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-13270
    ABT-751
    		Inducer 98.74%
    ABT-751 (E7010) 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 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer.
    ABT-751
  • HY-143230
    Custirsen
    Custirsen is a highly specific antisense oligonucleotide that inhibits the production of clusterin , an antiapoptotic protein that is upregulated in response to chemotherapy and that confers treatment resistance.
    Custirsen
  • HY-N1378
    (E)-Cardamonin
    		Inducer 99.84%
    (E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
    (E)-Cardamonin
  • HY-10088
    Zibotentan
    		Inducer 99.37%
    Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.
    Zibotentan
  • HY-12456
    Duocarmycin SA
    		Inducer 99.89%
    Duocarmycin SA is an orally active antitumor antibiotic with an IC50 of 10 pM. Duocarmycin SA is an extremely potent cytotoxic agent capable of inducing a sequence-selective alkylation of duplex DNA. Duocarmycin SA demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells treated with proton radiation in vitro.
    Duocarmycin SA
  • HY-13010
    Laquinimod
    		Inducer 99.46%
    Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research.
    Laquinimod
  • HY-16350
    BOLD-100
    		Inducer
    BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.
    BOLD-100
  • HY-156671
    RMC-4998
    		Inducer 99.31%
    RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research.
    RMC-4998
  • HY-P99371
    Lirentelimab
    		Inducer 99.91%
    Lirentelimab (AK002) is a humanized IgG1 monoclonal antibody that targets sialic acid-binding Ig-like lectin 8 (SIGLEC8). Lirentelimab induces cell apoptosis of IL-5-activated eosinophils and inhibits IgE-mediated mast cell activation. Lirentelimab can be used for the research of eosinophilic gastritis and duodenitis.
    Lirentelimab
  • HY-13334
    BGT226 maleate
    		Activator 99.92%
    BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
    BGT226 maleate
  • HY-124586
    Streptonigrin
    		Activator 99.20%
    Streptonigrin (Bruneomycin) is an orally active antibiotic and pan-PAD inhibitor, inhibiting PAD1, PAD2, PAD3 and PAD4 with IC50 of 48.3 μM, 26.1 μM, 0.43 μM and 2.5 μM, respectively. Streptonigrin inhibits SENP1 (IC50 of 0.518 μM) and reduces HIF1α. Streptonigrin increases p53 and Apoptosis. Streptonigrin shows antiviral activity against Rauscher murine leukemia virus. Streptonigrin has immunosuppressive effects. Streptonigrin has antitumor activity against osteosarcoma.
    Streptonigrin
  • HY-136650A
    Fludarabine triphosphate trisodium
    		Inducer 99.98%
    Fludarabine triphosphate (F-ara-ATP) trisodium, the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate trisodium inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate trisodium inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis.
    Fludarabine triphosphate trisodium
  • HY-B0174
    Olsalazine Disodium
    		Inducer 99.82%
    Olsalazine Disodium is an orally active prodrug of 5-ASA (HY-15027). Olsalazine Disodium can inhibit cells proliferation and induce apoptosis. Olsalazine Disodium can reduce DAI and MPO activity and inhibit inflammatory cytokines levels. Olsalazine Disodium can be used for the researches of cancer, inflammation and metabolic disease, such as colorectal cancer, inflammatory bowel disease (IBD) and hyperuricemic.
    Olsalazine Disodium
  • HY-133121
    WDR5-IN-1
    		Inducer 98.0%
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.
    WDR5-IN-1
  • HY-153385
    TMX1
    		99.57%
    TMX1 is a BRD4 covalent molecular glue degrader. TMX1 selectively recruits DCAF16 to the BRD4BD2, leading to BRD4 degradation.
    TMX1
  • HY-13775
    XL019
    		Inducer 99.65%
    XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
    XL019
  • HY-B0174A
    Olsalazine
    		Inducer 99.83%
    Olsalazine is an orally active prodrug of 5-ASA (HY-15027). Olsalazine can inhibit cells proliferation and induce apoptosis. Olsalazine can reduce DAI and MPO activity and inhibit inflammatory cytokines levels. Olsalazine can be used for the researches of cancer, inflammation and metabolic disease, such as colorectal cancer, inflammatory bowel disease (IBD) and hyperuricemic.
    Olsalazine
  • HY-144256
    CHD1Li 6.11
    		Inducer 99.54%
    CHD1Li 6.11 is a potent and orally active Chromodomain Helicase DNA Binding Protein 1 Like (CHD1L) (oncogenic gene) inhibitor (IC50 = 3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 can inhibit EMT, induce mesenchymal-epithelial transition (reverse EMT) and promote apoptosis in tumor organoid models. CHD1Li 6.11 can be used for the research of cancer, such as colorectal cancer.
    CHD1Li 6.11
  • HY-50672
    MK-0731
    		Inducer 99.85%
    MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy.
    MK-0731
  • HY-19934A
    Pifusertib hydrochloride
    		Inducer 99.90%
    Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy.
    Pifusertib hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity