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-146217
    MMP-9-IN-4
    		Inducer
    MMP-9-IN-4 is a MMP-9 inhibitor (IC50: 7.46 nM) that has H-π interactions with MMP-9. MMP-9-IN-4 also inhibits AKT activity (IC50: 8.82 nM). MMP-9-IN-4 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-4 can be used in the research of cancers.
    MMP-9-IN-4
  • HY-149566
    Thalidomide-5-O-C9-NH2 hydrochloride
    		Inducer 99.59%
    Thalidomide-5-O-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C9-NH2 hydrochloride
  • HY-123542
    ONO-3403
    		Inducer
    ONO-3403 is an orally active serine protease inhibitor. ONO-3403 inhibits the production of TNF-α and nitric oxide induced by LPS. ONO-3403 inhibits the cell growth and induces the apoptosis, and has an antitumor effect on malignant tumors.
    ONO-3403
  • HY-178448
    EGFR-IN-178
    		Inducer
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-178
  • HY-149805
    Anticancer agent 110
    		Inducer
    Anticancer agent 110 is an anticancer agent with in vitro anticancer activity and excellent anti-leukemia potency. Anticancer agent 110 is highly cytotoxic to K-562 lineage chronic myelogenous leukemia cells at nanomolar concentrations. Anticancer agent 110 causes DNA damage and leads to apoptosis.
    Anticancer agent 110
  • HY-111636
    VSW1198
    		Inducer
    VSW1198 is an inhibitor for geranylgeranyl diphosphate synthase (GGDPS) with an IC50 of 45 nM. VSW1198 reveals antitumor activity in myeloma- and prostate cancer with liver toxicity.
    VSW1198
  • HY-147934
    HDAC8-IN-3
    		Inducer
    HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines.
    HDAC8-IN-3
  • HY-163923
    Apoptosis inducer 24
    		Inducer
    Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg).
    Apoptosis inducer 24
  • HY-168597
    FGFR1/VEGFR2-IN-3
    		Inducer
    FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis.
    FGFR1/VEGFR2-IN-3
  • HY-173492
    EGFR-IN-156
    		Inducer
    EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC50 values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC50 values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers.
    EGFR-IN-156
  • HY-138854A
    Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride
  • HY-169400
    HDACs/EZH2-IN-1
    		Activator
    HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis.
    HDACs/EZH2-IN-1
  • HY-183780
    FGFR-IN-27
    		Inducer
    FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC50 of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma.
    FGFR-IN-27
  • HY-147862
    EGFR-IN-62
    		Inducer
    EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines.
    EGFR-IN-62
  • HY-N0378S
    D-Mannitol-d8
    		Inducer
    D-Mannitol-d8 is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
    D-Mannitol-d<sub>8</sub>
  • HY-182288
    YN11
    		Inducer
    YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer.
    YN11
  • HY-124693
    DB1055
    		Inducer
    DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34+ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia[1].
    DB1055
  • HY-P11114
    Periplanetasin-4
    		Inhibitor
    Periplanetasin-4 is an antimicrobial peptide that can be derived from the American cockroach (Periplaneta americana). Periplanetasin-4 reduces cell rounding and apoptosis. Periplanetasin-4 blocks Clostridium difficile toxin A-induced ROS production and the activation of downstream p38 MAPK and p21. Periplanetasin-4 significantly increases mitochondrial calcium level, reduces DPH fluorescence intensity and vacuolar dysfunction in Candida albicans ATCC 90028 cells. Periplanetasin-4 significantly ameliorates toxin A-induced mucosal damage in the mouse gut. Periplanetasin-4 can be used for the study of colitis.
    Periplanetasin-4
  • HY-D0988A
    R-Phycoerythrin (concentrated solution)
    		Inducer
    R-Phycoerythrin (R-PE) (concentrated solution) is found in Heterosiphonia japonica. R-Phycoerythrin (concentrated solution) is an orange-red fluorescent probe with α, β, and γ subunits. R-Phycoerythrin (concentrated solution) can be used in photodynamic therapy (PDT) to induce apoptosis in tumor cells. R-Phycoerythrin (concentrated solution) can be used in fluorescence microscopy, flow cytometry, and immunofluorescence analysis (Ex/Em = 496/578 nm).
    R-Phycoerythrin (concentrated solution)
  • HY-19565
    KW-2450 tosylate
    		Inducer
    KW-2450 tosylate is an orally active Aurora A and B kinases, IGF-1R, and IR tyrosine kinases inhibitor. KW-2450 tosylate induces Apoptosis. KW-2450 tosylate also exhibits anticancer activity against triple-negative breast cancer.
    KW-2450 tosylate
Cat. No. Product Name / Synonyms Application Reactivity