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-13502
    Mitoxantrone
    		Inducer 99.58%
    Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity. Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone
  • HY-B1081
    Oxidopamine hydrochloride
    		Inducer 99.91%
    Oxidopamine (6-OHDA) hydrochloride is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrochloride is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrochloride promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrochloride can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.
    Oxidopamine hydrochloride
  • HY-N0171A
    Beta-Sitosterol (purity>98%)
    		Inducer 99.74%
    Beta-Sitosterol (purity>98%) is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
    Beta-Sitosterol (purity>98%)
  • HY-N0176
    Dihydroartemisinin
    		Inducer 99.03%
    Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin
  • HY-10422
    AZD-8055
    		Inducer 99.60%
    AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
    AZD-8055
  • HY-101193
    Zinc Protoporphyrin
    		Inducer 99.87%
    Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor. Zinc Protoporphyrin regulates expression of HO-1 at the transcriptional level. The effect of Zinc Protoporphyrin on HO-1 expression is controversial.  It was shown to induce HO-1 expression in some cells, but suppress it in others. Zinc Protoporphyrin is used as a screening marker of iron deficiency in vivo. Zinc Protoporphyrin has anti-cancer activity.
    Zinc Protoporphyrin
  • HY-N0150
    Monensin sodium
    		Inducer ≥98.0%
    Monensin (Monensin A) sodium, an orally active antibiotic, is an ionophore that mediates Na+/H+ exchange. Monensin sodium is a potent Wnt signaling inhibitor. Monensin sodium causes a marked enlargement of the multivesicular bodies (MVBs) and regulates exosome secretion. Monensin sodium can be used for bacterial, fungal, and parasitic infections research, and shows anticancer effects.
    Monensin sodium
  • HY-P2149
    Concanavalin A
    		Inducer
    Concanavalin A is a Ca2+/Mn2+-dependent and mannose/glucose-binding plant lectin that can be found in jack bean. Concanavalin A can induce programmed cell death. Concanavalin A can be used to induce acute hepatic injury.
    Concanavalin A
  • HY-B0239
    Chloramphenicol
    		Inhibitor 99.93%
    Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research.
    Chloramphenicol
  • HY-12215
    Lorlatinib
    		Inducer 99.92%
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R), respectively.
    Lorlatinib
  • HY-16214
    FX-11
    		Inducer 99.21%
    FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.
    FX-11
  • HY-16591
    Birinapant
    		Inducer 99.70%
    Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.
    Birinapant
  • HY-15648B
    GSK-J4
    		Inducer 99.45%
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
    GSK-J4
  • HY-10005
    Flavopiridol
    		Inducer 99.73%
    Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
    Flavopiridol
  • HY-10585A
    Valproic acid sodium
    		Inducer 99.65%
    Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
    Valproic acid sodium
  • HY-P99974
    Nab-Paclitaxel
    		Inducer 99.70%
    Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and solid tumors. (The product specifications below only indicate the effective content of Paditaxel, the actual albumin quality depends on the batch; the ratio of each ingredient in this product is Paditaxel: albumin -1:7~1:11).
    Nab-Paclitaxel
  • HY-13001
    Quizartinib
    		Inducer 99.08%
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
    Quizartinib
  • HY-B0285
    Amiloride
    		Inducer 99.96%
    Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
    Amiloride
  • HY-156498
    RMC-7977
    		99.48%
    RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRASG12C cancer models, and demonstrates good tolerability across various RAS cancer models.
    RMC-7977
  • HY-12137
    Volasertib
    		Inducer 99.87%
    Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models.
    Volasertib
Cat. No. Product Name / Synonyms Application Reactivity