2. Signaling Pathways
  3. Apoptosis
  4. Apoptosis

Apoptosis

Apoptosis

Apoptosis

Related Products

PDF 16.38 MB

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-179387
    CXCR2-IN-3
    		Inducer
    CXCR2-IN-3 is a CXCR2 inhibitor with an IC50 of 11.37 μM. CXCR2-IN-3 mediates CXCR2-Ca2+ signalling inhibition halted autophagic flux, subsequently facilitating ROS-mediated apoptotic cell death. CXCR2-IN-3 suppresses the CXCR2-NLRP3 canonical pathway, suppressing pre-tumorigenic markers. CXCR2-IN-3 causes autophagy-dependent cell death in polyploid giant cancer cells (PGCCs). CXCR2-IN-3 can be used for the research of oral squamous cell carcinoma (OSCC).
    CXCR2-IN-3
  • HY-W777154
    Zoledronic acid-15N2,13C2
    Zoledronic acid-15N2,13C2 (CGP 42446-15N2,13C2) is the 13C- and 15N-labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
    Zoledronic acid-<sup>15</sup>N<sub>2</sub>,<sup>13</sup>C<sub>2</sub>
  • HY-N9534
    Xylopine
    		Inducer 98.0%
    Xylopine is an aporphine alkaloid with cytotoxic activity on cancer cells. Xylopine induces oxidative stress, causes G2/M cell cycle arrest and apoptosis in cancer cells.
    Xylopine
  • HY-149998
    Antimycobacterial agent-5
    		Inducer
    Antimycobacterial agent-5 (compound 27) is an imidazopyridine amide targeting mycobacterial electron transport chain (ETC) airway CIII2CIV2 supercomplexes. The IC50 value of Antimycobacterial agent-5 against Mycobacterium smegmatisCIII2CIV2 is 441 nM.
    Antimycobacterial agent-5
  • HY-179374
    Aurora kinase/HDAC-IN-1
    		Inducer
    Aurora kinase/HDAC-IN-1 is an orally active dual Aurora kinase and HDAC inhibitor that inhibits Aurora A (IC50 = 116 nM), Aurora B (IC50 = 225 nM), HDAC1 (IC50 = 164 nM), and HDAC2 (IC50 = 346 nM).Aurora kinase/HDAC-IN-1 promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis via G2/M cell-cycle arrest. Aurora kinase/HDAC-IN-1 exhibits potent antiproliferative activity in colorectal cancer cells, with an IC50 value of 30.2 nM in HCT-116 cells.Aurora kinase/HDAC-IN-1 significantly suppresses tumor growth in an HCT-116 colorectal cancer xenograft mouse model.
    Aurora kinase/HDAC-IN-1
  • HY-161210
    Thalidomide-azetidine-C-PIP-C-boc
    		Inducer
    Thalidomide-azetidine-C-PIP-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-C-PIP-C-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-azetidine-C-PIP-C-boc
  • HY-169037
    Δ8-Tetrahydrocannabinoquinone
    		Inducer
    Δ8-Tetrahydrocannabinoquinone (HU-336) is a potent antiangiogenic agent. Δ8-Tetrahydrocannabinoquinone inhibits angiogenesis by directly inducing apoptosis of vascular endothelial cells without changing the expression of pro- and antiangiogenic cytokines and receptors. Δ8-Tetrahydrocannabinoquinone is highly effective against tumor xenografts in nude mice.
    Δ8-Tetrahydrocannabinoquinone
  • HY-170925
    AChE-IN-81
    		Inhibitor
    AChE-IN-81 (compound 22) is a potent, irreversible and selective AChE inhibitor. AChE-IN-81 inhibits activity on AChE with inhibitory rates of 80.0%, with an IC50 of 3.7 μM. AChE-IN-81 binds to AChE with a binding affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces in zebrafish brain cells. AChE-IN-81 exhibits potential neuroprotective activities on H2O2-induced SH-SY5Y cell injury model.
    AChE-IN-81
  • HY-150540
    Bcl-2-IN-10
    		Inducer
    Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research.
    Bcl-2-IN-10
  • HY-155227
    ALK/EGFR-IN-1
    		Inducer
    ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research.
    ALK/EGFR-IN-1
  • HY-144676
    pan-HER-IN-1
    		Inducer
    pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities.
    pan-HER-IN-1
  • HY-109061A
    Lazertinib mesylate hydrate
    		Inducer
    Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.
    Lazertinib mesylate hydrate
  • HY-N0492AR
    α-Lipoic Acid sodium (Standard)
    		Inducer
    α-Lipoic Acid (sodium) (Standard) is the analytical standard of α-Lipoic Acid (sodium). This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
    α-Lipoic Acid sodium (Standard)
  • HY-B0261S1
    Meloxicam-d3-1
    		Inducer 98.0%
    Meloxicam-d3-1 is the deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively.
    Meloxicam-d<sub>3</sub>-1
  • HY-13062AS
    Daunorubicin-13C,d3 TFA
    		Inducer
    Daunorubicin-13C,d3 TFA (Daunomycin-13C,d3 TFA) is the deuterium and 13C-labeled Daunorubicin TFA. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin-<sup>13</sup>C,d<sub>3</sub> TFA
  • HY-179023
    CDK9-IN-45
    		Inducer
    CDK9-IN-45 (Compound B11) is a highly selective CDK9 inhibitor with IC50 values for CDK9 and CDK1 of 7.13 and 489.5 nM respectively. CDK9-IN-45 exhibits a potent inhibitory effect on colorectal cancer cells. CDK9-IN-45 induces cell apoptosis and leads to significant accumulation of ROS. CDK9-IN-45 activates Caspase-3, downregulates Mcl-1, XIAP, and c-Myc. CDK9-IN-45 can be used for research on colorectal cancer.
    CDK9-IN-45
  • HY-167825
    Barakol
    		Inducer
    Barakol is a major compound found in Cassia siamea. Barakol inhibits MMP-3 activity. Barakol potentiates the anti-metastatic effect of Doxorubicin (HY-15142). Barakol induces apoptosis, with ROS generation, increase in expression ratio of Bax/Bcl-2, and caspase-9 activation. Barakol has laxative, anxiolytic, CNS depressant, and antioxidant, anticancer effects.
    Barakol
  • HY-17355AR
    Dexpramipexole dihydrochloride (Standard)
    		Inhibitor
    Dexpramipexole ((R)-Pramipexole) dihydrochloride (Standard) is the analytical standard of Dexpramipexole (dihydrochloride). This product is intended for research and analytical applications. Dexpramipexole dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
    Dexpramipexole dihydrochloride (Standard)
  • HY-120337B
    cis-V-11-0711
    		Inducer
    cis-V-11-0711 is the cis form of V-11-0711 (HY-120337). V-11-0711 is a potent and selective Chk-α (IC50 = 20 nM) inhibitor. V-11-0711 can significantly reduce PCho levels. V-11-0711 causes a reversible growth arrest. V-11-0711 induces apoptosis at high concentrations. V-11-0711 can be used for the study of cervical cancer and triple-negative breast cancer.
    cis-V-11-0711
  • HY-155474
    Me4Phen
    		Inducer
    Me4Phen (compound 3) is an oxygen rhenium (V) complex that depletes mitochondrial membrane potential and upregulates intracellular reactive oxygen species (ROS), leading to endoplasmic reticulum stress-mediated necrosis of cancer cells. Me4Phen is highly lipophilic and effectively overcomes Cisplatin (HY-17394) resistance in a variety of cancer cells.
    Me4Phen
Cat. No. Product Name / Synonyms Application Reactivity