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-183549
    Ferroptosis/apoptosis inducer-4
    		Inducer
    Ferroptosis/apoptosis inducer-4 is a pyridine-hydrazone-derived Cu (II) complex and a synergistic inducer of ferroptosis and apoptosis. Ferroptosis/apoptosis inducer-4 exerts anti-tumor proliferation and anti-metastasis effects with extremely low systemic toxicity. Ferroptosis/apoptosis inducer-4 disrupts cellular redox homeostasis by depleting glutathione and generating hydroxyl radicals through the Cu2+/Cu+ redox cycle. Ferroptosis/apoptosis inducer-4 also triggers mitochondrial dysfunction and endoplasmic reticulum stress, which in turn lead to Ca2+ release, mitochondrial Ca2+ overload, and the formation of a ROS−Ca2+ self-amplifying feedback loop. Ferroptosis/apoptosis inducer-4 can be used in studies related to cervical cancer.
    Ferroptosis/apoptosis inducer-4
  • HY-B0174AS
    Olsalazine-13C6
    		Inducer
    Olsalazine-13C6 is the 13C labeled Olsalazine (HY-B0174A). Olsalazine is an orally active prodrug of 5-ASA (HY-15027). Olsalazine can inhibit cells proliferation and induce apoptosis. Olsalazine can reduce DAI and MPO activity and inhibit inflammatory cytokines levels. Olsalazine can be used for the researches of cancer, inflammation and metabolic disease, such as colorectal cancer, inflammatory bowel disease (IBD) and hyperuricemic.
    Olsalazine-<sup>13</sup>C<sub>6</sub>
  • HY-P992437
    PF-03475952
    		Inducer
    PF-03475952 is a fully human IgG2 monoclonal antibody targeting CD44. PF-03475952 binds an epitope in CD44’s constant exons, blocks CD44-hyaluronic acid interaction, reduces cell surface CD44, and does not cross-react with rodent CD44 or LYVE-1. PF-03475952 induces cancer cell apoptosis, inhibits LPS (HY-D1056)-induced leukocyte cytokine release and cancer metastasis, and reduces CD44 expression on circulating CD3+ lymphocytes in cynomolgus monkeys. PF-03475952 can be used for the research of rheumatoid arthritis and hepatocellular carcinoma.
    PF-03475952
  • HY-G0017A
    N-Desmethyl imatinib mesylate
    		Inducer
    N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia.
    N-Desmethyl imatinib mesylate
  • HY-175230
    ZG-2492
    		Inducer
    ZG-2492 is an orally active LDHA inhibitor with an IC50 of 156 nM. ZG-2492 can reduce lactate production and induce cell cycle arrest and apoptosis in pancreatic cancer cells . ZG-2492 has antitumor activity and can be used in the research of tumors such as pancreatic cancer.
    ZG-2492
  • HY-181996
    BTK-IN-47
    		Activator
    BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies.
    BTK-IN-47
  • HY-N16066
    Candidusin A
    		Inducer
    Candidusin A (CHNQD-0803) (Compound 4) is a AMPK activator with a KD of 47.28 nM. Candidusin A can be isolated from marine fungus Aspergillus candidus. Candidusin A has cytotoxic activity and induces apoptosis in human prostate cancer cells (22Rv1, PC-3 and LNCaP cells). Candidusin A reduces adipogenesis genes expression and fat deposition, negatively regulates the NF-κB-TNFα inflammatory axis to suppress inflammation, and ameliorates liver injury and fibrosis. Candidusin A can be used for non-alcoholic steatohepatitis (NASH) research.
    Candidusin A
  • HY-14291S1
    Vildagliptin-d7
    		Inhibitor
    Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.
    Vildagliptin-d<sub>7</sub>
  • HY-105409
    Discodermolide
    		Inducer
    Discodermolide (NVP-XAA-296) is a potent microtubule-stabilizing agent with a Ki of 0.4 μM. Discodermolide stabilizes microtubules, induces G2 or M phase cell cycle arrest and apoptosis, leading to inhibition of cancer cell proliferation. Discodermolide competitively inhibits the binding of Paclitaxel (HY-B0015) to tubulin polymers, and inhibits the growth of Paclitaxel-resistant cells. Discodermolide can be used for breast and colon cancer research.
    Discodermolide
  • HY-184116
    A2AR/EGFR-IN-1
    		Inducer
    A2AR/EGFR-IN-1 is a dual A2AR/EGFR inhibitor, with an IC50 of 0.037 μM against A2AR and an IC50 of 8.37 μM against EGFR. A2AR/EGFR-IN-1 induces cell cycle arrest at S and G2/M phases. A2AR/EGFR-IN-1 upregulates the expression of TP53, Caspase3 and Bax, downregulates the expression of Bcl2, and promotes cell Apoptosis. A2AR/EGFR-IN-1 restores colon crypt structure in an azoxymethane (HY-111375)-induced colorectal cancer model in vivo. A2AR/EGFR-IN-1 can be used for research related to colorectal cancer.
    A2AR/EGFR-IN-1
  • HY-179165
    Gαq/11 protein-IN-2
    		Inducer
    Gαq/11 protein-IN-2 (Compound 9g) is a Gαq/11 protein inhibitor, with an IC50 of 11.3 μM. Gαq/11 protein-IN-2 induces Apoptosis, increases p-YAP. Gαq/11 protein-IN-2 has anticancer activity against uveal melanoma.
    Gαq/11 protein-IN-2
  • HY-160777A
    VNPP433-3β dihydrochloride
    		Inducer
    VNPP433-3β (Galeterone 3β-imidazole) dihydrochloride is an orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β dihydrochloride induces cell apoptosis. VNPP433-3β dihydrochloride inhibits tumor growth in the CWR22Rv1 xenograft mouse model. VNPP433-3β dihydrochloride can be used for the study of castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC).
    VNPP433-3β dihydrochloride
  • HY-134985A
    Thalidomide-NH-PEG1-NH2 diTFA
    		Inducer
    Thalidomide-NH-PEG1-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-PEG1-NH2 diTFA
  • HY-173232
    VEGFR-2-IN-66
    		Inducer
    VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 value of 0.509 µM and an IC50 value of 7.48 μM for inhibiting the proliferation of MCF-7 cells. VEGFR-2-IN-66 exerts its anti-cancer activity by arresting the cell cycle, inducing apoptosis, and regulating gene expression, and can be used in the research of the breast cancer field.
    VEGFR-2-IN-66
  • HY-172394
    ZSNI-21
    		Inducer
    ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC50 0.939 μM and HDAC2 IC50 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer.
    ZSNI-21
  • HY-151428
    Antitumor agent-78
    		Inducer
    Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells.
    Antitumor agent-78
  • HY-149291
    ATM Inhibitor-7
    		Inducer
    ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity.
    ATM Inhibitor-7
  • HY-P10433
    EGFRvIII peptide
    		Inducer
    EGFRvIII peptide is an EGFRvIII-derived epitope for binding to MHC I molecules. EGFRvIII peptide induces apoptosis, and causes specific immune responses against glioblastoma, especially in combination with Flagellin B.
    EGFRvIII peptide
  • HY-W012875R
    3-Nitropropanoic acid (Standard)
    		Inducer
    3-Nitropropanoic acid (Standard) is the analytical standard of 3-Nitropropanoic acid. This product is intended for research and analytical applications. 3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible and orally active inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM. 3-Nitropropanoic acid can induce cell apoptosis[1][2].
    3-Nitropropanoic acid (Standard)
  • HY-W584522
    Thalidomide-4-NH-PEG1-COO(t-Bu)
    		Inducer
    Thalidomide-4-NH-PEG1-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG1-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG1-COO(t-Bu)
Cat. No. Product Name / Synonyms Application Reactivity