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-179408
    β-catenin-IN-9
    		Inducer
    β-catenin-IN-9 is a β-catenin inhibitor. β-catenin-IN-9 induces apoptosis, cell cycle arrest, and inhibits migration, invasion, and epithelial-mesenchymal transition (EMT) in colorectal cancer cells. β-catenin-IN-9 suppresses the transcription of β-catenin and vimentin, and significantly inhibits β-catenin at the protein level. β-catenin-IN-9 can be used for the research of colorectal cancer.
    β-catenin-IN-9
  • HY-163612
    XY077
    		Inducer
    XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro.
    XY077
  • HY-128366
    Waltonitone
    		Activator 99.91%
    Waltonitone is a ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill. Waltonitone significantly inhibits hepatocellular carcinoma cells growth and induces apoptosis in vitro and in vivo.
    Waltonitone
  • HY-N16929
    Gymnoside II
    		Inhibitor
    Gymnoside II is one of the main bioactive constituents isolated from Bletilla striata. Gymnoside II inhibits nano SiO2-induced A549 cell viability reduction, apoptosis, and ROS generation by activating Nrf2. Gymnoside II upregulates HO-1 and γ-GCSc, while downregulating the Bax/Bcl-2 ratio. Gymnoside II is applicable for research on nano SiO2-induced pulmonary injury.
    Gymnoside II
  • HY-175815
    Apoptosis inducer 44
    		Inducer
    Apoptosis inducer 44 is an apoptosis inducer. Apoptosis inducer 44 triggers apoptosis in MDA-MB-231 cells by increasing the levels of Bax and Cyt C, reducing Bcl-2, and initiating caspase-3 cleavage. Apoptosis inducer 44 suppresses the invasion and migration of MDA-MB-231 cells by down-regulating MMP-2 and MMP-9 expression and up-regulating E-cadherin protein levels. Apoptosis inducer 44 can be used for the study of breast cancer.
    Apoptosis inducer 44
  • HY-B0285AS
    Amiloride-15N3 hydrochloride
    Amiloride-15N3 (hydrochloride) is the 15N labeled Amiloride hydrochloride. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2;TRPP2) channel.
    Amiloride-<sup>15</sup>N<sub>3</sub> hydrochloride
  • HY-161874
    RPS6-IN-1
    		Inducer
    RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity.
    RPS6-IN-1
  • HY-W127530R
    α-Tocopherol phosphate disodium (Standard)
    		Inhibitor
    α-Tocopherol phosphate (Standard) (alpha-Tocopherol phosphate (Standard)) disodium is the analytical standard of α-Tocopherol phosphate disodium (HY-W127530). This product is intended for research and analytical applications. α-Tocopherol phosphate disodium is an antioxidant that protects against long-wave UVA1 induced cell death and scavenge UVA1 induced ROS in a skin cell model. α-Tocopherol phosphate disodium exhibits angiogenesis-promoting activity.
    α-Tocopherol phosphate disodium (Standard)
  • HY-183284
    GZD-552
    		Inducer
    GZD-552 is a potent orally active FAK inhibitor with a human FAK IC50 of 5.8 nM. GZD-552 suppresses FAK phosphorylation activation and downstream ERK signaling. GZD-552 induces apoptosis and G2/M cell cycle arrest, and exhibits antiproliferative activities in glioblastoma multiforme cells. GZD-552 exhibits antitumor efficacy in mice xenograft model. GZD-552 can be used for the research of glioblastoma multiforme.
    GZD-552
  • HY-155153
    CDK9-IN-24
    		Inducer
    CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research.
    CDK9-IN-24
  • HY-17507S1
    Pantoprazole-d3
    		Inducer
    Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
    Pantoprazole-d<sub>3</sub>
  • HY-151985
    TACC3 inhibitor 1
    		Inducer
    TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity.
    TACC3 inhibitor 1
  • HY-W720917
    Junicedric acid
    		Inhibitor
    Junicedric acid is a diterpenoid compound that can be isolated from the resin of the Araucaria araucana tree. Junicedric acid exerts neuroprotective activity by increasing intracellular calcium levels in hippocampal neurons, activating PKC and calcium/calmodulin-dependent protein kinase (CaMKII), and preventing Amyloid-β oligomer-induced synaptic protein loss, apoptosis, and long-term potentiation (LTP) inhibition. Junicedric acid can be used in the study of the pathological mechanisms of neurodegenerative diseases such as Alzheimer's disease.
    Junicedric acid
  • HY-170563
    Tubulin polymerization-IN-72
    		Inducer
    Tubulin polymerization-IN-72 (Compound 4a4) is an anticancer agent that acts as a tubulin polymerization inhibitor. It inhibits tubulin polymerization by binding to the colchicine site, leading to cancer cell arrest in the G2/M phase and inducing their apoptosis (Apoptosis). Tubulin polymerization-IN-72 has an IC50 of 0.4-2.7 nM against cancer cells.
    Tubulin polymerization-IN-72
  • HY-106364A
    Peplomycin sulfate
    		Inducer
    Peplomycin (Bleomycin PEP) sulfate is an analog of Bleomycin (HY-108345) and an antitumor antibiotic. Peplomycin sulfate exhibits potent antitumor activity and relatively low pulmonary toxicity. Peplomycin sulfate can induce various skin abnormalities and trigger apoptosis in SSCKN cells of oral squamous cell carcinoma. Peplomycin sulfate can also induce pulmonary fibrosis. Peplomycin sulfate is applicable for the research of tumors, pulmonary fibrosis and other related diseases.
    Peplomycin sulfate
  • HY-10201S4
    Sorafenib-d3 tosylate
    Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-d<sub>3</sub> tosylate
  • HY-147854
    B-Raf IN 9
    		Inducer
    B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM.
    B-Raf IN 9
  • HY-168954
    CSF1R-IN-26
    		Inducer
    CSF1R-IN-26 (Compound III-1) is the inhibitor for CSF-1R with an IC50 of 20.07 nM. CSF1R-IN-26 promotes the polarization of M2 macrophages to M1 macrophages, thereby inducing apoptosis in MC-38 cancer cell. CSF1R-IN-26 inhibits the activation of AKT/ERK/STAT3 signaling pathway. CSF1R-IN-26 reconstructs the tumor immune microenvironment and exhibits antitumor activity in mouse models. CSF1R-IN-26 exhibits pharmacokinetics characteristics in SD rats with a half-life 1.86 hours, and an oral bioavailability of 79.22%.
    CSF1R-IN-26
  • HY-113952R
    Actinonin (Standard)
    		Inducer
    Actinonin (Standard) is the analytical standard of Actinonin. This product is intended for research and analytical applications. Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
    Actinonin (Standard)
  • HY-180523
    PKM2-IN-13
    		Inducer
    PKM2-IN-13 is a selective PKM2 inhibitor inhibiting PKM2 with an IC50 value of 55.13 μM. PKM2-IN-13 exhibits broad-spectrum anticancer activity with low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevated ROS levels and activation of caspases 3/7, and interacts with and inhibits the glycolytic activity of Pyruvate Kinase M2 in virto. PKM2-IN-13 demonstrates a favorable safety profile with no significant adverse effects in vivo. PKM2-IN-13 can be used for oral squamous cell carcinoma (OSCC), colon carcinoma, breast cancer and melanoma research.
    PKM2-IN-13
Cat. No. Product Name / Synonyms Application Reactivity