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-14930
    Mirodenafil
    		Inhibitor 99.88%
    Mirodenafil (SK3530) is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil is a glucocorticoid receptor (GR) modulator Mirodenafil activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc).
    Mirodenafil
  • HY-B1139
    Tolperisone hydrochloride
    		Inducer 99.84%
    Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity.
    Tolperisone hydrochloride
  • HY-18696
    AMG-337
    		Inducer 99.42%
    AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.
    AMG-337
  • HY-15228
    RX-3117
    		Inducer 99.25%
    RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis.
    RX-3117
  • HY-18707
    K-Ras(G12C) inhibitor 12
    		Inducer 99.57%
    K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity.
    K-Ras(G12C) inhibitor 12
  • HY-112724
    Ivarmacitinib
    		Inducer 99.82%
    Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
    Ivarmacitinib
  • HY-157396
    JAB-2485
    		Inducer 98.11%
    JAB-2485 is a potent and selective Aurora kinase A (AURKA) inhibitor, with an IC50 of 0.33 nM. JAB-2485 exhibits around 1700-fold selectivity for AURKA over AURKB. JAB-2485 induces cell cycle arrest and apoptosis. JAB-2485 can be used for the research of cancer.
    JAB-2485
  • HY-156694
    Hydroxy-PP-Me
    		Modulator 99.92%
    Hydroxy-PP-Me is a selective CBR1 inhibitor with an IC50 of 759 nM. Hydroxy-PP-Me can inhibit serum starvation-induced apoptosis. Hydroxy-PP-Me can enhance the cytotoxic effects of Daunorubicin (HY-13062A) and As2O3 on tumor cells. Hydroxy-PP-Me can be used in the research of cancer such as leukemia.
    Hydroxy-PP-Me
  • HY-159480
    AD1058
    		Inducer 98.11%
    AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC50: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases.
    AD1058
  • HY-102048
    STAT5-IN-2
    		Inhibitor 99.08%
    STAT5-IN-2 is a STAT5 inhibitor, extracted from reference 1, example 17f. STAT5-IN-2 has potent antileukemic effect.
    STAT5-IN-2
  • HY-157562
    DS68591889
    		Inducer 99.18%
    DS68591889 is a selective and orally active phosphatidylserine synthase 1 (PTDSS1) inhibitor. DS68591889 has no inhibitory activity against PTDSS2. DS68591889 induces the phospholipid imbalance in a wide range of cancer cells. DS68591889 negatively regulates B cell receptor (BCR)-induced Ca2+ signaling and subsequent apoptotic cell death. DS68591889 can be used for the cancer research, such as B cell lymphoma.
    DS68591889
  • HY-B0185B
    Lidocaine hydrochloride hydrate
    		Inducer 99.90%
    Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine hydrochloride hydrate
  • HY-B0612
    Lercanidipine
    		Inhibitor 99.65%
    Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research.
    Lercanidipine
  • HY-13224
    AZD4877
    		Degrader 99.49%
    AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity.
    AZD4877
  • HY-101029
    MBM-55
    		Inducer 99.94%
    MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
    MBM-55
  • HY-13628
    Etalocib
    		Inducer 99.03%
    Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
    Etalocib
  • HY-145729
    Danvatirsen
    		Inducer
    Danvatirsen is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.
    Danvatirsen
  • HY-P99332
    Visilizumab
    		Inducer 98.48%
    Visilizumab (Anti-Human CD3E Recombinant Antibody) is a humanized low-Fc receptor binding anti-CD3 monoclonal IgG2 antibody. Visilizumab can be used for ulcerative colitis and Crohn's disease research.
    Visilizumab
  • HY-147293
    Nenocorilant
    		Inducer 99.72%
    Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research.
    Nenocorilant
  • HY-N2554
    Osthenol
    		Inducer 99.27%
    Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC50=0.74 μM, Ki=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer.
    Osthenol
Cat. No. Product Name / Synonyms Application Reactivity