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-W042191R
    Oxychlororaphine (Standard)
    		Inducer
    Oxychlororaphine (Standard) is the analytical standard of Oxychlororaphine. This product is intended for research and analytical applications. 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[1][2].
    Oxychlororaphine (Standard)
  • HY-163661
    p53-MDM2-IN-5
    		Inducer
    p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity.
    p53-MDM2-IN-5
  • HY-180537
    Apoptosis inducer 57
    		Inducer
    Apoptosis inducer 57 is a apoptosis inducer and Thymidylate Synthase (TS) inhibitor. Apoptosis inducer 57 exhibits cytotoxic activity against SW480 and MCF-7 cancer cells with IC50 values of 15.7 and 16.5 µM, and induces dose-dependent apoptosis and S-phase cell cycle arrest. Apoptosis inducer 57 stalely binds the TS active site via interactions with Asp218 and Met311. TS-IN-9 can be used for breast cancer and colorectal cancer research.
    Apoptosis inducer 57
  • HY-158969
    EGFR-IN-113
    		Inducer
    EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC50 of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer.
    EGFR-IN-113
  • HY-14930S
    Mirodenafil-d7
    		Inhibitor
    Mirodenafil-d7 (SK3530-d7) is the deuterium labeled Mirodenafil (HY-14930). Mirodenafil (SK3530) is an orally active, potent, reversible, and selective?phosphodiesterase?5 (PDE5)?inhibitor. Mirodenafil is a?glucocorticoid receptor?(GR)?modulator Mirodenafil activates the?Wnt/β-catenin?signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil-d<sub>7</sub>
  • HY-N0054S
    Osthole-d3
    		Inducer
    Osthole-d3 (Osthol-d3) is the deuterium-labeled Osthole (HY-N0054).
    Osthole-d<sub>3</sub>
  • HY-147826
    EGFR-IN-60
    		Activator
    EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.
    EGFR-IN-60
  • HY-172092
    BG11
    		Inducer
    BG11 induces the accumulation of Fe2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models.
    BG11
  • HY-N0595R
    Genistin (Standard)
    		Inducer
    Genistin (Standard) is the analytical standard of Genistin. This product is intended for research and analytical applications. Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.
    Genistin (Standard)
  • HY-18343
    CP-31398
    CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth.
    CP-31398
  • HY-147864
    c-Fms-IN-12
    		Inducer
    c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis.
    c-Fms-IN-12
  • HY-17371S
    Oxaliplatin-d10
    		Inducer
    Oxaliplatin-d10 is a deuterium labeled Oxaliplatin (HY-17371). Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. Oxaliplatin can be used for cancer research.
    Oxaliplatin-d<sub>10</sub>
  • HY-168718
    FAK-IN-22
    		Inducer
    FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway.
    FAK-IN-22
  • HY-138853
    Thalidomide-NH-amido-C8-NH2
    		Inducer
    Thalidomide-NH-amido-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C8-NH2
  • HY-177501
    Otviciclib
    		Inducer
    Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer.
    Otviciclib
  • HY-170576
    FLT3-IN-28
    		Inducer
    FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD.
    FLT3-IN-28
  • HY-110067
    VO-OHPic
    		Inhibitor
    VO-OHPic is a reversible, noncompetitive PTEN inhibitor with an human IC50 value of 46 nM. VO-OHPic inhibits PTEN signaling, activates Akt-GSK3β and Nrf-2/HO-1 pathways, induces apoptosis resistance and elevates IL-10 levels. VO-OHPic inhibits autophagy, ferroptosis and oxidative stress. VO-OHPic can be used for the research of acute myocardial infarction, intervertebral disc degeneration, cardiomyopathy and cancer.
    VO-OHPic
  • HY-W724397
    3-Phenoxybenzoic acid-d9
    3-Phenoxybenzoic acid-d9 (3-PBA-d9) is the deuterium labeled 3-Phenoxybenzoic acid (HY-W014225). 3-Phenoxybenzoic acid is the metabolite of pyrethroid insecticides. 3-Phenoxybenzoic acid induces immunotoxicity and oxidative stress, and inhibits the phagocytic ability of macrophages.
    3-Phenoxybenzoic acid-d<sub>9</sub>
  • HY-P10793
    Cyclic(YCDGFYACYMDV)
    Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model.
    Cyclic(YCDGFYACYMDV)
  • HY-170927
    JAK-IN-40
    		Inducer
    JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC50s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI50 of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772).
    JAK-IN-40
Cat. No. Product Name / Synonyms Application Reactivity