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-126251
    CDK9-IN-7
    		Inducer 98.05%
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
    CDK9-IN-7
  • HY-18756A
    NSC-87877 disodium
    		Inducer 98.0%
    NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
    NSC-87877 disodium
  • HY-173119
    SKLB-D18
    		Inducer 98.06%
    SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC50 of 38.69 nM and a Kd of 126.9 nM against human ERK1, an IC50 of 40.12 nM and a Kd of 209.8 nM against ERK2, and an IC50 of 59.72 nM and a Kd of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer.
    SKLB-D18
  • HY-13636S
    Fulvestrant-d3
    		Inducer
    Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
    Fulvestrant-d<sub>3</sub>
  • HY-119378
    AK 295
    		Inhibitor 99.0%
    AK 295 (CX 295) is a selective calpain inhibitor. AK 295 can inhibit apoptosis through a calpain-dependent pathway. AK 295 shows potent neuroprotective effect. AK 295 can inhibit the activity of the cysteine protease calpain and reduce myocardial injury. AK 295 can be used for the researches of infection, inflammation, cardiovascular and neurological disease, such as stroke and viral myocarditis.
    AK 295
  • HY-10220
    SF1126
    		Inducer
    SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 proagent, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
    SF1126
  • HY-128360
    dMCL1-2
    		Inducer 99.29%
    dMCL1-2 is a potent, selective MCL1 PROTAC degrader based on a Cereblon ligand, with a KD value of 30 nM for binding to MCL1. dMCL1-2 induces ubiquitination and degradation of MCL1. dMCL1-2 degrades MCL1, cleaves Caspase-3, and induces Apoptosis. dMCL1-2 can be used in research related to multiple myeloma.
    dMCL1-2
  • HY-108701
    Nampt-IN-3
    		Activator 98.97%
    Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
    Nampt-IN-3
  • HY-109146
    Imifoplatin
    		Activator
    Imifoplatin (PT-112) is a platinum-based active molecule and a member of the phosphaplatins family. Imifoplatin can induce Apoptosis and exhibits antitumor activity.
    Imifoplatin
  • HY-W014423S2
    L-Histidine-13C6 hydrochloride hydrate
    		Inducer 98.00%
    L-Histidine-13C6 (hydrochloride hydrate) is the 13C-labeled L-Histidine hydrochloride hydrate (HY-W014423). L-Histidine hydrochloride hydrate is an endogenous metabolite. L-Histidine hydrochloride hydrate scavenges hydroxyl radicals and singlet oxygen, regulate the absorption of zinc, copper and iron, exhibits anti-inflammatory and antioxidant activities. L-Histidine hydrochloride hydrate is blood brain barrier penetrable.
    L-Histidine-<sup>13</sup>C<sub>6</sub> hydrochloride hydrate
  • HY-177578
    NN3201
    		Inducer 99.15%
    NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research[1][2].
    NN3201
  • HY-130952
    Thalidomide-O-C8-COOH
    		Inducer
    Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-O-C8-COOH
  • HY-B0228S4
    Adenosine-1′-13C
    Adenosine-1′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
    Adenosine-1′-<sup>13</sup>C
  • HY-109109
    Alteminostat
    		Inducer 98.66%
    Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research.
    Alteminostat
  • HY-19747
    HPOB
    		Inducer 99.54%
    HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
    HPOB
  • HY-110339
    RKI-1447 dihydrochloride
    		Inducer 99.94%
    RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
    RKI-1447 dihydrochloride
  • HY-132334S
    9-cis-Retinoic acid-d5
    		Inducer 99.24%
    9-cis-Retinoic acid-d5 is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.
    9-cis-Retinoic acid-d<sub>5</sub>
  • HY-122710A
    Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride
    		Inducer
    Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
    Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride
  • HY-126249
    AAPK-25
    		Activator 98.09%
    AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.
    AAPK-25
  • HY-145260
    BRD4/CK2-IN-1
    		Inducer 98.21%
    BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
    BRD4/CK2-IN-1
Cat. No. Product Name / Synonyms Application Reactivity