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-14942A
    Berubicin hydrochloride
    Inducer
    Berubicin (RTA 744) hydrochloride is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin hydrochloride inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin hydrochloride exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin hydrochloride can be used in the study of tumors related to the nervous system.
    Berubicin hydrochloride
  • HY-113225S4
    Guanosine triphosphate-15N5,d14 (dilithium)
    Inducer 98.4%
    Guanosine triphosphate-15N5,d14 (GTP-15N5,d14) dilithium is deuterium and 15N labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate dilithium (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate dilithium promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate dilithium links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate dilithium accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate dilithium is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism.
    Guanosine triphosphate-<sup>15</sup>N<sub>5</sub>,d<sub>14</sub> (dilithium)
  • HY-120960
    N-Arachidonoyl-L-serine
    Inhibitor 98%
    N-Arachidonoyl-L-serine (ARA-S) is an endocannabinoid. N-Arachidonoyl-L-serine induces phosphorylation of Akt and MAPK in endothelial cells. N-Arachidonoyl-L-serine also induces endothelium-dependent vasodilation in isolated rat mesenteric and abdominal aortas. N-Arachidonoyl-L-serine exhibits neuroprotective effects after traumatic brain injury by reducing apoptosis. N-Arachidonoyl-L-serine promotes the opening of KV7.1/KCNE1 channels in mammalian cells and shortens the action potential duration in cardiomyocytes. N-Arachidonoyl-L-serine may be used in research on cardiovascular and cerebrovascular diseases and neurological disorders.
    N-Arachidonoyl-L-serine
  • HY-145944
    ASR-488
    Inducer 99.73%
    ASR-488 activates the mRNA-binding protein CPEB1, induces apoptosis and inhibits bladder cancer growth.
    ASR-488
  • HY-N9802
    n-Butyl-β-D-fructofuranoside
    Inducer
    n-Butyl-β-D-fructofuranoside could be isolated from kangaisan. n-Butyl-β-D-fructofuranoside induces apoptosis through the mitochondrial pathway. n-Butyl-β-D-fructofuranoside can be used for cancer research.
    n-Butyl-β-D-fructofuranoside
  • HY-155050
    PRMT5-IN-31
    Inducer 99.25%
    PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min).
    PRMT5-IN-31
  • HY-13864
    PF-4989216
    Activator 99.38%
    PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
    PF-4989216
  • HY-161470
    WS-384
    Inducer 98.23%
    WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC).
    WS-384
  • HY-N3096
    Penduletin
    Inducer 99.59%
    Penduletin is a flavone, that can be isolated from Brickelia pendula and Vitex negundo. Penduletin shows anticancer activity. Penduletin induces apoptosis in the cancer cells through ROS generation.
    Penduletin
  • HY-10181G
    Dasatinib (GMP)
    Inducer
    Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values ​​for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50 values ​​of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib (GMP)
  • HY-N8306
    Isojacareubin
    Inducer 98.0%
    Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis.
    Isojacareubin
  • HY-126423
    Isorhamnetin 3-glucuronide
    Inducer
    Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase.
    Isorhamnetin 3-glucuronide
  • HY-P11115A
    CIGB-552 TFA
    Inhibitor
    CIGB-552 TFA is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 TFA can increase the level of protein COMMD1. CIGB-552 TFA significantly inhibits the NF-κB signaling pathway. CIGB-552 TFA can promote apoptosis of the tumor cells. CIGB-552 TFA can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 TFA has anti-inflammatory and anti-angiogenic effects. CIGB-552 TFA can be used for the research of the lung cancer and colon cancer.
    CIGB-552 TFA
  • HY-13757AS1
    Tamoxifen-d3
    Tamoxifen-d3 is the deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen-d<sub>3</sub>
  • HY-180277
    PROTAC CDK6 Degrader 1
    Inducer
    PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC50 of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC50 > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML).
    PROTAC CDK6 Degrader 1
  • HY-13272S2
    Dacomitinib-d10 dihydrochloride
    Inducer
    Dacomitinib-d10 dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
    Dacomitinib-d<sub>10</sub> dihydrochloride
  • HY-N10149
    Nauclefine
    Inducer 99.65%
    Nauclefine is an indole alkaloid isolated from Nauclea officinalis. Nauclefine acts as a PDE3A modulator to induce cancer cell apoptosis through a PDE3A-SLFN12-dependent death pathway.
    Nauclefine
  • HY-N2490
    Dehydrotrametenolic acid
    Inducer 99.95%
    Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects.
    Dehydrotrametenolic acid
  • HY-141010
    Thalidomide-O-PEG4-amine
    Inducer
    Thalidomide-O-PEG4-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-PEG4-amine
  • HY-162477
    TS-24
    Inducer 98.96%
    TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis.
    TS-24
Cat. No. Product Name / Synonyms Application Reactivity