2. Signaling Pathways
  3. Apoptosis
  4. Apoptosis

Apoptosis

Apoptosis

Apoptosis

Related Products

PDF 16.38 MB

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-162755
    SHP2-IN-30
    		Inducer
    SHP2-IN-30 (compound 14i) is an allosteric SHP2 inhibitor with an IC50 of 104 nM. SHP2-IN-30 shows low inhibitory effect on SHP2-PTP. SHP2-IN-30 induces cell apoptosis and arrests the cell cycle at the G0/G1 phase.
    SHP2-IN-30
  • HY-167911
    Cidofovir sodium
    		Inducer
    Cidofovir sodium is an acyclic monophosphate nucleotide analogue and CMV inhibitor with antiviral activity. Cidofovir sodium inhibits cytomegalovirus (CMV) replication by selectively inhibiting viral DNA polymerase. Cidofovir sodium induces apoptosis and can be used in studies of AIDS cytomegalovirus retinitis, herpes, and cancer. Cidofovir sodium also has anti-orthopoxvirus and anti-variola activities.
    Cidofovir sodium
  • HY-180912
    HS-36
    		Inducer
    HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC50 values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia.
    HS-36
  • HY-173309
    P53/TLR2 modulator-1
    		Inhibitor
    P53/TLR2 modulator-1 (Compound Z9) is a modulator that targets both the P53 pathway and TLR2 simultaneously, exhibiting anti-radiation activity. P53/TLR2 modulator-1 reduces apoptosis by inhibiting the radiation-induced expression of P53 and Bax. At the same time, it activates the TLR2 pathway, upregulates the expression of downstream proteins MyD88 and P65, and promotes the secretion of cytokines such as IL-6, thus exerting an anti-radiation effect. P53/TLR2 modulator-1 shows significant anti-radiation activity against both AHH-1 cells and HUVECs. It can also increase the survival rate of C57BL/6J mice irradiated with a lethal dose of radiation and reduce the damage to their hematopoietic system, the villous structure of the small intestine, and the spleen caused by radiation. P53/TLR2 modulator-1 can be used in the research of radiation injury-related diseases.
    P53/TLR2 modulator-1
  • HY-168559
    EGFR-IN-131
    		Inducer
    EGFR-IN-131 (compound 3a) is a potent and cross the blood-brain barrier EGFR inhibitor with an IC50 value of 272.9 nM. EGFR-IN-131 shows antiproliferative activity. EGFR-IN-131 induces apoptosis and cell cycle arrest at G0/G1 phase. EGFR-IN-131 decreases the protein expression of p-EGFR.
    EGFR-IN-131
  • HY-B1218S
    Sulfaphenazole-d4
    		99.66%
    Sulfaphenazole-d4 is the deuterium labeled Sulfaphenazole (HY-B1218). Sulfaphenazole is a selective inhibitor of human cytochrome P450 (CYP) 2C9 enzyme. Sulfaphenazole is a cytoprotective agent against light-induced death of photoreceptors. Sulfaphenazole inhibits light-induced necrosis and mitochondrial stress-initiated apoptosis. Sulfaphenazole is an off patent sulfonamide antibiotic and demonstrates bactericidal activity through enhanced M1 macrophage activity. Sulfaphenazole can significantly reduce infarct size and restore post-ischemic coronary flow following ischemia and reperfusion.
    Sulfaphenazole-d<sub>4</sub>
  • HY-155227S
    ALK/EGFR-IN-1-d5
    		Inducer
    ALK/EGFR-IN-1-d5 (Compound (-)-9a) is a deuterated dual-target inhibitor of EGFR and ALK, with an IC50 of 1.08 nM for EGFR and an IC50 of 2.395 nM for ALK. ALK/EGFR-IN-1-d5 inhibits the phosphorylated proteins in the EGFR, ALK, and BRK signaling pathways, blocking the cell cycle, leading to a reduction in mitochondrial membrane potential and cell apoptosis (Apoptosis). ALK/EGFR-IN-1-d5 also significantly inhibits tumor growth in animal models and demonstrates good safety. ALK/EGFR-IN-1-d5 holds promise for research in the field of cancer treatment
    ALK/EGFR-IN-1-d<sub>5</sub>
  • HY-N9778
    Phoyunbene B
    		Inducer
    Phoyunbene B is a similar substance to Resveratrol (HY-16561). Phoyunbene B exhibits stronger growth inhibitory activity against human liver cancer cells HepG2 compared to Resveratrol. Phoyunbene B induces G2/M phase cell cycle arrest and apoptosis. Phoyunbene B increases Bax/Bcl-2 and activates Caspase-3. Phoyunbene B inhibits the invasion and migration of cancer cells. Phoyunbene B can be used for research on liver cancer.
    Phoyunbene B
  • HY-B1204S4
    Histamine-15N3
    		Inducer
    Histamine-15N3 is the 15N3-labeled Histamine (HY-B1204). Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
    Histamine-<sup>15</sup>N<sub>3</sub>
  • HY-B1315S1
    Carbaryl-d7
    		Inducer 99%
    Carbaryl-d7 is the deuterium labeled Carbaryl (HY-B1315). Carbaryl is the inhibitor for acetylcholinesterase that inhibits the degradation of acetylcholine in the synaptic cleft, leads to the accumulation of acetylcholine and causes neurotoxicity. Carbaryl can be used as an insecticide.
    Carbaryl-d<sub>7</sub>
  • HY-178899
    C14-Tri-LAN-Gly
    		Inhibitor
    C14-Tri-LAN-Gly is a highly selective and potent NOD1 agonist. C14-Tri-LAN-Gly activates NOD1. C14-Tri-LAN-Gly inhibits the expression of cleaved-caspase3. C14-Tri-LAN-Gly upregulates A20 expression. C14-Tri-LAN-Gly protects mice from lethal hepatitis by inhibiting hepatocyte Apoptosis. C14-Tri-LAN-Gly inhibits osteoblastogenesis and promots osteoclastogenesis.
    C14-Tri-LAN-Gly
  • HY-161705
    Anti-apoptotic agent 1
    		Inhibitor
    Anti-apoptotic agent 1 (Compound B4) exhibits neuroprotective activity and good pharmacokinetic properties. Anti-apoptotic agent 1 inhibits apoptosis, prevents stroke recurrence in photothrombotic rat model.
    Anti-apoptotic agent 1
  • HY-163160
    BET-IN-23
    		Inducer
    Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro.
    BET-IN-23
  • HY-146209
    Tubulin polymerization-IN-13
    		Inducer
    Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity.
    Tubulin polymerization-IN-13
  • HY-182763
    EGFR/BRAFV600E-IN-7
    		Inducer
    EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAFV600E kinase inhibitor with human IC50 values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAFV600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAFV600E, including hydrogen bonding with EGFR Met769 and BRAFV600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer.
    EGFR/BRAFV600E-IN-7
  • HY-16457
    Simotaxel
    		Inducer
    Simotaxel (MST 997) is an orally active derivative of the taxane class. Simotaxel binds to β-tubulin and promotes tubulin polymerization (EC₅₀ = 0.9 μM), inhibits tubulin depolymerization, and causes cell cycle arrest at the G₂-M phase. Simotaxel disrupts the formation of the mitotic spindle and triggers the caspase-dependent apoptotic pathway (apoptosis). Simotaxel has inhibitory effects on Paclitaxel (HY-B0015) sensitive cell lines and overcomes drug resistance. Simotaxel can be used to study Paclitaxel / Docetaxel (HY-B0011) resistant solid tumors.
    Simotaxel
  • HY-145542S
    Isovalerylcarnitine-d9 chloride
    		Inducer
    Isovalerylcarnitine-d9 chloride is the deuterium labeled Isovalerylcarnitine chloride (HY-145542). Isovalerylcarnitine chloride is a metabolite of leucine. Isovalerylcarnitine chloride can specifically activate calpain in human neutrophils. Isovalerylcarnitine chloride inhibits tumor cell proliferation and induces apoptosis. Elevated circulating levels of Isovalerylcarnitine chloride are negatively correlated with reduced lung cancer risk.
    Isovalerylcarnitine-d<sub>9</sub> chloride
  • HY-146354
    Antiproliferative agent-4
    		Inducer
    Antiproliferative agent-4 (compound 2y) has excellent anti-proliferative activity against certain cancer cell lines. Antiproliferative agent-4 reduces the mitochondrial membrane potential, and increases the apoptosis rate and the level of ROS on EC109. Antiproliferative agent-4 inhibits tumour growth in nude mice, with low toxicity.
    Antiproliferative agent-4
  • HY-175009
    MRC-G-001
    		Inducer
    MRC-G-001 is a Genipin (HY-17389) derivative with an IC50 of 117 μM against A549 cancer cells. MRC-G-001 inhibits the phosphorylation of EGFR, JAK1, and STAT3, and modulates epithelial-mesenchymal transition (EMT)-related protein expression, thereby attenuating cell migration and invasion. MRC-G-001 induces cell cycle arrest and cell apoptosis. MRC-G-001 can be used for the study of cancers such as non-small-cell lung cancer.
    MRC-G-001
  • HY-170436
    NFh-NMe-2
    		Inducer
    NFh-NMe-2 is a photosensitizer, that interacts with nitroreductase, generates singlet oxygen in tumor cells, exhibits cytotoxicity in cancer cells, and induces apoptosis. NFh-NMe-2 exhibits antitumor efficacy in mouse models.
    NFh-NMe-2
Cat. No. Product Name / Synonyms Application Reactivity