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-179615
    Entadamide A-CO-C12
    		Inducer
    Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer.
    Entadamide A-CO-C12
  • HY-144394
    Antitumor agent-45
    		Inducer
    Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells.
    Antitumor agent-45
  • HY-185584
    OKI-005
    		Inducer
    OKI-005 is an orally active inhibitor of Class I HDACs, with primary targeting of HDAC1, HDAC2 and HDAC3. OKI-005 is a prodrug of OKI-006 (HY-144893). OKI-005 increases histone acetylation levels, induces apoptosis and inhibits cancer cell proliferation. OKI-005 can be used in research related to triple-negative breast cancer and colorectal cancer.
    OKI-005
  • HY-174382
    ROR1-IN-3
    		Inducer
    ROR1-IN-3 (Compound 24d) is a potent and highly selective ROR1 kinase inhibitor (IC50 = 17.6 nM). ROR1-IN-3 demonstrates robust antitumor activity and inhibitory effect against ROR1 both in vitro and in vivo. ROR1-IN-3 has robust antiproliferative efficacy in vitro and in vivo. ROR1-IN-3 induces apoptosis in cancer cell lines. ROR1-IN-3 inhibits ROR1 downstream AKT/mTOR and NF-κB signaling pathway. ROR1-IN-3 can be studied in antitumor research.
    ROR1-IN-3
  • HY-P3906
    Melittin free acid
    		Inducer
    Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways.
    Melittin free acid
  • HY-176481
    ML-20
    		Inducer
    ML-20, Malabaricone C (HY-N8518) analogue, is a autophagy inhibitor and radiosensitizer. ML-20 inhibits cell growth, induces cell apoptosis . ML-20 induces DNA double-strand breaks, loss of mitochondrial membrane potential (MMP), and lysosomal membrane permeabilization (LMP). ML-20 induces endoplasmic reticulum stress and concurrent inhibition of autophagy flux due to LMP .
    ML-20
  • HY-149343
    Anticancer agent 132
    		Inducer
    Anticancer agent 132 (compound Rh1) is an inducer of apoptosis and autophagy with antitumor and antimetastasis activity. Anticancer agent 132 arrests cell cycle and inhibits cell proliferation.
    Anticancer agent 132
  • HY-W705820
    (±)-Enterodiol-d6
    (±)-Enterodiol-d6 is the deuterium labeled (±)-Enterodiol (HY-108695B). (±)-Enterodiol is the racemate of Enterodiol (HY-108695). Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Enterodiol has anti-cancer activities.
    (±)-Enterodiol-d<sub>6</sub>
  • HY-175002
    PI3Kδ-IN-24
    		Inducer
    PI3Kδ-IN-24 is a selective PI3Kδ inhibitor (IC50 = 0.1 nM). PI3Kδ-IN-24 exhibits significant antiproliferative effects against PI3Kδ-overexpressing cancer cell lines. PI3Kδ-IN-24 reduces p-AKT levels and induces cell cycle arrest and apoptosis in tumor cells. PI3Kδ-IN-24 is useful in cancer research, such as diffuse large B-cell lymphoma (DLBCL).
    PI3Kδ-IN-24
  • HY-147670
    TPB15
    		Inducer
    TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity.
    TPB15
  • HY-115718B
    PZ703b hydrochloride
    		Inducer 99.18%
    PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research.
    PZ703b hydrochloride
  • HY-179734
    PROTAC BRD4 Degrader-41
    		Inducer
    PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc.
    PROTAC BRD4 Degrader-41
  • HY-143462
    c-Met/HDAC-IN-2
    		Inducer
    c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance.
    c-Met/HDAC-IN-2
  • HY-156470
    Multi-kinase-IN-6
    		Inducer
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
    Multi-kinase-IN-6
  • HY-162751
    Anticancer agent 249
    		Inducer
    Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice.
    Anticancer agent 249
  • HY-138846
    Thalidomide-NH-C8-NH2
    		Inducer
    Thalidomide-NH-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-C8-NH2
  • HY-171682
    Anti-CCL2 (Carlumab)-McMMAF
    		Inducer
    Anti-CCL2 (Carlumab)-McMMAF is an antibody-drug conjugate (ADC) consisting of the humanized anti-CCL2 (chemokine ligand 2) antibody Carlumab (HY-P99188) conjugated to the protective group maleimidocaproyl and the tubulin inhibitor MMAF (HY-15579). The ADC toxic molecule and linker part are McMMAF (HY-15578). Anti-CCL2 (Carlumab)-McMMAF induces apoptosis and can be used in cancer research.
    Anti-CCL2 (Carlumab)-McMMAF
  • HY-181800
    SHP2-IN-47
    		Inducer
    SHP2-IN-47 is a selective and potent SHP2 inhibitor with an IC50 of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2E76K (IC50 = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia.
    SHP2-IN-47
  • HY-179501
    PDK1-IN-5
    		Inducer
    PDK1-IN-5 is a selective PDK1 inhibitor. PDK1-IN-5 activaties PDH by diminishing phosphorylation level via PDK1 inhibition. PDK1-IN-5 effectively reverses the Warburg effect and shifts cellular energy metabolism from glycolysis toward oxidative phosphorylation by increased acetyl-CoA, reduced lactate, elevated mitochondrial ROS, and subsequent induction of apoptosis. PDK1-IN-5 robustly inhibits tumor growth in vivo without inducing systemic toxicity. PDK1-IN-5 can be used for lung adenocarcinoma, human non-small cell lung adenocarcinoma and gastric colorectal.
    PDK1-IN-5
  • HY-N0718R
    Valepotriate (Standard)
    		Inducer
    Valepotriate (Standard) is the analytical standard of Valepotriate. This product is intended for research and analytical applications. Valepotriate can be isolated from Valeriana jatamansi Jones, has anti-epileptic and anti-cancer activities.
    Valepotriate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity