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-181074
    Tubulin polymerization-IN-88
    		Inducer
    Tubulin polymerization-IN-88 is a tubulin inhibitor that blocks tubulin polymerization, leading to microtubule destabilization and disruption of the mitotic spindle. Tubulin polymerization-IN-88 induces G2/M phase arrest and apoptosis in cancer cells, and inhibits cancer cell migration and self-renewal of cancer stem cells. It exhibits in vitro anti-proliferative activity against cancer cells with selectivity over normal cells. Tubulin polymerization-IN-88 also demonstrates in vivo anti-cancer activity without significant toxicity. Tubulin polymerization-IN-88 is applicable for research on glioblastoma, lung cancer, endometrial cancer, ovarian cancer, and leukemia.
    Tubulin polymerization-IN-88
  • HY-D3153
    PbQ
    		Inducer
    PbQ is a tubulin inhibitor (with an IC50 of 5 μM against goat tubulin) and a fluorescent probe for cuprous ions Cu (I). PbQ can penetrate the membrane of peripheral blood mononuclear cells, form a stable 1:1 complex with Cu+ ions, and exhibits low toxicity and good biocompatibility toward macrophage cell lines. In addition, PbQ promotes tubulin degradation and disrupts the microtubule network in lung epithelial cells without affecting actin. PbQ also possesses genotoxicity by forming DNA base adducts, and it can activate caspase-3 and apoptosis-related genes, induce loss of mitochondrial membrane potential, and trigger cell apoptosis. PbQ can be used in studies related to chronic obstructive pulmonary disease.
    PbQ
  • HY-179439
    Multi-kinase-IN-8
    		Inducer
    Multi-kinase-IN-8 is a muti-kinase inhibitor. Multi-kinase-IN-8 inhibits COX-1 (IC50 of 12.6 μM), COX-2 (IC50 of 0.05 μM) and VEGFR-2 (IC50 of 0.12 nM). Multi-kinase-IN-8 inhibits tumor-associated carbonic anhydrases (CA IX and CA XII with Ki of 31.5 nM and 386.9 nM, respectively). Multi-kinase-IN-8 triggers cell cycle arrest and apoptosis through upregulation of Caspase 9 and Bax along with downregulation of Bcl 2. Multi-kinase-IN-8 suppresses PGE2, p-VEGFR-2, MMP-9 and HIF-1α and exhibits growth-inhibitory activity against breast cancer, lung cancer, and colorectal adenocarcinoma.
    Multi-kinase-IN-8
  • HY-146105
    Anticancer agent 65
    		Inducer
    Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells.
    Anticancer agent 65
  • HY-N12603
    Typhatifolin B
    		Inducer
    Typhatifolin B (Compd 2), an anti-cancer agent, could remarkably induce cell apoptosis and G0/G1 cycle arrest, as well as block cell migration and invasion.
    Typhatifolin B
  • HY-13287A
    SGI-1776
    		Inducer
    SGI-1776 is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, Pim-2 and Pim-3, respectively.
    SGI-1776
  • HY-170402
    SIRT6-IN-4
    		Inducer
    SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models.
    SIRT6-IN-4
  • HY-P3707
    Tumor targeted pro-apoptotic peptide
    		Inducer
    Tumor targeted pro-apoptotic peptide (CNGRC-GG-D(KLAKLAK)2) is an anti-tumor peptide. Tumor targeted pro-apoptotic peptide disrupts mitochondrial membranes and promotes apoptosis, showing anticancer activity in mice.
    Tumor targeted pro-apoptotic peptide
  • HY-118084
    LS-104
    		Inducer
    LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies.
    LS-104
  • HY-120561
    PC-046
    		Inducer
    PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC50 of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC50 of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice.
    PC-046
  • HY-175874
    Tubulin-IN-55
    		Inducer
    Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer.
    Tubulin-IN-55
  • HY-138851A
    Thalidomide-NH-amido-C5-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-amido-C5-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-amido-C5-NH2 hydrochloride
  • HY-147682
    NF-κB-IN-5
    		Inducer
    NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase.
    NF-κB-IN-5
  • HY-159175
    XM-U-14
    		Inducer
    XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)).
    XM-U-14
  • HY-147513
    AKT-IN-12
    		Inducer
    AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia.
    AKT-IN-12
  • HY-172789
    mTOR inhibitor-27
    		Inducer
    mTOR inhibitor-27 (Compound 7e) is a mammalian target of rapamycin (mTOR) inhibitor with an IC50 value of 5.47 μM. mTOR inhibitor-27 can induce tumor cell apoptosis and arrest the cell cycle in the S-phase, thereby inhibiting cancer cell growth. mTOR inhibitor-27 is promising for research of cancers, such as skin cancer.
    mTOR inhibitor-27
  • HY-168300
    Antiangiogenic agent 7
    		Inducer
    Antiangiogenic agent 7 (Compound 1) can induce cell apoptosis, increase Reactive Oxygen Species, and inhibit the intracellular enzyme thioredoxin reductase. Antiangiogenic agent 7 has anti-cancer activity, with an IC50 of 0.08-3.5 μM against cervical cancer cells HeLa, prostate cancer cells PC-3, and non-small cell lung cancer A549. Antiangiogenic agent 7 inhibits tumor growth in mouse xenograft models.
    Antiangiogenic agent 7
  • HY-170568
    Tubulin polymerization-IN-73
    		Inducer
    Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model.
    Tubulin polymerization-IN-73
  • HY-121382R
    Gypsogenin (Standard)
    		Inducer
    Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia.
    Gypsogenin (Standard)
  • HY-123357
    IMM-H004
    		Inhibitor
    IMM-H004, a coumarin derivative, possesses neuroprotective and potent free radical scavenging abilities. IMM-H004 significantly inhibits amyloid-β (Aβ)-induced cytotoxicity and apoptosis, offering potential value for research into neurodegenerative diseases such as Alzheimer's disease. Additionally, IMM-H004 is also capable of effectively blocking the calcium mobilization and chemotaxis induced by CKLF1-C27 (HY-P3418), thereby alleviating asthmatic pathological changes in the lung tissue of CKLF1 transgenic mice.
    IMM-H004
Cat. No. Product Name / Synonyms Application Reactivity