1. Signaling Pathways
  2. Apoptosis
  3. 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.

Apoptosis Related Products (942):

Cat. No. Product Name Effect Purity
  • HY-10108
    LY294002 Activator 99.95%
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM.
  • HY-15142
    Doxorubicin hydrochloride Activator 99.47%
    Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase.
  • HY-12041
    SP600125 Activator 98.82%
    SP600125 is a cell-permeable, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively.
  • HY-10583
    Y-27632 dihydrochloride Activator 99.83%
    Y-27632 dihydrochloride is a cell-permeable, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • HY-10201
    Sorafenib Activator 99.92%
    Sorafenib (Bay 43-9006) is a potent, orally active multikinase inhibitor with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
  • HY-N6687
    Calcimycin hydrate Activator >99.0%
    Calcimycin hydrate (A23187 hydrate) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hydrate induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hydrate inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hydrate also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hydrate induces apoptosis.
  • HY-120394
    TVB-3166 Activator 99.55%
    TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth.
  • HY-130250
    SR-4835 Activator
    SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
  • HY-10999
    Trametinib Activator 99.44%
    Trametinib (GSK1120212;JTP-74057) is a potent MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM.
  • HY-10227
    Bortezomib Activator 99.97%
    Bortezomib (PS-341) is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib (PS-341) disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib (PS-341) is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans.
  • HY-16749
    Pexidartinib Activator 99.64%
    Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Anti-tumor activity.
  • HY-13757A
    Tamoxifen Activator 99.95%
    Tamoxifen (ICI 47699) is a 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.
  • HY-13453
    BAY 11-7082 Activator 99.42%
    BAY 11-7082 (BAY 11-7821) is an IKK Inhibitor. BAY 11-7082 (BAY 11-7821) decreases NF-κB by inhibiting TNF-α-induced phosphorylation of IκB-α. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50s of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-A0004
    Decitabine Activator 99.99%
    Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML). Decitabine (NSC 127716) incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme.
  • HY-B0215
    Acetylcysteine Activator >98.0%
    Acetylcysteine is a mucolytic agent which reduces the thickness of the mucus. Acetylcysteine is a ROS inhibitor.
  • HY-13966
    2-Deoxy-D-glucose Activator >99.0%
    2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.
  • HY-17364
    Temozolomide Activator 99.96%
    Temozolomide (NSC 362856; CCRG 81045) is an oral DNA alkylating agent used to treat some brain cancers.
  • HY-13027
    DAPT Activator 99.97%
    DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.
  • HY-B0011
    Docetaxel Activator 99.96%
    Docetaxel is an antineoplastic drug by inhibiting microtubule depolymerization, and attenuating of the effects of bcl-2 and bcl-xL gene expression.
  • HY-10181
    Dasatinib Activator 99.84%
    Dasatinib (BMS-354825) is a dual Bcr-Abl and Src family tyrosine kinase inhibitor with IC50s of 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit and c-KitD816V, respectively.
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