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-181757
    DCAF11 ligand-Linker Conjugate 1
    		Control
    DCAF11 ligand-Linker Conjugate 1 is a conjugate of a DCAF11 ligand and a linker. DCAF11 ligand-Linker Conjugate 1 can be used for the synthesis of PROTAC LGF308 (HY-181756).
    DCAF11 ligand-Linker Conjugate 1
  • HY-15682R
    TTNPB (Standard)
    		Inducer
    TTNPB (Standard) is the analytical standard of TTNPB. This product is intended for research and analytical applications. TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
    TTNPB (Standard)
  • HY-P10656
    Ac-DEVDD-TPP
    		Inducer
    Ac-DEVDD-TPP is a porphyrin derivative that can be converted into D-TPP by caspase-3 cleavage and laser irradiation. The formed porphyrin nanofibers can effectively induce Apoptosis and Pyroptosis. Ac-DEVDD-TPP has antitumor activity.
    Ac-DEVDD-TPP
  • HY-N7063R
    Nerol (Standard)
    		Inducer
    Nerol (Standard) is the analytical standard of Nerol. This product is intended for research and analytical applications. Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca2+ and ROS. Antifungal activity.
    Nerol (Standard)
  • HY-155226
    FLT3-IN-21
    		Inducer
    FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%).
    FLT3-IN-21
  • HY-13270A
    ABT-751 hydrochloride
    		Inducer
    ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer.
    ABT-751 hydrochloride
  • HY-183120
    EGFR T790M/FAK-IN-2
    		Inducer
    EGFR T790M/FAK-IN-2 is an orally active dual FAK and EGFRT790M kinase inhibitor, with an IC50 of 1.03 nM against FAK and an IC50 of 3.89 nM against EGFRT790M. EGFR T790M/FAK-IN-2 exerts antiproliferative effects in drug-resistant cancer cells overexpressing FAK, inducing apoptosis and cell cycle arrest. EGFR T790M/FAK-IN-2 exhibits antitumor activity in a pancreatic cancer xenograft mouse model. EGFR T790M/FAK-IN-2 can be used for the research of pancreatic cancer, breast cancer and non-small cell lung cancer.
    EGFR T790M/FAK-IN-2
  • HY-163451
    Apoptosis inducer 17
    		Inducer
    Apoptosis inducer 17 is a Curcumin-Piperlongumine hybrid molecule that increases cell cycle arrest and apoptosis through activating JNK signaling pathway in lung cancer cells.
    Apoptosis inducer 17
  • HY-138185
    Collismycin A
    		Inhibitor
    Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae in a model of neuronal cell death induced by all-trans retinoic acid.
    Collismycin A
  • HY-117182
    LG190178
    LG190178 is a non-steroidal vitamin D receptor (VDR) ligand that can induce the formation of heterodimer complexes between VDR and retinoid X receptor (RXR), stabilizing the agonistic conformation of the VDR ligand-binding domain and promoting its interaction with co-activators. LG190178 has functions in regulating calcium homeostasis, bone mineralization, as well as cell proliferation, differentiation, and apoptosis, making it useful for research in psoriasis, osteoporosis, and cancer.
    LG190178
  • HY-W751179
    Midostaurin-13C6
    Midostaurin-13C6 (PKC412-13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
    Midostaurin-<sup>13</sup>C<sub>6</sub>
  • HY-155242
    VEGFR-2-IN-36
    		Inducer
    VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM).
    VEGFR-2-IN-36
  • HY-106981
    Orazipone
    		Inducer
    Orazipone (OR 1384) is a small molecule immunomodulator with strong anti-inflammatory properties. Orazipone exerts its immunomodulatory effect by forming reversible thiol complexes, which bind to intracellular signaling proteins and the thiol groups of glutathione. Orazipone exhibits potent anti-eosinophilic activity by inducing apoptosis. Orazipone inhibits activation of inflammatory transcription factors NF-kB and STAT 1 and decreases inducible iNOS expression and NO production in response to inflammatory stimuli. Orazipone reduces NADPH oxidase activity and thereby decreases ROS production. Orazipone has a protective effect in intestinal radiation injury.
    Orazipone
  • HY-155490
    Nur77 antagonist 1
    		Inducer
    Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells.
    Nur77 antagonist 1
  • HY-168843
    PSP205
    		Inducer
    PSP205 is a potent anticancer agent. PSP205 shows cytotoxicity. PSP205 induces apoptosis. PSP205 induces ER-stress-mediated autophagy. PSP205 increases the protein expression of LC3BII and increases the CHOP and spliced XBP1 at the mRNA and protein levels.
    PSP205
  • HY-N2435R
    [8]-Shogaol (Standard)
    		Inducer
    -Shogaol (Standard) is the analytical standard of -Shogaol. This product is intended for research and analytical applications. -Shogaol, a kind of stimulating compound in ginger, has antiplatelet (IC50=5 μM), anti-cancer and anti-inflammatory activity. -Shogaol inhibited COX-2 (IC50=17.5 μM), which led to the decline of human leukemia cells. 8-Shogaol Selective direction TAK1 sum TAK1-TAB1 (IC50=5 μM), suppress IKK, Akt sum MAPK signal pathway, and reverse synovitis synovial sum Air dampness (RA).
    [8]-Shogaol (Standard)
  • HY-168502
    HDAC-IN-81
    		Inducer
    HDAC-IN-81 (Compound 11g) is an HDAC inhibitor that can effectively inhibit HDAC1 (IC50 = 4.5 nM). HDAC-IN-81 possesses anti-cancer cell proliferation activity and can induce cell apoptosis.
    HDAC-IN-81
  • HY-175176
    HDAC1/6-IN-3
    		Inducer
    HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.
    HDAC1/6-IN-3
  • HY-13605S1
    Cytarabine-13C,15N2
    		Inducer
    Cytarabine-13C,15N2 (Cytosine β-D-arabinofuranoside-13C,15N2) is the 13C- and 15N-labeled Cytarabine (HY-13605). Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV. Cytarabine shows anti-orthopoxvirus activity.
    Cytarabine-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • HY-W794759
    Valproic acid magnesium
    		Inducer
    Valproic acid magnesium (Magnesium valproate) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid magnesium inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid magnesium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid magnesium is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
    Valproic acid magnesium
Cat. No. Product Name / Synonyms Application Reactivity