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-N17440
    2-Methoxyjuglone
    Inducer
    2-Methoxyjuglone, a naphthoquinone, is an apoptosis inducer. 2-Methoxyjuglone activates caspase-9 and caspase-3 via the mitochondrial cytochrome c-dependent intrinsic apoptosis cascade. 2-Methoxyjuglone increases pro-apoptotic Bax levels, decreases anti-apoptotic Bcl-2 levels, and promotes mitochondrial cytochrome c release. 2-Methoxyjuglone induces apoptosis morphological features, early apoptosis, S-phase and G2/M-phase cell cycle arrest, and DNA double-strand breaks. 2-Methoxyjuglone exerts activity against Gram-positive bacteria, pathogenic fungi, and phytopathogenic fungi. 2-Methoxyjuglone can be used for the research of hepatocellular carcinoma, osteosarcoma, colon adenocarcinoma, breast cancer, fungal infection, bacterial infection.
    2-Methoxyjuglone
  • HY-183546
    TDP1-IN-6
    Inducer
    TDP1-IN-6 is a TDP1 inhibitor with an IC50 of 1.52 μM. Combination of TDP1-IN-6 with Topotecan (HY-13768) enhances DNA damage, induces Apoptosis, triggers S-phase cell cycle arrest, and promotes Ferroptosis. TDP1-IN-6 can be used for the research of cervical cancer.
    TDP1-IN-6
  • HY-182747
    HDAC6-IN-79
    Inducer
    HDAC6-IN-79 is a HDAC6 inhibitor with an IC50 of 98.40 nM, and it also exhibits inhibitory activity against other HDAC subtypes (HDAC1: 639.0 nM, HDAC2: 798.9 nM, HDAC8: 865.7 nM, HDAC4: 1187 nM). HDAC6-IN-79 induces acetylation of α-tubulin and histone H3, reduces the viability of cancer cells, activates the autophagy pathway and induces apoptosis. HDAC6-IN-79 can be used for research related to urothelial carcinoma (bladder cancer).
    HDAC6-IN-79
  • HY-178961
    PROTAC ERα Degrader-13
    Inducer
    PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research.
    PROTAC ERα Degrader-13
  • HY-P991656
    LY-2624587
    Inducer
    LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research.
    LY-2624587
  • HY-181629
    ZSTK3744
    Inducer
    ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.
    ZSTK3744
  • HY-N0168S
    Hesperetin-d3
    Hesperetin-d3 is the deuterium labeled Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin regulates apoptosis.
    Hesperetin-d<sub>3</sub>
  • HY-N1639
    1-Decarboxy-3-oxo-ceanothic acid
    Inducer
    1-Decarboxy-3-oxo-ceanothic acid is an anticancer agent. 1-Decarboxy-3-oxo-ceanothic acid inhibits DNA synthesis. 1-Decarboxy-3-oxo-ceanothic acid induces Apoptosis.
    1-Decarboxy-3-oxo-ceanothic acid
  • HY-149029
    TH-6
    Inducer
    TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity.
    TH-6
  • HY-175836
    CYP1B1-IN-12
    Inducer
    CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC).
    CYP1B1-IN-12
  • HY-D1267
    PAO-Nap
    Inducer
    PAO-Nap is the modified PAO attached a naphthalimide fluorophore using aminocaproic acid as a linker. PAO induces oxidative stress-mediated apoptosis in HL-60 cells by selectively targeting thioredoxin reductase.
    PAO-Nap
  • HY-P4157A
    FOXO4-DRI acetate
    Inducer
    FOXO4-DRI acetate is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI acetate is a senolytic peptide that induces apoptosis of senescent cells.
    FOXO4-DRI acetate
  • HY-12440
    HM90822
    Inducer
    HM90822 is an orally active IAP antagonist. HM90822 induces ubiquitination and proteasome-dependent degradation of XIAP, cIAP1 and cIAP2 in sensitive pancreatic cancer cells. HM90822 induces Apoptotic cell death. HM90822 inhibits tumor growth in Panc-1 pancreatic cancer xenograft and orthotopic mouse models. HM90822 can be used for the research of pancreatic cancer.
    HM90822
  • HY-W011404R
    Tributyrin (Standard)
    Inducer
    Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed proagent of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
    Tributyrin (Standard)
  • HY-172795
    EGFR-IN-158
    Inducer
    EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis.
    EGFR-IN-158
  • HY-158233
    Apoptotic agent-4
    Inducer
    Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases.
    Apoptotic agent-4
  • HY-179633
    ZLMT-72
    Inducer
    ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC).
    ZLMT-72
  • HY-P991914
    FTL004
    Activator
    FTL004 is an anti-CD38 monoclonal antibody. FTL004 exhibits enhanced Proapoptotic activity and displays stronger ADCC against CD38+ malignant cells. FTL004 can be used for the research of multiple myeloma and non-Hodgkin lymphoma[1].
    FTL004
  • HY-N12534
    Monaspin B
    Inducer
    Monaspin B is a natural product produced by the co-culture of Monascus purpureus and Aspergillus oryzae. Monaspin B exerts anti-proliferation activity by inducing apoptosis of HL-60 cells, IC50 160 nM. Monaspin B has antitumor activity.
    Monaspin B
  • HY-N0667S1
    L-Asparagine-15N2,d8
    L-Asparagine-15N2,d8 is the 15N- and deuterium labeled L-Asparagine (HY-N0667). L-Asparagine is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia.
    L-Asparagine-<sup>15</sup>N<sub>2</sub>,d<sub>8</sub>
Cat. No. Product Name / Synonyms Application Reactivity