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-N1988R
    Cucurbitacin IIa (Standard)
    		Inducer
    Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
    Cucurbitacin IIa (Standard)
  • HY-N0103R
    Sophocarpine (Standard)
    		Inducer
    Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
    Sophocarpine (Standard)
  • HY-15449R
    Kaempferide (Standard)
    		Inducer
    Kaempferide (Standard) is the analytical standard of Kaempferide. This product is intended for research and analytical applications.
    Kaempferide (Standard)
  • HY-152225
    MC2625
    		Inducer
    MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction.
    MC2625
  • HY-10446S1
    Pralatrexate-13C5,15N
    		Inducer
    Pralatrexate-13C5,15N is the 13C- and 15N-labeled Pralatrexate (HY-10446). Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Pralatrexate-<sup>13</sup>C<sub>5</sub>,<sup>15</sup>N
  • HY-16938S2
    5'-Methylthioadenosine-13C5
    		Inducer
    5'-Methylthioadenosine-13C5 (5'-(Methylthio)-5'-deoxyadenosine-13C5) is the 13C--labeled 5'-Methylthioadenosine (HY-16938). 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
    5'-Methylthioadenosine-<sup>13</sup>C<sub>5</sub>
  • HY-13613S2
    Dutasteride-13C,15N,d
    		Inducer
    Dutasteride-13C,15N,d is 15N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
    Dutasteride-<sup>13</sup>C,<sup>15</sup>N,d
  • HY-B0444A
    Maprotiline
    		Activator
    Maprotiline is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1.
    Maprotiline
  • HY-115944
    BTK-IN-9
    		Inducer
    BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells.
    BTK-IN-9
  • HY-175010
    STAT3-IN-44
    		Inducer
    STAT3-IN-44 is a potent STAT3 inhibitor with IC50s of 1.84 (C6 cells) and 4.81 μM (A549 cells). STAT3-IN-44 inhibits STAT3 phosphorylation, downregulates Bcl-2, and upregulates Caspase-3 to promote late-stage apoptosis. STAT3-IN-44 significantly suppresses tumor cell proliferation and migration. STAT3-IN-44 can be used for the study of cancers such as glioma and lung cancer.
    STAT3-IN-44
  • HY-147865
    Apoptosis inducer 8
    		Inducer
    Apoptosis inducer 8 (Compound 7c) is a galectin-1 (gal-1) mediated apoptosis-inducing agent against global major leading lung cancer burden. Apoptosis inducer 8 significantly reduced the gal-1 protein level. Apoptosis inducer 8 is also a PET imaging agent.
    Apoptosis inducer 8
  • HY-N2575R
    Hypocrellin A (Standard)
    		Inducer
    Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].
    Hypocrellin A (Standard)
  • HY-130237R
    Cinnamtannin B-1 (Standard)
    		Inducer
    Cinnamtannin B-1 (Standard) is the analytical standard of Cinnamtannin B-1. This product is intended for research and analytical applications. Cinnamtannin B-1 is a anthocyanidin. Cinnamtannin B-1 inhibits the osteoclast formation by inhibiting NF-kB signaling pathway and ROS generation. Cinnamtannin B-1 exhibits antioxidant, anti-inflammatory, antitumor and anti-platelet aggregation activities. Cinnamtannin B-1 is orally active.
    Cinnamtannin B-1 (Standard)
  • HY-174128
    Multi-target kinase-IN-5
    		Inducer
    Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor (IC50 values are 3.04 nM and 1.57 nM, respectively). Multi-target kinase-IN-5 significantly inhibits cancer cell proliferation, migration and invasion, and induces cell apoptosis and cell cycle arrest. Multi-target kinase-IN-5 inhibits the phosphorylation of ERK1/2 and downregulates the activity of its downstream substrate RSK to exert anti-tumor effects. Multi-target kinase-IN-5 can be used in cancer research.
    Multi-target kinase-IN-5
  • HY-144125
    Antitumor agent-41
    		Activator
    Antitumor agent-41 (compound N-12), a potent antitumor agent, enhibits excellent antimigration and anti-invasion activity. Antitumor agent-41 (compound N-12) induces tumor inhibition via tumor necrosis and inflammatory response.
    Antitumor agent-41
  • HY-P991639
    BIW-8962
    		Inducer
    BIW-8962 is a humanized anti-ganglioside GM2 antibody. BIW-8962 exhibits ADCC/CDC activity against multiple myeloma cells. BIW-8962 demonstrates potent anti-tumor activity in mouse xenograft models. BIW-8962 is indicated for research in myeloma and other cancers.
    BIW-8962
  • HY-P11782
    GTGKT
    		Activator
    GTGKT is a CAGE inhibitor. GTGKT binds to CAGE and blocks the binding of CAGE to GSK3β. GTGKT alters the localization of CAGE and inhibits the binding of CAGE to the promoter sequence of Cyclin D1. GTGKT enhances the Apoptotic effect of anticancer agents. GTGKT reduces the expression of Cyclin D1. GTGKT decreases the tumorigenic potential of melanoma and hepatocellular carcinoma cells.
    GTGKT
  • HY-P10326
    Z-ATAD-FMK
    		Inhibitor
    Z-ATAD-FMK is an inhibitor of caspase-12. Z-ATAD-FMK is an inhibitor of caspase-12. Z-ATAD-FMK prevents endoplasmic reticulum stress-mediated apoptosis by inhibiting the activity of caspase-12 and reducing the activity of caspase-9.
    Z-ATAD-FMK
  • HY-P992451
    RLYB331
    		Inhibitor
    RLYB331 (KY1066) is a is a monoclonal antibody targeting Matriptase-2 (TMPRSS6). RLYB331 binds to the serine protease active site of matriptase-2, blocking protease activity to increase hepcidin expression. RLYB331 reduces iron overload, inhibits α-aggregates, reduces ROS, inhibits apoptosis, and enhances erythroid differentiation. RLYB331 ameliorates ineffective erythropoiesis in β-thalassemic mouse models. RLYB331 can be used for the research of β-thalassemia.
    RLYB331
  • HY-146228
    HSP90-IN-13
    		Inducer
    HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway.
    HSP90-IN-13
Cat. No. Product Name / Synonyms Application Reactivity