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-124617
    AMXT-1501
    		Inducer 98.17%
    AMXT1501 is a novel inhibitor of the polyamine transport system. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells.
    AMXT-1501
  • HY-14933
    Prinaberel
    		Inducer 98.05%
    Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.
    Prinaberel
  • HY-18741
    VR23
    		Inducer 99.58%
    VR23 is a small molecule that potently inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
    VR23
  • HY-131717
    Thalidomide-NH-CH2-COOH
    		Inducer 98.07%
    Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
    Thalidomide-NH-CH2-COOH
  • HY-103706
    ROC-325
    		Inducer 99.61%
    ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
    ROC-325
  • HY-109117
    Iadademstat
    		Inducer 99.82%
    Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research.
    Iadademstat
  • HY-14806A
    Teneligliptin hydrobromide
    		Inhibitor 99.99%
    Teneligliptin (MP-513) hydrobromide is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin hydrobromide
  • HY-13203
    NVP-TAE 226
    		Inducer 99.77%
    NVP-TAE 226 (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively. NVP-TAE 226 (TAE226) also effectively inhibits Pyk2 and insulin receptor (InsR) with IC50s of 3.5 nM and 44 nM, respectively.
    NVP-TAE 226
  • HY-100653
    AZD5153
    		Inducer 99.20%
    AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC50 of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma.
    AZD5153
  • HY-114317
    MARK4 inhibitor 1
    		Inducer 98.29%
    MARK4 inhibitor 1 is a potent and selective microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
    MARK4 inhibitor 1
  • HY-134463
    NHWD-870
    		Inducer 99.36%
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
    NHWD-870
  • HY-P99730
    Mezagitamab
    		Inducer 99.76%
    Mezagitamab (TAK-079) is a IgG1λ anti-CD38 monoclonal antibody. Mezagitamab depletes tumor cells expressing CD38 through antibody and complement dependent cytotoxicity. Mezagitamab has potential application in relapsed/refractory multiple myeloma (RRMM) and idiopathic thrombocytopenic purpura (ITP).
    Mezagitamab
  • HY-133121
    WDR5-IN-1
    		Inducer ≥98.0%
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
    WDR5-IN-1
  • HY-12660
    MPI-0479605
    		Inducer 99.54%
    MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC50 of 1.8 nM.
    MPI-0479605
  • HY-125858
    MI-1061
    		Activator 99.72%
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
    MI-1061
  • HY-13960
    GSK1324726A
    		Inducer 99.75%
    GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
    GSK1324726A
  • HY-110228
    Metformin-d6 hydrochloride
    		Inhibitor 98.79%
    Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
    Metformin-d<sub>6</sub> hydrochloride
  • HY-108639
    MIRA-1
    		Inducer 99.76%
    MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity.
    MIRA-1
  • HY-N0222
    Avicularin
    		Inducer 99.80%
    Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities.
    Avicularin
  • HY-13680
    Meisoindigo
    		Inducer 99.91%
    Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity.
    Meisoindigo
Cat. No. Product Name / Synonyms Application Reactivity