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-175821
    PRMT1-IN-3
    		Inducer
    PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC.
    PRMT1-IN-3
  • HY-108654
    PSB 0474
    		Inducer
    PSB 0474 (3-phenacyl-UDP) is a UDP (HY-113359) analog and selective P2Y6 receptor agonist, with an EC50 value of 70 nM for the hP2Y6 receptor. PSB 0474 activates Phospholipase C-coupled receptors to increase intracellular inositol phosphate levels. PSB 0474 enhances NO release by upregulating inducible iNOS and induces Apoptosis. PSB 0474 increases micturition frequency in urine of anesthetized rats, without altering bladder contraction amplitude/duration or causing urothelial damage. PSB 0474 can be used in studies related to chronic brain inflammation.
    PSB 0474
  • HY-N6258R
    Kahweol (Standard)
    		Inducer
    Kahweol (Standard) is the analytical standard of Kahweol. This product is intended for research and analytical applications. Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
    Kahweol (Standard)
  • HY-181717
    TKL002
    		Inducer
    TKL002 is a blood-brain barrier-permeable inhibitor of the CTH/H2S/NF-κB/EMT signaling axis. TKL002 induces G2/M phase cell cycle arrest and apoptosis in glioblastoma cells. TKL002 inhibits the migration and invasion of glioblastoma cells by upregulating E-cadherin and downregulating N-cadherin and vimentin. TKL002 is applicable to relevant research on glioblastoma.
    TKL002
  • HY-15733R
    Lucidin (Standard)
    		Inducer
    Lucidin (Standard) is the analytical standard of Lucidin. This product is intended for research and analytical applications. Lucidin (NSC 30546) is a natural component of madder and can induce mutations in bacterial and mammalian cells.
    Lucidin (Standard)
  • HY-149633
    EGFR/HER2/DHFR-IN-3
    		Inducer
    EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells.
    EGFR/HER2/DHFR-IN-3
  • HY-149017
    Apoptosis inducer 7
    		Inducer
    Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity.
    Apoptosis inducer 7
  • HY-118874C
    Oblimersen sodium scrambled negative control
    		Inhibitor
    Oblimersen sodium scrambled negative control is the sequence scrambled negative control of Oblimersen sodium.
    Oblimersen sodium scrambled negative control
  • HY-157212
    PARP-1/Proteasome-IN-1
    		Inducer
    PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis.
    PARP-1/Proteasome-IN-1
  • HY-181611
    Polθ-IN-10
    		Inducer
    Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers.
    Polθ-IN-10
  • HY-180838
    WW-104
    		Inducer
    WW-104 is a selective USP10 inhibitor with an IC50 of 16.75 μM, a Kd of 237 nM. WW-104 induces the G2 phase arrest and cell Apoptosis. WW-104 exhibits significant anti-proliferative effects across USP10-overexpressing cell lines. WW-104 has anti-cancer effects against hepatocellular carcinoma.
    WW-104
  • HY-N0128R
    Sclareol (Standard)
    		Inducer
    Sclareol (Standard) is the analytical standard of Sclareol. This product is intended for research and analytical applications. Sclareol is isolated from Salvia sclarea with anticarcinogenic activity. Sclareol shows strong cytotoxic activity against mouse leukemia (P-388), human epidermal carcinoma (KB) cells and human leukemia cell lines. Sclareol induces cell apoptosis.
    Sclareol (Standard)
  • HY-181823
    HOXA1-IN-1
    		Inducer
    HOXA1-IN-1 is a HOXA1 inhibitor. HOXA1-IN-1 downregulates HOXA1 protein levels, suppresses its transcriptional activity, and alters the expression of its downstream target genes. HOXA1-IN-1 induces DNA damage and apoptosis in cancer cells. HOXA1-IN-1 exhibits antitumor efficacy in xenograft models of colorectal cancer and triple-negative breast cancer. HOXA1-IN-1 shows synergistic activity in combination with Cisplatin (HY-17394). HOXA1-IN-1 can be used for the research of colorectal cancer and triple-negative breast cancer.
    HOXA1-IN-1
  • HY-170762A
    (+)-Mcl-1 inhibitor 21
    		Inducer
    (+)-Mcl-1 inhibitor 21 (Example 1-37) is a Mcl-1 inhibitor with an IC50 of 172 nM. (+)-Mcl-1 inhibitor 21 exhibits proapototic and anti-proliferation activities against SUDHL5 and SUDHL10 cell lines and can be utilized in cancer research.
    (+)-Mcl-1 inhibitor 21
  • HY-168953
    Lysosomal P-gp targeted agent 1
    		Inducer
    Lysosomal P-gp targeted agent 1 (Compound 14) is an anti-tumor agent targeting lysosomal P-glycoprotein (Pgp). Lysosomal P-gp targeted agent 1 is selectively transported into lysosomes by overexpressed Pgp, release nitric oxide (NO) to generate reactive oxygen species (ROS), resulting in lysosomal membrane permeabilization (LMP) and inducing apoptosis. Lysosomal P-gp targeted agent 1 can overcome P-glycoprotein-mediated drug resistance and lead to cell cycle arrest, but relatively low toxicity to normal cells. Lysosomal P-gp targeted agent 1 has antitumor activity, significantly inhibits tumor volume.
    Lysosomal P-gp targeted agent 1
  • HY-N0747R
    Oxypeucedanin (Standard)
    		Inducer
    Oxypeucedanin (Standard) is a furanocoumarin derivative found in Angelica dahurica. Oxypeucedanin (Standard) is an orally active PI3K/AKT/NF-κB, MAPK, and ROS inhibitor. Oxypeucedanin (Standard) induces cell cycle arrest and apoptosis. Oxypeucedanin (Standard) inhibits hKv1.5 channel currents (IC50: 76 nM). Oxypeucedanin (Standard) exhibits anticancer, anti-inflammatory, antioxidant and antiarrhythmic activities.
    Oxypeucedanin (Standard)
  • HY-126675G
    AS2863619 (GMP)
    		Inducer
    AS2863619 GMP is AS2863619 (HY-126675) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AS2863619 is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 targets Stat5a-CDK8/19 to promote the differentiation of CD4+ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 can be applied to research in related fields such as periodontitis-induced bone defects.
    AS2863619 (GMP)
  • HY-167839
    (R)-JAK2/STAT3-IN-1
    (R)-JAK2/STAT3-IN-1 is a GP130 D1 domain inhibitor with anti-tumor activity. (R)-JAK2/STAT3-IN-1 can inhibit the phosphorylation of JAK2 and STAT3. The affinity of (R)-JAK2/STAT3-IN-1 for GP130 protein is 3.8 μM. (R)-JAK2/STAT3-IN-1 effectively inhibits the viability and migration of tumor cells and promotes apoptosis.
    (R)-JAK2/STAT3-IN-1
  • HY-149062
    Anticancer agent 102
    		Inducer
    Anticancer agent 102 is a derivative of tetracaine. Anticancer agent 102 has anti-cancer activity. Anticancer agent 102 induces apoptosis.
    Anticancer agent 102
  • HY-149571
    Thalidomide-5-O-C14-NH2 hydrochloride
    		Inducer
    Thalidomide-5-O-C14-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C14-NH2 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity