed death-1 (PD-1). It shows potential for research in various cancer types.</p>

<p>(Iso)-Z-VAD(OMe)-FMK is an isomer of Z-VAD(OMe)-FMK, which is a pan-caspase inhibitor with irreversible properties. Z-VAD(OMe)-FMK is also an inhibitor UCHL1.</p>

<p>H-20 is a PD-1 agonist that reduces the required dosage of morphine for analgesia. It can be used in studies related to chronic pain.</p>

<p>AS-99 TFA: potent ASH1L inhibitor, IC50=0.79 μM, combats leukemia, inhibits cell growth, induces apoptosis.</p>

<p>VEGFR-2-IN-36 (compound 15) serves as a potent VEGFR-2 inhibitor, exhibiting an IC50 value of 0.067 μM, and acts as an apoptosis inducer with demonstrated</p>

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

<p>Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM.</p>

<p>Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. It effectively blocks estrogen production and inhibits the proliferation of breast cancer cell lines such as MCF-7, arresting the cell cycle in the G1 phase and inducing apoptosis. Aromatase-IN-5 shows promise for breast cancer research.</p>

<p>Cardanol (C15:1), found in cashew nut shell liquid, induces mitochondria-associated apoptosis in human melanoma cells.</p>

<p>IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug that suppresses IDO expression. It induces apoptosis, reduces mitochondrial membrane potential, and inhibits tumor cell migration and invasion. Additionally, IDOi-Pt(IV) prodrug-1 triggers reactive oxygen species-mediated endoplasmic reticulum stress and the secretion of damage-associated molecular patterns (DAMPs), leading to immunogenic cell death (ICD). Compared to cisplatin, IDOi-Pt(IV) prodrug-1 exhibits relatively high efficiency and low toxicity in its antitumor activity.</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>Thalidomide-O-C7-NH2 is a cereblon ligand-linked E3 ligase for PROTAC use.</p>

<p>ROTACMNK1degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM and a Dmax greater than 96% in MV4-11 cells. It significantly reduces p-eIF4E levels with an IC50 of 22.07 nM, induces apoptosis, and causes cell cycle arrest at the G1 phase. This compound exhibits potent antitumor activity, demonstrating strong anti-leukemic effects in MV4-11 xenograft mouse models with acceptable drug safety.</p>

<p>TopoII/tubulin-IN-1 (Compound 1B8) is an inhibitor of TopoII/tubulin. It effectively suppresses the proliferation of tumor cells and reduces ROS levels, while inducing apoptosis and cell cycle arrest, without showing significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 exhibits antitumor activity.</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>PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis.</p>

<p>JGB1741, a SIRT1 inhibitor (IC50=15µM), modulates apoptosis markers and p53 acetylation in breast cancer research.</p>

<p>Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.</p>

<p>XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2/3/T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.</p>

<p>Schisandronic acid is a triterpenoid acid isolated from the stems of Schisandra propinqua.</p>

<p>Arg-Gly-Asp-D-Phe-Val (TFA) has anti-tumor activity and is an inhibitor of integrin αvβ3.</p>

<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>Thalidomide-O-C2-acid: E3 ligase ligand-linker for PROTAC, with cereblon-derived Thalidomide component.</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>VEGFR-2-IN-61 (Compound 7b) is an inhibitor of VEGFR-2 with an IC50 of 2.83 µM. It effectively inhibits the proliferation of various cancer cells, including MCF-7 cells, with an IC50 of 2.12 µM. Additionally, VEGFR-2-IN-61 suppresses cell migration and induces oxidative stress and apoptosis in MCF-7 cells.</p>

<p>RMC-7977 is a inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.</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>(+)-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>Poly(I:C):Kanamycin (1:1) sodium is a complex.Poly(I:C) is a TLR3 and RIG-I/MDA5 agonist.Kanamycin is an antimicrobial,Gram-negative and positive bacteria.</p>

<p>EGFR-IN-153 (Compound 5l) is an EGFR inhibitor that suppresses the proliferation of MDA-MB-231 cells with an IC50 of 0.73 μM and induces apoptosis. It is applicable for research in breast cancer.</p>

<p>α-Tubulin polymerization-IN-1 (Compound 8l) functions as an inhibitor of α-tubulin polymerization. This compound modulates the NRF2/KEAP-1 signaling pathway and induces ROS production in PC-3 cells, leading to apoptosis. It inhibits the proliferation of PC-3 cells with a GI50 of 0.17 µM, causing cell cycle arrest in the G2/M phase. Additionally, α-Tubulin polymerization-IN-1 demonstrates antitumor activity in mouse models.</p>

<p>NSC 295642: phosphatase inhibitor, boosts phospho-Erk in cells, aids cancer research.</p>

<p>PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal</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>