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-107311
    Hederacholchiside E
    Hederacholchiside E (compound 6) is a kind of saponin. Hederacholchiside E can be isolated from the Anemone raddeana.
    Hederacholchiside E
  • HY-178112
    CDK2-IN-47
    Inducer
    CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer.
    CDK2-IN-47
  • HY-173228
    Anticancer agent 269
    Inducer
    Anticancer agent 269 (Compound 11c) is an orally active caspase-3 activator that promotes ROS generation by activating caspase-3, induces cancer cell apoptosis (Apoptosis), and exhibits significant anticancer activity. It can be used for research in the field of cancer.
    Anticancer agent 269
  • HY-159897
    PAK4-IN-5
    Inducer
    PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.).
    PAK4-IN-5
  • HY-P10285S
    d-KLA Peptide-d30
    d-KLA Peptide (D-(KLAKLAK)2)-d30 is the deuterium labeled d-KLA Peptide (HY-P10285). d-KLA Peptide, KLA peptide (HY-P5345) isomer, is a pro-apoptosis peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrial membrane. d-KLA Peptide increases caspase 3/7 activity, exerts proapoptotic activity and enhances antitumor efficacy in mouse melanoma models.
    d-KLA Peptide-d<sub>30</sub>
  • HY-176284
    OXPHOS-IN-2
    Inducer
    OXPHOS-IN-2 is an orally active OXPHOS inhibitor. OXPHOS-IN-2 exhibits potent inhibitory activity in PC9 (IC50 = 12.3 nM) and Bxpc-3 cells (IC50 = 250 nM in glucose medium, IC50 = 17.5 nM in galactose medium). OXPHOS-IN-2 decreases the NADH/NAD+ ratio and reduces ATP levels. OXPHOS-IN-2 induces tumor cells apoptosis by activating reactive oxygen species (ROS) and downregulating the level of Nrf2. OXPHOS-IN-2 can be used for research on cancer such as non-small cell lung cancer and pancreatic cancer.
    OXPHOS-IN-2
  • HY-163238
    Thalidomide-azetidine-CH-piperazineethanol
    Inducer
    Thalidomide-azetidine-CH-piperazineethanol is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-CH-piperazineethanol can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-CH-piperazineethanol
  • HY-152191
    ChoKα inhibitor-3
    Inducer
    ChoKα inhibitor-3 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-3 can inhibit HChoK α1 with an IC50 value of 0.66 μM. ChoKα inhibitor-3 also can induce apoptosis. ChoKα inhibitor-3 can be used for the research of cancer.
    ChoKα inhibitor-3
  • HY-122778R
    δ-Tocotrienol (Standard)
    Inducer
    δ-Tocotrienol (Standard) is the analytical standard of δ-Tocotrienol. This product is intended for research and analytical applications. δ-Tocotrienol is a Vitamin E in vegetables, fruits, seeds, nuts, grains and oils. Vitamin E has become well known for its role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
    δ-Tocotrienol (Standard)
  • HY-169096
    DPP-21
    Inducer
    DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax).
    DPP-21
  • HY-133222
    STX140
    Inducer
    STX140 is an orally active microtubule disruptor. STX140 induces apoptosis in the hormone-independent PC-3 prostate cell lines. STX140 has anti-angiogenic and anti-tumour activities.
    STX140
  • HY-149239
    Topo II/HDAC-IN-2
    Inducer
    Topo II/HDAC-IN-2 (8d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-2 (8d) induces apoptosis.
    Topo II/HDAC-IN-2
  • HY-149523
    Anticancer agent 157
    Inducer
    Anticancer agent 157 (compound 15) is a NO inhibitor (IC50=0.62 μg/mL) with anti-inflammatory and anticancer activities. Anticancer agent 157 can bind to iNOS (inducible NO synthase) and caspase 8, causing nuclear fragmentation and chromatin condensation, inducing apoptosis. Anticancer agent 157 inhibits HT29 colon cancer cells (IC50=2.45 μg/mL), Hep-G2 liver cancer cells (IC50=3.25 μg/mL), and B16-F10 murine melanoma cells (IC50=3.84 μg/mL).
    Anticancer agent 157
  • HY-B0011AR
    Docetaxel Trihydrate (Standard)
    Inducer
    Docetaxel (Trihydrate) (Standard) is the analytical standard of Docetaxel (Trihydrate). This product is intended for research and analytical applications. Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule?depolymerization with an IC50 value of 0.2 μM. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of?bcl-2?and?bcl-xL?gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis.
    Docetaxel Trihydrate (Standard)
  • HY-147926
    VEGFR-2-IN-28
    Inducer
    VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC50 value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity.
    VEGFR-2-IN-28
  • HY-163679
    PROTAC ERα Degrader-9
    Inducer
    PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), MCF-7Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
    PROTAC ERα Degrader-9
  • HY-181867
    PROTAC BET Degrader-16
    Inducer
    PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia.
    PROTAC BET Degrader-16
  • HY-181011
    PROTAC Cdc25 degrader-1
    Inducer
    PROTAC Cdc25 degrader-1 (Compound D3) is an efficient Cdc25 PROTAC degrader. Its DC50 values for Cdc25A, Cdc25B, and Cdc25C are 0.97, 2.02, and 4.67 μM respectively. PROTAC Cdc25 degrader-1 induces cell cycle arrest and apoptosis in cancer cells and inhibits cell migration ability. PROTAC Cdc25 degrader-1 significantly increases the ROS level. PROTAC Cdc25 degrader-1 can be used for the study of colorectal adenocarcinoma.
    PROTAC Cdc25 degrader-1
  • HY-B0107R
    Acitretin (Standard)
    Inducer
    Acitretin (Standard) is the analytical standard of Acitretin. This product is intended for research and analytical applications. Acitretin (Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin also can be used for the research of Alzheimer’s disease.
    Acitretin (Standard)
  • HY-182760
    MN33-63
    Inducer
    MN33-63 is a Bcl-2 inhibitor, caspase-3 activator and DNA crosslinker with broad-spectrum anticancer activity. MN33-63 improves the water solubility of SN-38 (HY-13704), inhibits tumor growth and proliferation in a dose-dependent manner, and causes no obvious toxicity. MN33-63 relieves the inhibition of the mitochondrial apoptotic pathway, initiates the apoptosis program, inhibits Topo I activity, and promotes its degradation via the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-63 induces DNA crosslinking, G2/M cell cycle arrest, inhibition of cancer cell migration, and cancer cell apoptosis through the mitochondrial pathway. MN33-63 can be used in the research of colorectal cancer, cervical cancer, hepatocellular carcinoma, lung adenocarcinoma and gastric cancer.
    MN33-63
Cat. No. Product Name / Synonyms Application Reactivity