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-161192
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc
    		Inducer
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-O-C4H4-N(Me)-piperidine-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-O-C4H4-N(Me)-piperidine-C-boc
  • HY-136293
    Mechercharmycin A
    		Inducer
    Mechercharmycin A is a cytotoxic substance isolated from marine-derived Thermoactinomyces sp. YM3-251. Mechercharmycin A exhibits relatively strong antitumor activity.
    Mechercharmycin A
  • HY-146138
    EGFR-IN-57
    		Inducer
    EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis.
    EGFR-IN-57
  • HY-12294B
    (Rac)-PEAQX
    		Inducer
    (Rac)-PEAQX is a NMDA receptor agonist. (Rac)-PEAQX can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures .
    (Rac)-PEAQX
  • HY-115906
    K783-0308
    		Inhibitor
    K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase.
    K783-0308
  • HY-162332
    EGFR-PK/JNK-2-IN-1
    		Inducer
    EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2 with IC50s of 2.7 and 3.0 μM, respectively. EGFR-PK/JNK-2-IN-1 can induce apoptosis and induce cell cycle arrest at different cell phases. EGFR-PK/JNK-2-IN-1 can be used for the research of cancer.
    EGFR-PK/JNK-2-IN-1
  • HY-157419
    FL77-24
    		Inducer
    FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases.
    FL77-24
  • HY-177869
    CHNQD-00824
    		Inducer
    CHNQD-00824 is a Terphenyllin (HY-119821) derivative with potent anticancer effect. CHNQD-00824 inhibits the proliferation and migration of cancer cells via DNA damage. CHNQD-00824 triggers apoptosis and inhibits Doxycin Hydrochloride (DOX)-induced liver-specific enlargement in zebrafish embryos. CHNQD-00824 can be used for cancer research, such as liver and breast cancer.
    CHNQD-00824
  • HY-W016145S
    L-Glutamic acid-13C5 hydrate salt
    		Inducer
    L-Glutamic acid-13C5 hydrate salt is the 13C labeled L-Glutamic acid hydrate salt. L-Glutamic acid monosodium hydrate is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium hydrate has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium hydrate can be used in the study of neurological diseases. L-Glutamic acid monosodium hydrate acts at ionotropic and?metabotropic glutamate receptors.
    L-Glutamic acid-<sup>13</sup>C<sub>5</sub> hydrate salt
  • HY-162651
    PROTAC BRD9 Degrader-8
    		Inducer
    PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
    PROTAC BRD9 Degrader-8
  • HY-161145
    EGFR/microtubule-IN-1
    		Inducer
    EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis.
    EGFR/microtubule-IN-1
  • HY-146350
    TrxR-IN-4
    		Inducer
    TrxR-IN-4 is a thioredoxin reductase (TrxR) inhibitor with a rat IC50 of 0.37 μM. TrxR-IN-4 inhibits TrxR activity, elevates reactive oxygen species (ROS) and induces apoptosis. TrxR-IN-4 mediates endoplasmic reticulum stress and induces mitochondrial dysfunction. TrxR-IN-4 can be used for the research of hepatocellular carcinoma.
    TrxR-IN-4
  • HY-131405
    β-Eleostearic acid
    β-Eleostearic acid is an apoptosis inducer with antiproliferative properties. β-Eleostearic acid down-regulates and up-regulates the mRNA levels of Bcl-2 and Bax, respectively.
    β-Eleostearic acid
  • HY-162679
    c-Met degrader-1
    		Inducer
    c-Met degrader-1 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors.
    c-Met degrader-1
  • HY-182430
    NVP-BVB808
    		Inducer
    NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia.
    NVP-BVB808
  • HY-178441
    PKM2-IN-11
    		Inducer
    PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer.
    PKM2-IN-11
  • HY-108556
    RWJ-56110
    		Inducer
    RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
    RWJ-56110
  • HY-181982
    HJ03
    		Inducer
    HJ03 is a blood-brain barrier-permeable, orally active DNA damage and ferroptosis inducer. HJ03 triggers ferroptosis by increasing intracellular ROS, Fe2+ accumulation and lipid peroxidation. HJ03 induces DNA adducts and interstrand crosslinks, blocks DNA replication and transcription, arrests cells at the G2/M phase and induces apoptosis. HJ03 can be used in the research of glioblastoma multiforme and colorectal cancer.
    HJ03
  • HY-W744741
    Lupeol-d3
    Lupeol-d3 is the deuterium labeled Lupeol (HY-N0790). Lupeol is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor?(AR)?inhibitor and can be used for?cancer?research, especially prostate?cancer?of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
    Lupeol-d<sub>3</sub>
  • HY-115908
    ZDLD13
    		Inducer
    ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model.
    ZDLD13
Cat. No. Product Name / Synonyms Application Reactivity