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-N3710
    Dehydrocrenatidine
    Activator 98.0%
    Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
    Dehydrocrenatidine
  • HY-W674241A
    4-Ethylphenyl sulfate sodium
    Inducer
    4-Ethylphenyl sulfate sodium is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate sodium downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate sodium induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate sodium impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate sodium alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice.
    4-Ethylphenyl sulfate sodium
  • HY-P1142
    GLP-2(rat)
    Inhibitor 99.54%
    GLP-2(rat) is an intestinal growth factor. GLP-2(rat) stimulates cell proliferation and inhibits apoptosis. GLP-2(rat) enhances mucosal mass and function in residual small intestine after massive small bowel resection (MSBR).
    GLP-2(rat)
  • HY-W747676
    Glyphosate-13C
    99.2%
    Glyphosate-13C is the 13C-labeled Glyphosate (HY-B0863). Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.
    Glyphosate-<sup>13</sup>C
  • HY-134984
    Thalidomide-NH-amido-C4-NH2
    Inducer
    Thalidomide-NH-amido-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C4-NH2
  • HY-A0077S1
    Perphenazine-d4
    98.83%
    Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
    Perphenazine-d<sub>4</sub>
  • HY-103612
    Thalidomide-O-amido-C3-COOH
    Inducer 98.43%
    Thalidomide-O-amido-C3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-amido-C3-COOH
  • HY-162863
    ERK-MYD88 interaction inhibitor 1
    Inducer 99.02%
    ERK-MYD88 interaction inhibitor 1 is an ERK-MYD88 interaction inhibitor. ERK-MYD88 interaction inhibitor 1 can induce an HRI-mediated integrated stress response (ISR), leading to cancer cell-specific immunogenic cell apoptosis (apoptosis). ERK-MYD88 interaction inhibitor 1 can induce anti-tumor T cell responses in Lewis lung cancer mice, exhibiting anti-tumor activity.
    ERK-MYD88 interaction inhibitor 1
  • HY-10255C
    Sunitinib glucuronate
    Inducer
    Sunitinib (SU 11248) glucuronate is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib glucuronate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib glucuronate
  • HY-116852S
    Thiocolchicine-d3
    Inducer 99.0%
    Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 μM) and competitively binds to tubulin with a Ki of 0.7 μM. Thiocolchicine induces cell apoptosis. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.
    Thiocolchicine-d<sub>3</sub>
  • HY-B0261S2
    Meloxicam-13C,d3
    Inducer ≥99.90%
    Meloxicam-13C,d3 is 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-<sup>13</sup>C,d<sub>3</sub>
  • HY-108695B
    (±)-Enterodiol
    Inducer
    (±)-Enterodiol is the racemate of Enterodiol (HY-108695). Enterodiol is transformed by human intestinal bacteria from lignans contained in various whole-grain cereals, nuts, legumes, flaxseed, and vegetables. Enterodiol has an apoptotic effect in colorectal cancer (CRC) cells. Enterodiol has anti-cancer activities.
    (±)-Enterodiol
  • HY-158208A
    (1S)-PMMB276
    Control
    (1S)-PMMB276 is the (1S)-enantiomer of PMMB276 (HY-158208). PMMB276 is a potent inhibitor of β-tubulin isotype III (Tubb3) polymerization and induced apoptosis.
    (1S)-PMMB276
  • HY-138846A
    Thalidomide-NH-C8-NH2 hydrochloride
    Inducer
    Thalidomide-NH-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-C8-NH2 hydrochloride
  • HY-163129
    BPU
    99.04%
    BPU arrests cell cycle progression in the sub-G1 phase. BPU is an anticancer agent through inhibiting blood vessel formation in tumor tissues.
    BPU
  • HY-156163
    Thalidomide-5-NH-PEG1-NH2 hydrochloride
    Inducer 98.90%
    Thalidomide-5-NH-PEG1-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG1-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG1-NH2 hydrochloride
  • HY-120448
    QTX125
    Activator
    QTX125 is a potent and highly selective HDAC6 inhibitor. QTX125 exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.
    QTX125
  • HY-114803
    Kokusaginine
    Inducer 98%
    Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC50 of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells.
    Kokusaginine
  • HY-120448A
    QTX125 TFA
    Inducer 99.93%
    QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.
    QTX125 TFA
  • HY-154860
    PTD10
    PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease.
    PTD10
Cat. No. Product Name / Synonyms Application Reactivity