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-10211S
    Tanespimycin-d5
    Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
    Tanespimycin-d<sub>5</sub>
  • HY-173118
    EGFR-IN-152
    		Inducer
    EGFR-IN-152 (compound D4) is a potent EGFR tyrosine kinase inhibitor, exhibiting potent EGFRL858R/T790M/C797S inhibition activity (IC50 = 40 nM). EGFR-IN-152 induces G0/G1 phase cell cycle arrest and apoptosis, thereby inhibiting colony formation and cell proliferation of non-small cell lung cancer (NSCLC) cells. EGFR-IN-152 can be used for NSCLC research.
    EGFR-IN-152
  • HY-161205
    Thalidomide-PIP-(R)C-pyrrolidine-boc
    		Inducer
    Thalidomide-PIP-(R)C-pyrrolidine-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-PIP-(R)C-pyrrolidine-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-PIP-(R)C-pyrrolidine-boc
  • HY-183683
    DQ-9
    		Inducer
    DQ-9 is a selective immunoproteasome β5i inhibitor (IC50=0.0019 μM). DQ-9 generates additional inhibitory substances via iron-mediated intracellular activation, and induces oxidative stress, carbon-centered free radicals and macromolecular damage through its artemisinin domain. DQ-9 induces apoptosis in leukemia and multiple myeloma cells. DQ-9 exhibits selective cytotoxicity against leukemia and multiple myeloma cells by elevating the labile iron pool. DQ-9 can be used in the research of hematological malignancies (leukemia, multiple myeloma, mantle cell lymphoma, acute myeloid leukemia).
    DQ-9
  • HY-182003
    Anticancer agent 308
    		Inducer
    Anticancer agent 308 is an AKT inhibitor with antitumor activity. Anticancer agent 308 reduces total AKT protein levels, thereby inhibiting the pro-survival PI3K/AKT signaling pathway. Anticancer agent 308 induces apoptosis, disrupts mitochondrial membrane potential, promotes ROS accumulation in mitochondria, and induces cell cycle arrest. Anticancer agent 308 inhibits cancer cell migration. Anticancer agent 308 is applicable to research related to breast cancer, lung adenocarcinoma, cervical cancer, prostate cancer, and hepatocellular carcinoma.
    Anticancer agent 308
  • HY-W759435
    Niraparib-d5
    Niraparib-d5 (MK-4827-d5) is the deuterium labeled Niraparib (HY-10619). Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
    Niraparib-d<sub>5</sub>
  • HY-N4098R
    Incensole Acetate (Standard)
    		Modulator
    Incensole Acetate (Standard) is the analytical standard of Incensole Acetate. This product is intended for research and analytical applications. Incensole acetate is a main constituent of Boswellia carterii resin, has neuroprotective effects against neuronal damage in traumatic and ischemic head injury. Incensole acetate reduces Aβ25–35-triggered apoptosis in hOBNSCs.
    Incensole Acetate (Standard)
  • HY-173023
    IDOi-Pt(IV) prodrug-1
    		Inducer
    IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug. IDOi-Pt(IV) prodrug-1 inhibits IDO expression. IDOi-Pt(IV) prodrug-1 induces apoptosis, decreases the mitochondrial membrane potential, inhibits tumor cell migration and invasion. IDOi-Pt(IV) prodrug-1 induces reactive oxygen species-mediated endoplasmic reticulum stress and secretion of damage-associated molecular patterns (DAMPs), thereby presenting immunogenic cell death (ICD) effects. IDOi-Pt(IV) prodrug-1 has high-efficiency and low-toxicity antitumor effects compared to Cisplatin (HY-17394).
    IDOi-Pt(IV) prodrug-1
  • HY-156160
    Thalidomide-NH-C10-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-NH-C10-NH2 hydrochloride
  • HY-157432
    EGFR-IN-97
    		Inducer
    EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFRL858R/T790M/C797S and Ba/F3-EGFRDel19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFRL858R/T790M/C797S cells at the concentration of 0.8 μM.
    EGFR-IN-97
  • HY-168475
    DD0-2363
    		Inhibitor
    DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia.
    DD0-2363
  • HY-125209A
    TH5427 hydrochloride
    		Control
    TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9.TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis.TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells.TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells.TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay.TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA).TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells.TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells.TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines.TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer.
    TH5427 hydrochloride
  • HY-161184
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
    		Inducer
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-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.
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
  • HY-181009
    HDAC-IN-98
    		Inducer
    HDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively. HDAC-IN-98 induces H3K9 acetylation, p21 upregulation, G2/M arrest, cell apoptosis, has strong antiproliferative effects in colorectal cancer cells, low toxicity in healthy colon epithelium, modulates short-term in vitro effects via autophagy, and shows strong antitumor efficacy in vivo in the chorioallantoic membrane model (CAM) assay. HDAC-IN-98 can be used for the research of colorectal cancer.
    HDAC-IN-98
  • HY-179418
    Ceritinib-platinum(IV)-4-phenylbutyrate
    		Inducer
    Ceritinib-platinum(IV)-4-phenylbutyrate (complex 7) is a Ceritinib (HY-15656)-conjugated Platinum(IV) prodrug with anticancer activity. Ceritinib-platinum(IV)-4-phenylbutyrate induces S-phase arrest, DNA damage responses, and apoptosis. Ceritinib-platinum(IV)-4-phenylbutyrate combines cytotoxicity with immune and anti-invasive activation in cancer cell models. Ceritinib-platinum(IV)-4-phenylbutyrate can be used for cancer research, such as non-small cell lung cancer (NSCLC).
    Ceritinib-platinum(IV)-4-phenylbutyrate
  • HY-180948
    PZ-11
    		Inducer
    PZ-11 is a derivative of thiazolidinedione with anti-tumor activity. PZ-11 can induce cancer cells apoptosis by downregulating anti-apoptotic gene AIFM1, BAG3 and BIRC3 and regulating pro-apoptotic gene BAD, HRK, CASP10 and CASP10. PZ-11 can be used for research of breast cancer.
    PZ-11
  • HY-181587
    PDGFRA/CAIX/XII-IN-1
    		Inducer
    PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.
    PDGFRA/CAIX/XII-IN-1
  • HY-P10508
    Pantinin-1
    Pantinin-1 is an antimicrobial peptide found in the venom of the Pandinus imperator scorpion. Pantinin-1 has potent antimicrobial activity against Gram-positive bacteria and fungi, weak antimicrobial activity against Gram-negative bacteria, and very low hemolytic activity against human erythrocytes. Pantinin-1 also has anticancer activity and can induce apoptosis in tumor cells.
    Pantinin-1
  • HY-144340
    Antitumor agent-43
    		Inducer
    Antitumor agent-43 (Compound 4B) is a potent antitumor agent, with an IC50of 0.5 µM for (T-24 cell). Antitumor agent-43 (Compound 4B) induces cell cycle arrest at G2/M phase.
    Antitumor agent-43
  • HY-115589
    YLT-11
    		Inducer
    YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity.
    YLT-11
Cat. No. Product Name / Synonyms Application Reactivity