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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. Nom du produit Effet Pureté Chemical Structure
  • HY-B0146R
    Verteporfin (Standard)
    Inducer
    Verteporfin (Standard) is the analytical standard of Verteporfin. This product is intended for research and analytical applications. Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
    Verteporfin (Standard)
  • HY-147905
    CDK9-IN-18
    Inducer
    CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.
    CDK9-IN-18
  • HY-153685
    NISC-6
    Inducer
    NISC-6 is a novel dual Topo-IIα/Akt inhibitor. NISC-6 has inhibitory activity against various cells, such as UACC903 (IC50 = 2.5 µM) and CHL-1 (IC50 = 0.8 µM) cells. NISC-6 dose dependently induces early and late apoptosis. NISC-6 can be used for research on melanoma.
    NISC-6
  • HY-179712
    As-CA11
    Inducer
    As-CA11 is a Thioredoxin reductase (TrxR) inhibitor with an IC50 of 18.7 nM. As-CA11 can induce cancer cells apoptosis and ROS production. As-CA11 can reduce the level of reduced Trx and increase the level of oxidized Trx. As-CA11 demonstrates anti-tumor activity in the 4T1 tumor-bearing mouse model.
    As-CA11
  • HY-178353
    EGFR/Cytokine-IN-1
    Inducer
    EGFR/Cytokine-IN-1 is an EGFR (IC50 = 0.03 μM) and Cytokine inhibitor (TNF-α, IC50 = 3.1 μM; IL-6, IC50 = 1.6 μM). EGFR/Cytokine-IN-1 shows potent anticancer activity on A549 and MCF7, respectively. EGFR/Cytokine-IN-1 significantly reduces IL-6 and TNF-α levels in A549 cells, and also shows promising ADMET profiles. EGFR/Cytokine-IN-1 can induce apoptosis in a dose-dependent manner. compound 5h can be used for the study of breast cancer and lung cancer.
    EGFR/Cytokine-IN-1
  • HY-122698
    CCI-007
    Activator 98.45%
    CCI-007 is a small molecule with cytotoxic activity against infant leukemia with MLL rearrangements, with IC50 values of 2.5-6.2 μM in sensitive cells.
    CCI-007
  • HY-N0835R
    (20S)-Protopanaxatriol (Standard)
    Inducer
    (20S)-Protopanaxatriol (Standard) is the analytical standard of (20S)-Protopanaxatriol. This product is intended for research and analytical applications. (20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
    (20S)-Protopanaxatriol (Standard)
  • HY-70006A
    Galeterone hydrochloride
    Inducer
    Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].
    Galeterone hydrochloride
  • HY-175849
    ALK degrader 1
    Activator
    ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research.
    ALK degrader 1
  • HY-10224S
    Panobinostat-d4
    Inducer
    Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
    Panobinostat-d<sub>4</sub>
  • HY-N5007
    Galgravin
    Inducer 99.21%
    Galgravin is an active compound in Nectandra megapotamica, with anti-inflammatory activity. Galgravin displays in vitro cytotoxic activity and induce apoptosis in leukemia cells.
    Galgravin
  • HY-133147
    HDAC3/6-IN-2
    Inducer
    HDAC3/6-IN-2 (compound 15) is a potent HDAC6 and HDAC3 inhibitor, with IC50 values of 0.368 and 0.635 μM, respectively. HDAC3/6-IN-2 shows antitumor activity, and induces cancer cell apoptosis. HDAC3/6-IN-2 decreases the levels of HDAC6 and HDAC3, associated with upregulation of acetylated H3 and α-tubulin.
    HDAC3/6-IN-2
  • HY-180823
    Topoisomerase II/EGFR-IN-2
    Inducer
    Topoisomerase II/EGFR-IN-2 (Compound 3) is an inhibitor of Topoisomerase IIα (IC50 = 0.122 μM) and EGFR-TKWT (IC50 = 16.8 μM). Topoisomerase II/EGFR-IN-2 inhibits the proliferation of HeLa and HepG2 cells, inducing cell cycle arrest and apoptosis. Topoisomerase II/EGFR-IN-2 upregulates caspase-3 and Bax, and downregulates Bcl-2. Topoisomerase II/EGFR-IN-2 can be used to study liver cancer and cervical cancer.
    Topoisomerase II/EGFR-IN-2
  • HY-149367
    Anticancer agent 136
    Inducer
    Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM; HY-15230), has an IC50 of 3.38 μM for HDF and a Kd of 3.86 μM for Hsp90. Anticancer agent 136 is an apoptosis-inducing agent.
    Anticancer agent 136
  • HY-161067
    EGFR-IN-96
    Inducer
    EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFRT790M.
    EGFR-IN-96
  • HY-147698
    ZLHQ-5f
    Inducer
    ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile.
    ZLHQ-5f
  • HY-181132
    dCASP1-55
    Inducer
    dCASP1-55 is a cereblon-dependent caspase-1 (CASP1) PROTAC degrader. dCASP1-55 induces excessive NF-κB activation, apoptosis, and moderate S-phase arrest in leukemic cells. dCASP1-55 suppresses colony formation of leukemic cells. dCASP1-55 can be used for the research of cancer, such as myeloid malignancies and acute myeloid leukemia.
    dCASP1-55
  • HY-181694
    SeSA-HCPT
    Inducer
    SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity.
    SeSA-HCPT
  • HY-156171
    Thalidomide-5-NH-PEG6-NH2 hydrochloride
    Inducer
    Thalidomide-5-NH-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-NH-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-NH-PEG6-NH2 hydrochloride
  • HY-175817
    PKMYT1-IN-10
    Inducer
    PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer.
    PKMYT1-IN-10
Cat. No. Nom du produit / Synonyms Application Reactivity