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-N0415S1
    Trigonelline-d3-1 chloride
    Trigonelline-d3-1 chloride (Trigonelline-d3-1 hydrochloride) is the deuterium labeled Trigonelline chloride (HY-N0415). Trigonelline chloride is an alkaloid with potential antidiabetic activity that can be isolated from Trigonella foenum-graecum L or Leonurus artemisia. Trigonelline chloride is a potent Nrf2 inhibitor that blocks Nrf2-dependent proteasome activity, thereby enhancing apoptosis in pancreatic cancer cells. Trigonelline chloride also has anti-HSV-1, antibacterial, and antifungal activity, and induces ferroptosis.
    Trigonelline-d<sub>3</sub>-1 chloride
  • HY-W714183
    Dinitramine
    		Inducer
    Dinitramine is a herbicide. Dinitramine activates the Erk/P38/JNK/MAPK pathway and inactivates the PI3k/Akt pathway in testicular cells. Dinitramine induces endoplasmic reticulum stress, dysregulation of calcium homeostasis in the cytoplasm and mitochondria, apoptosis, and downregulated expression of cell cycle genes in testicular cells. Dinitramine reduces the viability and proliferation capacity of testicular cells, and inhibits cell division by suppressing the synthesis of tubulin. Dinitramine induces abnormal heart development, inhibited angiogenesis, inflammatory responses, apoptosis, and impaired embryonic growth in zebrafish embryos.
    Dinitramine
  • HY-182044
    MRTX849-amide-C4-(o)-carborane
    		Inducer
    MRTX849-amide-C4-(o)-carborane is a KRASG12C inhibitor with mutation selectivity for cells expressing KRASG12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRASG12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRASG12C-positive cancers.
    MRTX849-amide-C4-(o)-carborane
  • HY-163692
    Tubulin polymerization-IN-64
    		Inducer
    Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549.
    Tubulin polymerization-IN-64
  • HY-17412AS
    Minocycline-d6
    		Inducer
    Minocycline-d6 is deuterium labeled Minocycline (HY-17412A). Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.
    Minocycline-d<sub>6</sub>
  • HY-179103
    PLK4-IN-5
    		Inducer
    PLK4-IN-5 (compound 5f) is a PLK4 (IC50 = 0.8 nM) inhibitor. PLK4-IN-5 can inhibit MCF-7 cell clone formation, induce cell cycle arrest (S/G2 phase), and apoptosis. PLK4-IN-5 has anti proliferative activity against MCF-7 cells (IC50 = 0.48 μM). PLK4-IN-5 can be used in the research of cancer such as breast cancer.
    PLK4-IN-5
  • HY-156165
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
    		Inducer
    Thalidomide-5-NH-PEG3-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG3-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
  • HY-135746S
    OR-1896-d3
    OR-1896-d3 is the deuterium labeled OR-1896 (HY-135746). OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
    OR-1896-d<sub>3</sub>
  • HY-163740
    VEGFR-2-IN-46
    		Inducer
    VEGFR-2-IN-46 (compound 4d) is a potent VEGFR-2 inhibitor with an EC50 value of 67.0 nM. VEGFR-2-IN-46 shows cytotoxicity and induces cell cycle arrest at the G2/M phase. VEGFR-2-IN-46 induces necrosis and apoptosis.
    VEGFR-2-IN-46
  • HY-175481
    CB2R agonist 4
    		Inducer
    CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. CB2R agonist 4 can induce cell apoptosis, ROS production and protein misfolding. CB2R agonist 4 shows cytotoxicity to a panel of tumor cell lines. CB2R agonist 4 can be used for the research of cancer.
    CB2R agonist 4
  • HY-183987
    ZINC000002107582
    		Inducer
    ZINC000002107582 is a UVRAG binder. ZINC000002107582 induces Apoptosis, increases intracellular ROS levels, arrests the cell cycle at the S phase, and elevates the proportion of cells in the Sub G0 phase. ZINC000002107582 exhibits anticancer activity against breast cancer.
    ZINC000002107582
  • HY-138849
    Thalidomide-NH-amido-C2-NH2
    		Inducer
    Thalidomide-NH-amido-C2-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-amido-C2-NH2
  • HY-136718
    CLEFMA
    		Activator 98.03%
    CLEFMA is a curcuminoid with antitumor activity. CLEFMA inhibits tumor growth is associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.
    CLEFMA
  • HY-N15686
    Torulene
    		Agonist
    Torulene (Torulin) is an orally active carotenoid with anti-cancer activity. Torulene inhibits proliferation and induces apoptosis of tumor cells via a mitochondrial signal pathway and the down-regulation of androgen receptor (AR) expression. Torulene can be used for the study of prostate cancer.
    Torulene
  • HY-178351
    HDAC6-IN-67
    		Inducer
    HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.
    HDAC6-IN-67
  • HY-181723
    Anticancer agent 304
    		Inducer
    Anticancer agent 304 is an anticancer agent. Anticancer agent 304 binds to CDC45 with a Kd value of 83.0 μM. Anticancer agent 304 arrests the cell cycle of liver cancer cells at the G2/M phase, induces Apoptosis by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2, and inhibits the migration, invasion and proliferation of liver cancer cells. Anticancer agent 304 suppresses tumor growth in animal models of hepatocellular carcinoma. Anticancer agent 304 is applicable to research related to liver cancer.
    Anticancer agent 304
  • HY-146254
    hCAIX-IN-12
    		Inducer
    hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 μM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
    hCAIX-IN-12
  • HY-181863
    Nampt-IN-18
    		Inducer
    Nampt-IN-18 (Compound Q24) is an orally active NAMPT inhibitor with an IC50 of 8.0 nM against hNAMPT. Nampt-IN-18 inhibits NAMPT enzymatic activity. Nampt-IN-18 inhibits DNA synthesis and induces Apoptosis. Nampt-IN-18 exhibits anticancer activity against gastric cancer and colorectal cancer. Nampt-IN-18 can be used for the research of gastrointestinal cancers.
    Nampt-IN-18
  • HY-N3000A
    6-Methoxydihydrosanguinarine hydrochloride
    		Inducer
    6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.
    6-Methoxydihydrosanguinarine hydrochloride
  • HY-W752724
    Flunisolide-d4
    Flunisolide-d4 is the deuterium labeled Flunisolide (HY-B1121). Flunisolide is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity