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-111753A
    WDR5-IN-4 TFA
    		Inducer 99.87%
    WDR5-IN-4 TFA (Compound C6) is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
    WDR5-IN-4 TFA
  • HY-125834
    GMB-475
    		Inducer 98.69%
    GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)).
    GMB-475
  • HY-112056
    DIM-C-pPhCO2Me
    		Activator 99.47%
    DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research.
    DIM-C-pPhCO2Me
  • HY-112698
    CA-5f
    		Inducer 99.14%
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
    CA-5f
  • HY-10987A
    ENMD-2076
    		Inducer 99.99%
    ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
    ENMD-2076
  • HY-16518
    Voreloxin Hydrochloride
    		Inducer 99.58%
    Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
    Voreloxin Hydrochloride
  • HY-110346
    AZD5582 dihydrochloride
    		Inducer 98.67%
    AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
    AZD5582 dihydrochloride
  • HY-15185B
    Nirogacestat dihydrobromide
    		Inducer 99.63%
    Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
    Nirogacestat dihydrobromide
  • HY-112299
    Zipalertinib
    		Inducer 99.81%
    Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.
    Zipalertinib
  • HY-13432
    Nanatinostat
    		Inducer 99.34%
    Nanatinostat (CHR-3996) is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat induces apoptosis in myeloma cells. Nanatinostat has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.
    Nanatinostat
  • HY-126222A
    MitoTam iodide, hydriodide
    		Activator 98.83%
    MitoTam iodide, hydriodide is a Tamoxifen derivative, an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology. MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells. MitoTam iodide, hydriodide causes apoptosis.
    MitoTam iodide, hydriodide
  • HY-B0382
    Fosinopril sodium
    		Inhibitor 99.89%
    Fosinopril Sodium is the ester prodrug of an angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension and some types of chronic heart failure.
    Fosinopril sodium
  • HY-153385
    TMX1
    		99.57%
    TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to the BRD4BD2, leading to BRD4 degradation.
    TMX1
  • HY-15222
    Menin-MLL inhibitor MI-2
    		Activator 99.81%
    Menin-MLL inhibitor MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.
    Menin-MLL inhibitor MI-2
  • HY-N0010
    Geniposidic acid
    		Inducer 99.18%
    Geniposidic acid is an effective anticancer and radioprotection agent.
    Geniposidic acid
  • HY-16397
    Phenformin
    		Inducer 99.72%
    Phenformin (1-phenethylbiguanide) is an orally active antidiabetic and anticancer agent. Phenformin has an incidence of associated lactic acidosis. Phenformin acts through acting AMPK activation and blocking mTOR pathway. Phenformin is also a substrate of P-glycoprotein (P-gp), and an OXPHOS inhibitor. Phenformin induces cancer cell apoptosis.
    Phenformin
  • HY-W042191
    Oxychlororaphine
    		Inducer 98.90%
    Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer.
    Oxychlororaphine
  • HY-B1839
    Fluazinam
    		Activator 99.36%
    Fluazinam is an orally active dinitroaniline fungicide. Fluazinam induces phosphorylation of JNK, activates p38 pathway, decreases Bcl-2, activates caspase-3, decreases complex I activity, increases Autophagy and Apoptosis. Fluazinam has strong antifungal activity against F. fujikuroi and B. maydis. Fluazinam has a negative impact on Brachydanio rerio and worker bees.
    Fluazinam
  • HY-143584
    AZ5576
    		Inducer 99.86%
    AZ5576 is a potent and highly selective CDK9 inhibitor (IC50: <5 nM). AZ5576 inhibits the phosphorylation of RNA polymerase II at Ser2, thereby inhibiting transcriptional elongation. AZ5576 can be used for hematological Malignancy research.
    AZ5576
  • HY-W014423
    L-Histidine hydrochloride hydrate
    		Inducer ≥98.0%
    L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable.
    L-Histidine hydrochloride hydrate
Cat. No. Product Name / Synonyms Application Reactivity