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-180853
    PI3K/Akt/mTOR-IN-6
    Inducer
    PI3K/Akt/mTOR-IN-6 (Compound JW4) is an orally active PI3K/Akt/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-6 induces Apoptosis in cells via the mitochondrial pathway. PI3K/Akt/mTOR-IN-6 shows potent anti-NSCLC activity.
    PI3K/Akt/mTOR-IN-6
  • HY-170912
    Topo I/II-IN-2
    Inducer
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-161045
    T-1-DOCA
    Inducer
    T-1-DOCA ia a EGFR inhibitor, with the IC50 of 56.94 and 269.01?nM for EGFRWT and EGFRT790M, respectively. T-1-DOCA can induces cell apoptosis of HCT-116 cells.
    T-1-DOCA
  • HY-10409S
    Fedratinib-d9
    Inducer
    Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
    Fedratinib-d<sub>9</sub>
  • HY-W747797
    Cinobufagine-d3
    Cinobufagine-d3 is the deuterium labeled Cinobufagin (HY-N0421). Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models.
    Cinobufagine-d<sub>3</sub>
  • HY-119767
    Jolkinolide A
    Inducer 98.0%
    Jolkinolide A is a diterpenoid, can be extracted from the roots of Euphorbia fischeriana Steud. Jolkinolide A exhibits anti-tumor activity, by affecting on angiogenesis of tumor tissues. Jolkinolide A significantly inhibits the Akt-STAT3-mTOR signaling pathway and reduces the expression of VEGF in A549 cells.
    Jolkinolide A
  • HY-169124
    Apoptosis inducer 28
    Inducer
    Apoptosis Inducer 28 (Compound X1) is an apoptosis-inducing agent with anticancer activity in vitro. Apoptosis Inducer 28 can arrest the cell cycle at the G1 phase, promote cell death, and induce apoptosis by disrupting mitochondrial membrane potential. Apoptosis inducer 28 can also decrease the production of reactive oxygen species, downregulate the gene expression of BAX, Bcl-xL, and Bcl-2, while upregulating the gene expression of PAR-4.
    Apoptosis inducer 28
  • HY-N1710
    28-Deoxonimbolide
    Inducer
    28-Deoxonimbolide is a Nimbin (HY-N3187) type limonoid, that can be isolated from Azadirachta indica seed extracts. 28-Deoxonimbolide shows anticancer activity. 28-Deoxonimbolide induces apoptotic cell death in HL60 cells via both the mitochondrial- and the death receptor-mediated pathways.
    28-Deoxonimbolide
  • HY-163090
    HR488B
    Inducer
    HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cell cycle G0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation.
    HR488B
  • HY-B1121AR
    Flunisolide hemihydrate (Standard)
    Inducer
    Flunisolide (hemihydrate) (Standard) is the analytical standard of Flunisolide (hemihydrate). This product is intended for research and analytical applications. Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.
    Flunisolide hemihydrate (Standard)
  • HY-172595
    Apoptosis inducer 48
    Inducer
    Apoptosis inducer 48 (5d) is an apoptotic agent. Apoptosis inducer 48 inhibits the growth of triple-negative breast cancer cells. Apoptosis inducer 48 attenuates proteasomal degradation via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic.
    Apoptosis inducer 48
  • HY-161187
    Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc
    Inducer
    Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc
  • HY-159518
    ROS inducer 4
    Inducer
    ROS inducer 4 (compound TE3) is a mitochondrial inhibitor. ROS inducer 4 causes a series of mitochondria-related physiological changes in tumors, such as mitochondrial fragmentation, explosive generation and accumulation of ROS, decreased mitochondrial membrane potential, decreased ATP content, and activation of ROS-mediated apoptotic signaling in mitochondria.
    ROS inducer 4
  • HY-161320
    EGFR-IN-105
    Inducer
    EGFR-IN-105 (Compound 5b) is an EGFR2 inhibitor with an IC50 value of 0.68 μM. EGFR-IN-105 exhibits anticancer activity and can induce apoptosis in cancer cells, which is used in the research of pancreatic cancer.
    EGFR-IN-105
  • HY-B0093AS
    Benazepril-d5 hydrochloride
    Inhibitor
    Benazepril-d5 hydrochloride is deuterium labeled Benazepril hydrochloride. Benazepril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor to reduce angiotensin-II production. Benazepril hydrochloride inhibits oxidative stress and inhibits apoptosis by the PI3K/Akt signaling pathway. In addition, Benazepril hydrochloride improves diabetic nephropathy and decreases proteinuria. Benazepril hydrochloride can be used in the study of hypertension, heart failure and diabetic nephropathy.
    Benazepril-d<sub>5</sub> hydrochloride
  • HY-147795
    Nampt-IN-8
    Inducer
    Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS.
    Nampt-IN-8
  • HY-N0104R
    Curcumol (Standard)
    Inducer
    Curcumol (Standard) is the analytical standard of Curcumol. This product is intended for research and analytical applications. Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.
    Curcumol (Standard)
  • HY-155965
    VEGFR/PARP-IN-1
    Inducer
    VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent.
    VEGFR/PARP-IN-1
  • HY-144069
    Pan-Trk-IN-3
    Inducer
    Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkAG595R, TrkAG667C, TrkAG667S, TrkAF589L and TrkCG623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis.
    Pan-Trk-IN-3
  • HY-136893
    SP-6-27
    Inducer
    SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer.
    SP-6-27
Cat. No. Product Name / Synonyms Application Reactivity