1. Signaling Pathways
  2. Apoptosis
  3. Apoptosis

Apoptosis

Apoptosis

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-P11354
    THR-123
    Inhibitor
    THR-123 is an orally active ALK3 peptide agonist. THR-123 has a relatively weak binding to ALK2, but does not bind to ALK6. THR-123 suppresses inflammation, apoptosis and the epithelial-to-mesenchymal transition program and reverses established fibrosis in five mouse models of acute and chronic renal injury. THR-123 can be used for the study of kidney fibrosis.
    THR-123
  • HY-B1622S
    Cyproheptadine-d3
    Cyproheptadine-d3 is deuterium labeled Cyproheptadine.
    Cyproheptadine-d<sub>3</sub>
  • HY-130624
    Hsp90-Cdc37-IN-2
    Inducer
    Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549.
    Hsp90-Cdc37-IN-2
  • HY-170543
    Dual Galectin-3/EGFR-IN-1
    Inducer
    Dual Galectin-3/EGFR-IN-1 (Compound 29) is the dual inhibitor for Galectin-3 and EGFR with the KD of 52.29 μM and 3.31 μM. Dual Galectin-3/EGFR-IN-1 inhibits TGF-β-induced hepatic stellate cell (HSCs) activation, induces apoptosis in LX-2 cell, and exhibits anti-liver fibrotic efficacy.
    Dual Galectin-3/EGFR-IN-1
  • HY-161647
    Antitumor agent-156
    Inducer
    Antitumor agent-156 (Compound 20) causes DNA damage and mitochondrial dysfunction, promotes reactive oxygen species generation, activates endoplasmic reticulum stress, and induce apoptosis, autophagy and ferroptosis. Antitumor agent-156 shows superior antitumor activity against cancer cells including Cisplatin (HY-17394) resistance cells. Antitumor agent-156 displayS good liver-targeting ability.
    Antitumor agent-156
  • HY-179386
    PARP1/EZH2-IN-1
    Inducer
    PARP1/EZH2-IN-1 is a selective PARP1 and EZH2 dual inhibitor. PARP1/EZH2-IN-1 has IC50s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and EZH2, respectively. PARP1/EZH2-IN-1 inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research.
    PARP1/EZH2-IN-1
  • HY-16322S
    Minodronic acid-d4
    Inducer
    Minodronic acid-d4 (YM-529-d4) is deuterium labeled Minodronic acid (HY-16322). Minodronic acid (YM-529) is an FPP synthase inhibitor with an IC50 of 3 nM, and also an antagonist of P2X2/3 receptors with an IC50 of 62.7 μM. Minodronic acid induces tumor cell apoptosis and inhibits cell growth. Minodronic acid also suppresses bone resorption. Minodronic acid can be used in research related to osteoporosis and cancer.
    Minodronic acid-d<sub>4</sub>
  • HY-181483
    CDK6-IN-2
    Inducer
    CDK6-IN-2 is a CDK6 covalent inhibitor with an IC50 of 0.013 μM. CDK6-IN-2 inhibits the proliferation and migration of triple-negative breast cancer cells, and induces cell cycle arrest and apoptosis. CDK6-IN-2 induces ROS accumulation and mitochondrial damage through cellular metabolic reprogramming. CDK6-IN-2 exhibits anti-tumor activity and can be used for the research of triple-negative breast cancer.
    CDK6-IN-2
  • HY-161970
    XSJ05
    Inducer
    XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis.
    XSJ05
  • HY-146392
    HDAC-IN-39
    Inducer
    HDAC-IN-39 (compound 16c) is a potent HDAC inhibitor, with IC50 values of 1.07 μM (HDAC1), 1.47 μM (HDAC2), and 2.27 μM (HDAC3), respectively. HDAC-IN-39 also significantly inhibits microtubule polymerization. HDAC-IN-39 induces cell cycle arrest at the G2/M phase. HDAC-IN-39 displays promising anticancer activity against resistant cancer cells.
    HDAC-IN-39
  • HY-173314
    EGFR-IN-155
    Inducer
    EGFR-IN-155 (compound 13a) is an EGFR inhibitor with IC50 values of 0.14 nM and 0.18 nM against EGFR TK and EGFR L858R, respectively. EGFR-IN-155 inhibits tumor growth, causes a cell cycle arrest at S phase, and and induces cell apoptosis.
    EGFR-IN-155
  • HY-161345
    Meriolin 16
    Inducer
    Meriolin 16 can induce cell apoptosis in rapid kinetics (within 2-3 h) with the IC50 of 50 nM.
    Meriolin 16
  • HY-116267
    MHY219
    Inducer
    MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer.
    MHY219
  • HY-P992200
    Anti-CD146 Antibody (AA98)
    Inducer
    Anti-CD146 Antibody (AA98) is an antibody targeting CD146 and an angiogenesis inhibitor. Anti-CD146 Antibody (AA98) blocks the dimerization of CD146 as well as its downstream PI3K/AKT, p38 MAPK and NF-κB signaling pathways; it inhibits the expression of MMP9 and ICAM1, epithelial-mesenchymal transition (EMT), and the proliferation, migration and tube formation of endothelial cells. Anti-CD146 Antibody (AA98) enhances radiation-induced cancer cell apoptosis and survival inhibition, reduces tumor microvessel density, and suppresses tumor growth, invasion and vasculogenic mimicry. Anti-CD146 Antibody (AA98) can be used in research related to cervical cancer, liver cancer, malignant phyllodes tumor of the breast, uveal melanoma, leiomyosarcoma, pancreatic cancer, other tumors and angiogenesis.
    Anti-CD146 Antibody (AA98)
  • HY-143472
    PI3Kδ-IN-11
    Inducer
    PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies.
    PI3Kδ-IN-11
  • HY-163288
    EZH2/HSP90-IN-29
    Inducer
    EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).
    EZH2/HSP90-IN-29
  • HY-180827
    VEGFR-2-IN-79
    Inducer
    VEGFR-2-IN-79 (Compound 17) is a VEGFR-2 inhibitor with an IC50 of 2.32 μM. VEGFR-2-IN-79 exhibits potent and broad-spectrum cytotoxicity and can induce apoptosis in MCF-7 cells. VEGFR-2-IN-79 does not cause a significant decrease in the mitochondrial membrane potential of MCF-7 cells. VEGFR-2-IN-79 can be used for research on breast cancer.
    VEGFR-2-IN-79
  • HY-173040
    Anticancer agent 266
    Inducer
    Anticancer agent 266 (Compound 3B) is an anticancer agent that can inhibit the proliferation of tumor cells. Anticancer agent 266 has an IC50 of 0.13 μM for MCF-7 breast cancer cell line.
    Anticancer agent 266
  • HY-N19727
    Chamissonolide
    Inhibitor
    Chamissonolide is a sesquiterpene lactone with cytotoxic, anti-inflammatory and trypanocidal activities. Chamissonolide reduces the mRNA levels of IL-2, IFN-γ, GM-CSF, iNOS and TNF-α, and upregulates the mRNA level of NF-ATc. Chamissonolide decreases the population of naturally occurring apoptotic cells. Chamissonolide can be used in research related to tumors, African trypanosomiasis and Chagas disease.
    Chamissonolide
  • HY-P10870
    Pep1-DNP conjugate 9
    Inducer
    Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models.
    Pep1-DNP conjugate 9
Cat. No. Product Name / Synonyms Application Reactivity