1. Signaling Pathways
  2. Apoptosis
  3. Apoptosis

Apoptosis

Apoptosis

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-41067
    Taltobulin intermediate-6
    Control
    Taltobulin intermediate-6 is an intermediate in the synthesis of Taltobulin (HY-15584). Taltobulin is a common toxin component in ADC preparation (ADC Cytotoxin), and it is also a powerful tubulin (Microtubule/Tubulin) inhibitor. Taltobulin disrupts tubulin polymerization, induces mitotic arrest, and induces apoptosis.
    Taltobulin intermediate-6
  • HY-156872
    MTX-216
    Inducer
    MTX-216 is a dual ATP-competitive inhibitor of PI3K and EGFR. MTX-216 cosuppresses Ki-67 and ribosomal S6 phosphorylation and induces apoptosis in NF1LOF cells. MTX-216 suppresses the activity of SYK kinase, with an IC50 of 281 nM. MTX-216 is used in the research of Melanoma.
    MTX-216
  • HY-107595
    SD-1008
    Inducer 99.10%
    SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway.
    SD-1008
  • HY-111207
    CA224
    Inducer 99.94%
    CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC50 of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.
    CA224
  • HY-161358
    FAK-IN-20
    Inducer
    FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS.
    FAK-IN-20
  • HY-10971A
    Alisertib sodium
    Inducer
    Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
    Alisertib sodium
  • HY-50895B
    Gefitinib dihydrochloride
    Inducer
    Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
    Gefitinib dihydrochloride
  • HY-18085S2
    Quercetin-13C3
    Inducer
    Quercetin-13C3 is the 13C-labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
    Quercetin-<sup>13</sup>C<sub>3</sub>
  • HY-17386B
    Rosiglitazone potassium
    Inducer 99.13%
    Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.
    Rosiglitazone potassium
  • HY-10587A
    BIX-01294 hydrochloride hydrate
    Inducer
    BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.
    BIX-01294 hydrochloride hydrate
  • HY-10261D
    Afatinib oxalate
    Inducer
    Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib oxalate
  • HY-18750A
    Zorifertinib hydrochloride
    Inducer
    Zorifertinib (AZD3759) hydrochloride is a potent, orally active, BBB-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research.
    Zorifertinib hydrochloride
  • HY-50895G
    Gefitinib (GMP)
    Inducer
    Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor.
    Gefitinib (GMP)
  • HY-13016A
    Cabozantinib hydrochloride
    Inducer
    Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
    Cabozantinib hydrochloride
  • HY-18174C
    Prexasertib mesylate
    Inducer
    Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity.
    Prexasertib mesylate
  • HY-10201S1
    Sorafenib-d4
    Inducer 99.9%
    Sorafenib-d4 (Bay 43-9006-d4) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
    Sorafenib-d<sub>4</sub>
  • HY-13768C
    Topotecan hydrochloride hydrate
    Inducer
    Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
    Topotecan hydrochloride hydrate
  • HY-130247C
    Flonoltinib sulfate
    Inducer
    Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. Flonoltinib maleate has anti-cancer activity.
    Flonoltinib sulfate
  • HY-135317B
    Emavusertib hydrochloride
    Inducer
    Emavusertib hydrochloride (CA-4948 tosylate) is the hydrochloride salt form of Emavusertib (HY-135317). Emavusertib hydrochloride is an orally active inhibitor for IRAK4 (IC50=57 nM) and FLT3. Emavusertib hydrochloride inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib hydrochloride exhibits antitumor activity in mouse model.
    Emavusertib hydrochloride
  • HY-183626
    TM5614 sodium
    Inducer
    TM5614 sodium is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. TM5614 sodium blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. TM5614 sodium restores macrophage efferocytosis and promotes macrophage polarization. TM5614 sodium alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. TM5614 sodium promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. TM5614 sodium can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.
    TM5614 sodium
Cat. No. Product Name / Synonyms Application Reactivity