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-10224S1
    Panobinostat-d4 hydrochloride
    		Inducer
    Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
    Panobinostat-d<sub>4</sub> hydrochloride
  • HY-179388
    PROTAC Sirt2 Degrader-2
    		Inducer
    PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer.
    PROTAC Sirt2 Degrader-2
  • HY-144132
    αβ-Tubulin-IN-1
    		Inducer
    αβ-Tubulin-IN-1 is a potent and orally active αβ-Tubulin inhibitor. αβ-Tubulin-IN-1 induces cell cycle arrest at G2/M and efficient apoptosis. αβ-Tubulin-IN-1 inhibits tumor cell migration and Metastasis. αβ-Tubulin-IN-1 shows significant antitumor efficacy in a dose dependent manner.
    αβ-Tubulin-IN-1
  • HY-184155
    LC1343
    		Inducer
    LC1343 is a human thymidylate synthase (hTS) inhibitor with an IC50 of 7 μM. LC1343 inhibits cancer cell growth and induces apoptosis in cancer cells. LC1343 can be used for the research of ovarian cancer, colorectal cancer, and pancreatic cancer.
    LC1343
  • HY-W013032R
    Oxamic acid (Standard)
    		Inducer
    Oxamic acid (Standard) is the analytical standard of Oxamic acid. This product is intended for research and analytical applications. Oxamic acid is a lactate dehydrogenase-A (LDH-A) inhibitor. Oxamic acid shows anti-tumor activity, and anti-proliferative activity against cancer cells, and can induce apoptosis[1][2][3].
    Oxamic acid (Standard)
  • HY-147901
    KDM1/CDK1-IN-1
    		Inducer
    KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC50 values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC50 values of 16.34, 3.45 and 7.79 μM, respectively.
    KDM1/CDK1-IN-1
  • HY-P11298
    d-T101 peptide
    		Activator
    d-T101 peptide, a human hormone-peptide, is a T1/ST2 receptor ligand. d-T101 peptide binds to the T1/ST2 receptor and activates caspases 8, 9 and 3 mediated apoptosis, together with activation of JNKinase and p38 MAPKinase. d-T101 peptide also changes Golgi structural with function loss and downregulation of the endoplasmic reticulum (ER) stress repair mechanism. d-T101 peptide has immunostimulatory and anticancer activity, selectively induces apoptosis in proliferating cancer cells and increases IL-2 and IFN-γ expression as well as the recruitment of NK cells and M1 macrophages to the tumor site.
    d-T101 peptide
  • HY-W127433R
    Isostearic acid (Standard)
    		Inducer
    Isostearic acid (Standard) is the analytical standard of Isostearic acid. This product is intended for research and analytical applications. Isostearic acid is a unique fatty acid. Isostearic acid promotes IL-1 release and Apoptosis. Isostearic acid has potent inflammatory properties. Isostearic acid can be used in pharmaceutical, personal care, and cosmetic applications[1][2].
    Isostearic acid (Standard)
  • HY-12455
    Duocarmycin A
    		Inducer
    Duocarmycin A is an antitumor antibiotic and DNA alkylating agent with broad-spectrum antibacterial activity, which can serve as a payload for synthesizing antibody-drug conjugates (ADCs). Duocarmycin A selectively binds to the AT-rich minor groove of DNA, forms covalent adducts by alkylating the adenine N3 residue, thereby disrupting DNA structure and inhibiting its replication and transcription. Duocarmycin A induces apoptosis, sub-G1 phase accumulation and chromatin condensation, reduces the levels of pro-caspase-3/9, and induces p53-independent p21 expression. Duocarmycin A is widely used in the research of various malignancies, including leukemia, sarcoma, glioblastoma, as well as multiple solid tumor models such as lung cancer, breast cancer, and colorectal cancer.
    Duocarmycin A
  • HY-13007A
    PF-3758309 hydrochloride
    		Inducer
    PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
    PF-3758309 hydrochloride
  • HY-162084
    BKN-1
    		Inducer
    BKN-1 is a bifunctional ligand that can not only track the formation of mtG4s (G-quadruplexes, four-stranded DNA structures containing Hoogsteen bonds) through far-red emission, but can also induce mitochondrial dysfunction. BKN-1 has anti-tumor activity and may cause mtDNA loss, damage mitochondrial integrity, reduce ATP levels, and trigger ROS imbalance, leading to apoptosis and autophagy.
    BKN-1
  • HY-120089
    UNC1666
    		Inducer
    UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 reduces the phosphorylation levels of Mer and Flt3, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia.
    UNC1666
  • HY-N15747
    Mycoleptodiscin A
    		Inducer
    Mycoleptodiscin A ((-)-Mycoleptodiscin A) is a cytotoxic indole alkaloid found in fungus. Mycoleptodiscin A exerts cytotoxic effects by inducing apoptosis or inhibiting cell cycle progression.
    Mycoleptodiscin A
  • HY-10539
    Enzastaurin dihydrochloride
    		Inducer
    Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
    Enzastaurin dihydrochloride
  • HY-124946
    C1A
    		Inducer
    C1A is a class I/II HDACs and sirtuin inhibitor with an IC50 of 479 nM for HDAC6. C1A induces sustained acetylation of HDAC6 substrates, α-tubulin and HSP90. C1A shows srtong anticancer effcts, and induces apoptosis in cancer cells.
    C1A
  • HY-B2046S
    Simazine-d10
    		Inducer
    Simazine-d10 is the deuterium labeled Simazine (HY-B2046). Simazine is a triazine herbicide. Simazine is widely used in agriculture, potted plant and tree production. In addition, Simazine can induce the apoptosis of immune cells in the spleen of mice and inhibit the proliferation of B cells and T cells in mice.
    Simazine-d<sub>10</sub>
  • HY-182405
    GQ127
    		Inducer
    GQ127 is an orally active Gαq/11 inhibitor with an IC50 of 22.6 μM. GQ127 binds directly to Gαq/11 protein and inhibits its activity. GQ127 induces Apoptosis, suppresses viability, migration and invasion of uveal melanoma cells. GQ127 increases the phosphorylation level of YAP and decreases the phosphorylation level of ERK. GQ127 inhibits the growth of uveal melanoma xenografts in mouse models. GQ127 can be used for research related to uveal melanoma.
    GQ127
  • HY-159122
    CA IX-IN-2
    		Inducer
    CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models.
    CA IX-IN-2
  • HY-168632
    Topoisomerase I/II inhibitor 6
    		Inducer
    Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC50s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC50 values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3.
    Topoisomerase I/II inhibitor 6
  • HY-B0174AS2
    Olsalazine-d3,15N
    		Inducer
    Olsalazine-d3,15N is 15N and deuterated labeled Olsalazine (HY-B0174A). Olsalazine is an orally active prodrug of 5-ASA (HY-15027). Olsalazine can inhibit cells proliferation and induce apoptosis. Olsalazine can reduce DAI and MPO activity and inhibit inflammatory cytokines levels. Olsalazine can be used for the researches of cancer, inflammation and metabolic disease, such as colorectal cancer, inflammatory bowel disease (IBD) and hyperuricemic.
    Olsalazine-d<sub>3</sub>,<sup>15</sup>N
Cat. No. Product Name / Synonyms Application Reactivity