2. Signaling Pathways
  3. Apoptosis
  4. Apoptosis

Apoptosis

Apoptosis

Apoptosis

Related Products

PDF 16.38 MB

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-130133
    DHW-221
    		Inducer
    DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.
    DHW-221
  • HY-117652
    Lobetyol
    		Inducer
    Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Lobetyol
  • HY-N2389R
    Formosanin C (Standard)
    		Inducer
    Formosanin C (Standard) is the analytical standard of Formosanin C. This product is intended for research and analytical applications. Formosanin C is a diosgenin saponin isolated from Paris polyphylla and an immunomodulator with antitumor activity. Formosanin C induces apoptosis.
    Formosanin C (Standard)
  • HY-155748
    Antitumor agent-116
    		Inducer
    Antitumor agent-116 (compound 6C) is an anti-tumor agent with anti-proliferative activities. Antitumor agent-11 induces cell apoptosis, and shows the binding affinity against the MELK receptor.
    Antitumor agent-116
  • HY-10227G
    Bortezomib (GMP)
    		Inducer
    Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
    Bortezomib (GMP)
  • HY-149407
    Multi-kinase-IN-4
    		Activator
    Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer.
    Multi-kinase-IN-4
  • HY-12898
    (S)-FTY-720 Vinylphosphonate
    		Inhibitor
    (S)-FTY-720 Vinylphosphonate is a chiral phosphonate analogue of Fingolimod (HY-11063). (S)-FTY-720 Vinylphosphonate can activate the S1P1 receptor with an EC50 value of 75 nM. (S)-FTY-720 Vinylphosphonate can significantly inhibit Camptothecin (HY-16560)-induced apoptosis in IEC-6 cells. (S)-FTY-720 Vinylphosphonate is applicable for the research of autoimmune diseases.
    (S)-FTY-720 Vinylphosphonate
  • HY-100642S
    3-O-Methyltolcapone-d7
    		Inducer 99.0%
    3-O-Methyltolcapone-d7 (Ro 40-7591 d7) is a deuterium labeled 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC50of 773 nM. Tolcapone can inhibits α-syn and Aβ42 oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma.
    3-O-Methyltolcapone-d<sub>7</sub>
  • HY-139132
    Met-F-AEA
    		Activator
    Met-F-AEA is a metabolically stable anandamine analogue. Met-F-AEA inhibits cell growth by activating apoptosis. Met-F-AEA has antitumor activity.
    Met-F-AEA
  • HY-10181GL
    Dasatinib (GMP Like)
    		Inducer
    Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib (GMP Like)
  • HY-155390
    Caspase-3 activator 3
    		Inducer
    Caspase-3 activator 3 (compound 2h) induces apoptosis in HL-60 and K562 cells via significant caspase 3 activation. Caspase-3 activator 3 shows antileukemic acticity against HL-60 and K562 cells, with IC50 values of 42.89 and 33.61 μM, respectively.
    Caspase-3 activator 3
  • HY-179112
    PROTAC IKKβ/NR4A1 degrader-1
    		Inducer
    PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).
    PROTAC IKKβ/NR4A1 degrader-1
  • HY-P10994
    Eps8 peptide 327
    		Inducer
    Eps8 peptide 327 is an HLA-A*2402-restricted peptide antigen derived from Eps8 protein. Eps8 peptide 327 has potent antitumor activity with significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cells proliferation, induces apoptosis and disrupts EGFR signal pathway by inhibiting downstream signals (such as IL-2, TNF-α and IFN-γ) expression and the Eps8/EGFR interaction. Eps8 peptide 327 significantly inhibits tumor growth in HT-29 xenograft mcie models.
    Eps8 peptide 327
  • HY-181073
    Apoptosis/necroptosis inducer 1
    		Inducer
    Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma.
    Apoptosis/necroptosis inducer 1
  • HY-182009
    DNMT-IN-6
    		Inducer
    DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma.
    DNMT-IN-6
  • HY-183354
    HLC40
    		Inducer
    HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model.
    HLC40
  • HY-W017443S3
    L-Asparagine-15N2,d3 monohydrate
    L-Asparagine-15N2,d3 monohydrate is the deuterium and 15N-labeled L-Asparagine monohydrate (HY-W017443). L-Asparagine monohydrate is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine monohydrate can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia.
    L-Asparagine-<sup>15</sup>N<sub>2</sub>,d<sub>3</sub> monohydrate
  • HY-149053B
    (R)-OY-101
    		Inducer
    (R)-OY-101 is an orally active and specific inhibitor of P-gp. (R)-OY-101 increases tumor sensitivity to anticancer agents. (R)-OY-101 has good activity in reversing tumor resistance and promoting apoptosis and can be used in cancer related research.
    (R)-OY-101
  • HY-W014701R
    1,4-Dihydroxy-2-naphthoic acid (Standard)
    		Inducer
    1,4-Dihydroxy-2-naphthoic acid (Standard) is the analytical standard for 1,4-Dihydroxy-2-naphthoic acid (HY-W014701). 1,4-Dihydroxy-2-naphthoic acid is an orally active aryl hydrocarbon receptor (AhR) agonist and a bifidogenic growth stimulator. 1,4-Dihydroxy-2-naphthoic acid can improve the motor dysfunction in parkinson's disease (PD) model through AhR-dependent and -independent pathways. 1,4-Dihydroxy-2-naphthoic acid exerts anti-inflammatory effects by regulating the gut microbiota (such as promoting the proliferation of Bifidobacterium) and directly regulating the host immune system. 1,4-Dihydroxy-2-naphthoic acid induces apoptosis through G0/G1 cell cycle arrest in human keratinocyte to inhibit psoriasis.
    1,4-Dihydroxy-2-naphthoic acid (Standard)
  • HY-178910
    Mcl-1-IN-20
    		Inducer
    Mcl-1-IN-20 (Compound 26d) is a Mcl-1 inhibitor with Kis of 0.59, 6.6 and 3.6 μM against Mcl-1, Bcl-xL and Bcl-2. Mcl-1-IN-20 exhibits significant anti-proliferative activity against pancreatic cancer cells and can induce apoptosis in BxPC-3 cells. Mcl-1-IN-20 can be used for the study of pancreatic cancer.
    Mcl-1-IN-20
Cat. No. Product Name / Synonyms Application Reactivity