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-120569
    NC-001
    		Inducer
    NC-001 is a selective apoptosis inducer targeting renal proximal tubular cells and renal cancer cells. NC-001 inhibits tumor growth in clear cell renal cell carcinoma (CCRCC) xenograft models. NC-001 is promising for research of metastatic renal cell carcinoma.
    NC-001
  • HY-182624
    FJ9
    		Inducer
    FJ9 is a NHERF1/PDZ inhibitor with human NHERF1 PDZ1 IC50 1540 μM, NHERF1 PDZ2 IC50 160 μM, and Frizzled-7-Dishevelled PDZ complex Ki 10 μM. FJ9 binds ligand-binding pockets of NHERF1 PDZ domains to block cognate ligand interactions, disrupts Frizzled-7-Dishevelled interactions, and down-regulates canonical Wnt signaling. FJ9 induces apoptosis in cancer cells with intact β-catenin signaling. FJ9 can be used for the research of non-small cell lung cancer, melanoma.
    FJ9
  • HY-P3779
    Amyloid 17-42
    		Inducer
    Amyloid 17-42 (Aβ(17-42)) is a major constituent of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, derived by alpha- and gamma-secretase cleavage of the amyloid precursor protein (APP). Amyloid 17-42 can induce neuronal apoptosis via a Fas-like/caspase-8 activation pathway.
    Amyloid 17-42
  • HY-174803
    WMJ-J-09
    		Inducer 98.44%
    WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].
    WMJ-J-09
  • HY-153802A
    Antitumor agent-100 hydrochloride
    		Inducer
    Antitumor agent-100 (compound A6) hydrochloride is an orally potent apoptosis inducer and molecular gel targeting PDE3A-SLFN12 (IC50: 0.3 μM) with antitumor activity. Antitumor agent-100 hydrochloride binds to the PDE3A enzyme pocket to recruit and stabilize SLFN12, thereby preventing protein translation and leading to apoptosis.
    Antitumor agent-100 hydrochloride
  • HY-N9684
    Degalactotigonin
    		Inducer
    Degalactotigonin is a saponin-selective inhibitor targeting the EGFR, GSK3β and Hedgehog/Gli1 pathways and can be isolated from Solanum nigrum (Solanum nigrum). Degalactotigonin inhibits EGFR phosphorylation and the downstream Akt/ERK signaling pathway, and at the same time inhibits the Hedgehog/Gli1 pathway through GSK3β inactivation, thereby inducing cancer cell apoptosis, arresting the cell cycle, and inhibiting migration and invasion. Degalactotigonin can be used in targeted research on malignant tumors such as pancreatic cancer and osteosarcoma.
    Degalactotigonin
  • HY-155785
    MTP
    		Inducer
    MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma.
    MTP
  • HY-162774
    GRP75-IN-1
    		Inducer
    GRP75-IN-1 (Compound 33) is an anti-endometrial cancer (EC) agent. GRP75-IN-1 induces apoptosis in endometrial cancer cells. GRP75-IN-1 hydrochloride reduces mitochondrial Ca2+ levels by targeting GRP75 and disrupting its interaction with IP3R. GRP75-IN-1 inhibits tumor growth in human endometrial cancer xenograft animal models. GRP75-IN-1 can be used for research in endometrial cancer.
    GRP75-IN-1
  • HY-150685
    Topo I/COX-2-IN-1
    		Inducer
    Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity.
    Topo I/COX-2-IN-1
  • HY-175020
    QNX-10
    		Inducer
    QNX-10 is a fatty acid synthase (FASN) inhibitor (IC50 = 0.7 μM) with anticancer activity. QNX-10 exhibits potent FASN inhibition and cytotoxicity against colorectal and breast cancer cells. QNX-10 induces apoptosis and cell cycle arrest in S phase by upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-xL. QNX-10 can be used to investigate anticancer therapies targeting FASN enzymes.
    QNX-10
  • HY-W011311S
    Eicosapentaenoic acid methyl ester-d5
    Eicosapentaenoic acid methyl ester-d5 is the deuterium labeled Eicosapentaenoic acid methyl ester. Eicosapentaenoic acid methyl ester is a degradant of a monogalactosyl diacylglycerol (an anticancer compound by inducing apoptosis).
    Eicosapentaenoic acid methyl ester-d<sub>5</sub>
  • HY-176719
    AKR1B1/STAT3/SLC7A11-regulator-1
    		Inducer
    AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is an AKR1B1/STAT3/SLC7A11 regulator that reverses DOX resistance in MCF-7/ADR cells by enhancing ferroptosis activity. AKR1B1/STAT3/SLC7A11-regulator-1 can be used in breast cancer research.
    AKR1B1/STAT3/SLC7A11-regulator-1
  • HY-161200
    Thalidomide-piperazine-C-azetidine-C2-OH
    		Inducer
    Thalidomide-piperazine-C-azetidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-C-azetidine-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-C-azetidine-C2-OH
  • HY-183335
    SMO-IN-6
    		Inducer
    Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma.
    SMO-IN-6
  • HY-P11264
    Cyclic peptide P1-1
    		Inhibitor
    Cyclic peptide P1-1 is a high-potent GPR55 antagonist. Cyclic peptide P1-1 antagonizes GPR55 and suppresses collagen secretion. Cyclic peptide P1-1 reduces ROS production, attenuates ER stress, and inhibits mitochondria-associated Apoptosis. Cyclic peptide P1-1 inhibits the expression of α-SMA and COL1α. Cyclic peptide P1-1 ameliorates CCl4 (HY-Y0298)-induce and MCD-diet-induce acute liver inflammation and fibrosis.
    Cyclic peptide P1-1
  • HY-149569
    Thalidomide-5-O-C12-NH2 hydrochloride
    		Inducer 99.90%
    Thalidomide-5-O-C12-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C12-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C12-NH2 hydrochloride
  • HY-151429
    Antitumor agent-77
    		Inducer
    Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells.
    Antitumor agent-77
  • HY-N17383
    Ligusticum cycloprolactam
    		Inhibitor
    Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease.
    Ligusticum cycloprolactam
  • HY-157323
    HDAC6-IN-28
    		Inducer
    HDAC6-IN-28 (compound 10C) is a potent inhibitor of HDAC6 with an IC50 of 261 nM. HDAC6-IN-28 significantly induces apoptosis and S-phase arrest in B16-F10 cells. HDAC6-IN-28 efficiently increases the expression of acetylated-α-tubulin in vitro and in vivo.
    HDAC6-IN-28
  • HY-153761
    ASK1-IN-4
    		Modulator
    ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC50=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1.
    ASK1-IN-4
Cat. No. Product Name / Synonyms Application Reactivity