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-111125
    AMRI-59
    		Inducer
    AMRI-59 is a potent inhibitor of PrxI used for parasitic infections. AMRI-59 can increase cellular ROS, leading to activation of signaling pathways mediated by mitochondria and apoptosis signal-regulated kinase 1, thereby leading to apoptosis in A549 human lung adenocarcinoma. AMRI-59 exhibits significant antitumor activity without apparent acute toxicity.
    AMRI-59
  • HY-145291
    CPT-Se4
    		Activator
    CPT-Se4, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT-Se4 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se4 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC50= 2.54-6.4 μM).
    CPT-Se4
  • HY-W778375
    Hesperetin triacetate
    		Inducer
    Hesperetin triacetate is an active compound with anti-inflammatory and anti-tumor activities. Hesperetin triacetate inhibits bovine serum albumin denaturation in vitro. Hesperetin triacetate inhibits carrageenan-induced paw swelling in mice in vivo. Hesperetin triacetate exhibits anti-proliferative activity against breast cancer cells. Hesperetin triacetate induces DNA degradation and apoptosis in breast cancer cells. Hesperetin triacetate can be used in studies related to breast cancer and inflammation.
    Hesperetin triacetate
  • HY-174302
    PIM-1/HDAC-IN-2
    		Inducer
    PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
    PIM-1/HDAC-IN-2
  • HY-138851
    Thalidomide-NH-amido-C5-NH2
    		Inducer
    Thalidomide-NH-amido-C5-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-C5-NH2
  • HY-P3501A
    Fexapotide TFA
    		Inducer
    Fexapotide (NX-1207) TFA induces apoptosis selectively, reducing prostate volume at a cellular level. Fexapotide can be used in lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH) research.
    Fexapotide TFA
  • HY-106015
    Tezacitabine hydrate
    		Inducer
    Tezacitabine hydrate is a cytostatic and cytotoxic antimetabolite and nucleoside analogue. Tezacitabine hydrate irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine hydrate effectively induces cells Apoptosis. Tezacitabine hydrate has the potential for leukemias and solid tumors (carcinomas) treatment.
    Tezacitabine hydrate
  • HY-168733
    LDHA-IN-9
    		Inducer
    LDHA-IN-9 (Compound 1g) is an inhibitor for LDH-A with an IC50 of 25 nM. LDHA-IN-9 inhibits the proliferation of DLD-1 cell (GI50 of 27 μM) through apoptosis induction. LDHA-IN-9 exhibits antitumor activity in mouse model without significant toxicity (25 mg/kg).
    LDHA-IN-9
  • HY-182064
    EGFR-IN-206
    		Inducer
    EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer.
    EGFR-IN-206
  • HY-172086
    TrxR-IN-7
    		Inducer
    TrxR-IN-7 is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 3.5 μM. TrxR-IN-7 induces reactive oxygen species (ROS) generation and apoptosis in tumor cells. TrxR-IN-7 can be used for the research of liver cancer and breast cancer.
    TrxR-IN-7
  • HY-176239
    PROTAC PI3Kδ degrader-1
    		Inducer
    PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model. Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
    PROTAC PI3Kδ degrader-1
  • HY-183090
    EGFR/VEGFR2-IN-13
    		Inducer
    EGFR/VEGFR2-IN-13 is a multi-target inhibitor, with an IC50 of 0.98 µM against VEGFR-2, 1.01 µM against EGFR, and 1.94 µM against topoisomerase II. EGFR/VEGFR2-IN-13 induces cell cycle arrest and apoptosis in tumor cells. As an anticancer agent, EGFR/VEGFR2-IN-13 exhibits cytotoxicity against cancer cells. EGFR/VEGFR2-IN-13 can be used in research related to breast cancer, colon cancer, and liver cancer.
    EGFR/VEGFR2-IN-13
  • HY-178939
    EGFR-IN-181
    		Inducer
    EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases.
    EGFR-IN-181
  • HY-N2132R
    Flavokawain B (Standard)
    		Inducer
    Flavokawain B (Standard) is the analytical standard of Flavokawain B. This product is intended for research and analytical applications. Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations.
    Flavokawain B (Standard)
  • HY-P10850
    PIYLGGVFQ
    		Inhibitor
    PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model.
    PIYLGGVFQ
  • HY-182002
    Apoptosis inducer 61
    		Activator
    Apoptosis inducer 61 (Compound 4E) is an Apoptosis inducer. Apoptosis inducer 61 significantly downregulates the expression of BIRC3 and activates Apoptosis. Anticancer agent 313 exhibits anticancer activity against ER+ breast cancer cells, triple-negative breast cancer cells, and gastric cancer cells.
    Apoptosis inducer 61
  • HY-13768S2
    Topotecan-d6 dihydrochloride
    		Inducer
    Topotecan-d6 dihydrochloride (SKF 104864A-d6 dihydrochloride) is the deuterium labeled Topotecan dihydrochloride. Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
    Topotecan-d<sub>6</sub> dihydrochloride
  • HY-178413S
    D-Mannitol-d4
    D-Mannitol-d4 (Mannitol-d4) is the deuterium labeled D-Mannitol (HY-N0378). D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells. D-Mannitol is commonly used to maintain osmotic pressure between the plant cytoplasm and the culture medium and protect cells when the cell wall is weakened or even removed.
    D-Mannitol-d<sub>4</sub>
  • HY-Y1362R
    Ethyl pyruvate (Standard)
    		Inducer
    Ethyl pyruvate (Standard) is the analytical standard of Ethyl pyruvate. This product is intended for research and analytical applications. Ethyl pyruvate is a simple derivative of the endogenous metabolite pyruvate. Ethyl pyruvate is an HMGB1 release inhibitor. Ethyl pyruvate can induce apoptosis by autophagy. Ethyl pyruvate has anti-inflammatory, antioxidant and anti-tumor activity. Ethyl pyruvate can be used in the study of neurodegenerative diseases such as Alzheimer's and Parkinson's disease.
    Ethyl pyruvate (Standard)
  • HY-182016
    PROTAC ATR degrader-3
    		Inducer
    PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.
    PROTAC ATR degrader-3
Cat. No. Product Name / Synonyms Application Reactivity