2. Signaling Pathways
  3. Apoptosis
  4. Apoptosis

Apoptosis

Apoptosis

Apoptosis

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Apoptosis is a distinctive form of cell death exhibiting specific morphological and biochemical characteristics, including cell membrane blebbing, chromatin condensation, genomic DNA fragmentation, and exposure of specific phagocytosis signaling molecules on the cell surface. Cells undergoing apoptosis differ from those dying through necrosis. Necrotic cells are usually recognized by the immune system as a danger signal and, thus, resulting in inflammation; in contrast, apoptotic death is quiet and orderly.

There are two major pathways of apoptotic cell death induction: The intrinsic pathway, also called the Bcl-2-regulated or mitochondrial pathway, is activated by various developmental cues or cytotoxic insults, such as viral infection, DNA damage and growth-factor deprivation, and is strictly controlled by the BCL-2 family of proteins. The extrinsic or death-receptor pathway is triggered by ligation of death receptors (members of the tumor necrosis factor (TNF) receptor family, such as Fas or TNF receptor-1 (TNFR1)) that contain an intracellular death domain, which can recruit and activate caspase-8 through the adaptor protein Fas-associated death domain (FADD; also known as MORT1) at the cell surface. This recruitment causes subsequent activation of downstream (effector) caspases, such as caspase-3, -6 or -7, without any involvement of the BCL-2 family.

Studies suggest that alterations in cell survival contribute to the pathogenesis of a number of human diseases, including cancer, viral infections, autoimmune diseases, neurodegenerative disorders, and AIDS (acquired immunodeficiency syndrome). Treatments designed to specifically alter the apoptotic threshold may have the potential to change the natural progression of some of these diseases.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-169403
    NW16
    		Inducer
    NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model.
    NW16
  • HY-126222B
    (E/Z)-MitoTam iodide, hydriodide
    		Inducer
    (E/Z)-MitoTam (iodide, hydriodide) (MitoTam (iodide, hydriodide)) is the E/Z mixture of MitoTam iodide, hydriodide. MitoTam iodide, hydriodide is a Tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.
    (E/Z)-MitoTam iodide, hydriodide
  • HY-100642S1
    3-O-Methyltolcapone-d4
    		Inducer
    3-O-Methyltolcapone-d4 (Ro 40-7591 d4) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma.
    3-O-Methyltolcapone-d<sub>4</sub>
  • HY-111524
    CPUY201112
    		Inducer
    CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research.
    CPUY201112
  • HY-N6725R
    Sterigmatocystine (Standard)
    		Inducer
    Sterigmatocystine (Standard) is the analytical standard of Sterigmatocystine. This product is intended for research and analytical applications. Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor. Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals.
    Sterigmatocystine (Standard)
  • HY-145856
    VEGFR-2-IN-11
    		Inducer
    VEGFR-2-IN-11 (Compound 8h) is a potent VEGFR-2 inhibitor with an IC50 of 60.27 nM. VEGFR-2-IN-11 shows antitumor activity and induces cell apoptosis.
    VEGFR-2-IN-11
  • HY-177780
    Cyclin K degrader 2
    		Inducer
    Cyclin K degrader 2 is a molecular glucose degrading agent that targets the cyclin K protein. Cyclin K degrader 2 has inhibitory activity against CDK1 and CDK9. Cyclin K degrader 2 causes a decrease in RNA polymerase II Ser2 phosphorylation levels, downregulation of DNA damage response gene expression, accumulation of DNA damage, G1 phase arrest of the cell cycle, and apoptosis. Cyclin K degrader 2 can be used for cancer research.
    Cyclin K degrader 2
  • HY-W010320R
    Ethyl maltol (Standard)
    		Inducer
    Ethyl maltol (Standard) is the analytical standard of Ethyl maltol. This product is intended for research and analytical applications. Ethyl maltol (2-Ethyl-3-hydroxy-4H-pyran-4-one) is an orally active and important food additive and flavor enhancer. Ethyl maltol is less toxic to rats and dogs. Ethyl maltol can enhance copper-mediated cytotoxicity and induce apoptosis in lung epithelial cells.
    Ethyl maltol (Standard)
  • HY-146040
    Anticancer agent 47
    		Inducer
    Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo.
    Anticancer agent 47
  • HY-13716S
    Noscapine-13C,d3
    		Inducer
    Noscapine-13C,d3 is a 13C- labeled and deuterated labeled Noscapine. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
    Noscapine-<sup>13</sup>C,d<sub>3</sub>
  • HY-181678
    DNA-PK/HDAC6-IN-1
    		Inducer
    DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia.
    DNA-PK/HDAC6-IN-1
  • HY-12482
    X-370
    		Inducer
    X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).
    X-370
  • HY-N0006S
    Demethoxycurcumin-d7
    		Inducer
    Demethoxycurcumin-d7 is the deuterium labeled Demethoxycurcumin. Demethoxycurcumin(Curcumin II), a major active curcuminoid, possess anti-inflammatory properties; also exert cytotoxic effects in human cancer cells via induction of apoptosis.
    Demethoxycurcumin-d<sub>7</sub>
  • HY-10820AS
    Pemetrexed-d5 disodium
    		Inducer
    Pemetrexed-d5 disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed-d<sub>5</sub> disodium
  • HY-149630
    VEGFR2/HDAC1-IN-1
    		Inducer
    VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect.
    VEGFR2/HDAC1-IN-1
  • HY-183753
    LC-TD-05
    		Inducer
    LC-TD-05 is a non-covalent inhibitor of TEAD1, TEAD2 and TEAD4, with IC50 values of 116.6 nM, 168.7 nM and 68.3 nM, respectively; it shows weak activity against TEAD3, with a human IC50 of 1261.0 nM. LC-TD-05 induces apoptosis in hepatocellular carcinoma cells. LC-TD-05 can be used for the research of hepatocellular carcinoma.
    LC-TD-05
  • HY-172094
    AMPK-IN-6
    		Inducer
    AMPK-IN-6 (compound 13a) is potent AMPK inhibitor with an IC50 value of 0.093 µM. AMPK-IN-6 induces apoptosis and inhibits autophagy. AMPK-IN-6 shows antiproliferative activity. AMPK-IN-6 has the potential for the research of pulmonary arterial hypertension.
    AMPK-IN-6
  • HY-181174
    Antioxidant agent-22
    Antioxidant agent-22 is a paraben derivative tetracyclic spermine cyclotriphosphazene compound. Antioxidant agent-22 exhibits antioxidant, anti-Inflammatory, and apoptotic activities. Antioxidant agent-22 significantly upregulates CAT, SOD, caspase-3 and IL-6 expression, suppresses GSH, IL-1β, and reduces BCL-2 and BAX levels. Antioxidant agent-22 can be used for the research of cancer, such as lung cancer.
    Antioxidant agent-22
  • HY-19471
    (rac)-ZK-304709
    		Inducer
    (rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET.
    (rac)-ZK-304709
  • HY-181477
    ERK5-IN-7
    		Inducer
    ERK5-IN-7 is an orally active ERK5 inhibitor with an IC50 of 403.4 nM. ERK5-IN-7 directly inhibits ERK5 kinase activity, and downregulates the phosphorylation level and total protein expression of ERK5. ERK5-IN-7 induces Apoptosis (upregulates Bax, downregulates Bcl-2, and induces Caspase-3 cleavage). ERK5-IN-7 induces ROS accumulation. ERK5-IN-7 exhibits anticancer effects against Lewis lung cancer.
    ERK5-IN-7
Cat. No. Product Name / Synonyms Application Reactivity