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-135317D
    Emavusertib mesylate
    Inducer
    Emavusertib mesylate (CA-4948 mesylate) is the mesylate salt form of Emavusertib (HY-135317). Emavusertib mesylate is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib mesylate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib mesylate exhibits antitumor activity in mouse model.
    Emavusertib mesylate
  • HY-10115AR
    PI-103 Hydrochloride (Standard)
    Inducer
    PI-103 (Hydrochloride) (Standard) is the analytical standard of PI-103 (Hydrochloride). This product is intended for research and analytical applications. PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
    PI-103 Hydrochloride (Standard)
  • HY-169483
    PDIC-NC
    Inducer
    PDIC-NC is a STING agonist. PDIC-NC is cytotoxic to tumor cells and induces ROS explosion, apoptosis and autophagy. PDIC-NC has lung specific distribution and can be used in the study of lung cancer.
    PDIC-NC
  • HY-P10393
    ERα17p
    Inducer
    ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models.
    ERα17p
  • HY-10325R
    CL-387785 (Standard)
    Inducer
    CL-387785 (EKI-785; WAY-EKI 785) (Standard) is the analytical standard of CL-387785 (HY-10325). This product is intended for research and analytical applications. CL-387785 is an orally active EGFR inhibitor with an IC50 of 370 pM. CL-387785 inhibits EGF-stimulated EGFR autophosphorylation with an IC50 of approximately 5 nM. CL-387,785 exerts selective inhibition on cell lines overexpressing EGFR or c-erbB-2, whereas it shows weak inhibitory effects on cell lines with low expression of these two receptors. CL-387785 effectively induces cell cycle arrest and apoptosis. CL-387785 can be used for the research of non-small cell lung cancer and autosomal recessive polycystic kidney disease.
    CL-387785 (Standard)
  • HY-18329
    TDP-665759
    Inducer
    TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models.
    TDP-665759
  • HY-14581R
    Palomid 529 (Standard)
    Inducer
    Palomid 529 (Standard) is the analytical standard of Palomid 529. This product is intended for research and analytical applications. Palomid 529 is a potent inhibitor of mTORC1 and mTORC2 complexes.
    Palomid 529 (Standard)
  • HY-B0124S2
    Zonisamide-13C6
    Inhibitor
    Zonisamide-13C6 (AD 810-13C6) is 13C labeled Zonisamide. Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy.
    Zonisamide-<sup>13</sup>C<sub>6</sub>
  • HY-N2115R
    Araloside A (Standard)
    Inducer
    Araloside A (Standard) (Chikusetsusaponin IV (Standard)), triterpenoid saponins, is an orally active component of Aralia elata. Araloside A (Standard) shows low-renin-inhibitory activity with an IC50 of 77.4 μM. Araloside A (Standard) can inhibit cell proliferation and induce apoptosis. Araloside A (Standard) suppresses inflammatory cytokines IL-1β and IL-6 production. Araloside A (Standard) can be used for the researches of cancer, inflammation and cardiovascular disease, such as renal cell carcinoma and rheumatoid arthritis.
    Araloside A (Standard)
  • HY-W042337S
    3-Methyl-4-nitrophenol-d3
    3-Methyl-4-nitrophenol-d3 is the deuterium labeled 3-Methyl-4-nitrophenol (HY-W042337). 3-Methyl-4-nitrophenol, an environmental contaminant, is a well-known constituent of diesel exhaust particles and degradation products of insecticide fenitrothion. 3-Methyl-4-nitrophenol can induce nasal epithelial cell apoptosis and increase the permeability of the nasal epithelial barrier. 3-Methyl-4-nitrophenol is also toxic to the female reproductive system.
    3-Methyl-4-nitrophenol-d<sub>3</sub>
  • HY-P0036S
    Octreotide-d8 TFA
    Octreotide-d8 (SMS 201-995-d8) TFA is the deuterium labeled Octreotide TFA. Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.
    Octreotide-d<sub>8</sub> TFA
  • HY-N10355
    27-TBDMS-4-Dehydrowithaferin A
    Activator
    27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent.
    27-TBDMS-4-Dehydrowithaferin A
  • HY-N10354
    27-Methyl withaferin A
    Inducer
    27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively.
    27-Methyl withaferin A
  • HY-N10351
    27-O-(tert-Butyldimethylsilyl)withaferin A
    Inducer
    27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells.
    27-O-(tert-Butyldimethylsilyl)withaferin A
  • HY-B0627S1
    Metformin-13C2 (hydrochloride)
    Metformin-13C2 (1,1-Dimethylbiguanide-13C2) hydrochloride is the 13C-labeled Metformin hydrochloride (HY-17471A). Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
    Metformin-<sup>13</sup>C<sub>2</sub> (hydrochloride)
  • HY-107439
    Thalidomide-O-amido-C8-NH2
    Inducer
    Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
    Thalidomide-O-amido-C8-NH2
Cat. No. Product Name / Synonyms Application Reactivity