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-176908
    SIOC-XJC-SF02
    		Inducer
    SIOC-XJC-SF02 is a Fenofibrate (HY-17356) derivative. SIOC-XJC-SF02 induces Apoptosis. SIOC-XJC-SF02 exhibits significant anti-cancer activity against hepatocellular carcinoma.
    SIOC-XJC-SF02
  • HY-177768
    HDAC-IN-96
    		Inducer
    HDAC-IN-96 (Compound 3f) is a selective HDAC1/2 inhibitor with IC50 values of 457.1 and 433.7 nM. HDAC-IN-96 has strong inhibitory activity against multiple hematological tumor cells (RS4;11, K562, RPMI-8226, U266), with IC50 values ranging from 2.11 to 5.35 μM. HDAC-IN-96 can induce cancer cells apoptosis and S phase arrest. HDAC-IN-96 can be used for the research of cancer, such as acute lymphoblastic leukemia.
    HDAC-IN-96
  • HY-144130
    hGGPPS-IN-3
    hGGPPS-IN-3 (Compound 13h) is a potent inhibitor of the human geranylgeranyl pyrophosphate synthase (hGGPPS). hGGPPS-IN-3 is an analogue of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs). hGGPPS-IN-3 induces target-selective apoptosis of multiple myeloma (MM) cells and exhibits antimyeloma activity in vivo.
    hGGPPS-IN-3
  • HY-168605
    DH-18
    		Inducer
    DH-18 is a matrix metalloproteinase-2 (MMP-2) inhibitor with the IC50 values of 139.45 nM, 518.11 nM and 833.34 nM for MMP-2, MMP-9 and MMP-8, respectively. DH-18 induces cell apoptosis and arrests cell cycle in the G0/G1 phase. DH-18 inhibits cell growth and can be used for study of chronic myeloid leukemia.
    DH-18
  • HY-B0144AS3
    Pitavastatin-d4-1 sodium
    		99.22%
    Pitavastatin-d4-1 (NK-104-d4-1) sodium is the deuterium labeled Pitavastatin sodium (HY-B0144B). Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
    Pitavastatin-d<sub>4</sub>-1 sodium
  • HY-B0028R
    Fludarabine phosphate (Standard)
    		Inducer
    Fludarabine (phosphate) (Standard) is the analytical standard of Fludarabine (phosphate). This product is intended for research and analytical applications. Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
    Fludarabine phosphate (Standard)
  • HY-163406
    PDE1-IN-6
    		Inducer
    PDE1-IN-6 (compound 6c) is a selectivity PDE1 inhibitor with the IC50 of 7.5 nM. PDE1-IN-6 significantly inhibits the proliferation and induced cell apoptosis in Acute myelogenous leukemia cells.
    PDE1-IN-6
  • HY-157324
    EGFR-IN-94
    		Inducer
    EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC50 of 0.086?μM, and also has IC50 of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .
    EGFR-IN-94
  • HY-173499
    HLDA-212
    		Inducer
    HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies).
    HLDA-212
  • HY-159111
    KS124
    		Inducer
    KS124 (compound 3) is a potent ALDH inhibitor. KS124 shows inhibition for ALDH1A1, ALDH1A3, ALDH3A1. KS124 shows antiproliferative activity. KS124 induces apoptosis and ROS production.
    KS124
  • HY-161946
    GBM CSCs-IN-1
    		Inducer
    GBM CSCs-IN-1 (Compound (−)-20), a derivative of rocaglate, is a potent inhibitor of glioblastoma stem cells (GBM CSCs) with an EC50 of 45 nM, functioning by targeting the RNA helicase DDX3. Furthermore, GBM CSCs-IN-1 is also capable of inducing apoptosis.
    GBM CSCs-IN-1
  • HY-14608AR
    L-Glutamic acid monosodium salt (Standard)
    		Inducer
    L-Glutamic acid (monosodium salt) (Standard) is the analytical standard of L-Glutamic acid (monosodium salt). This product is intended for research and analytical applications. L-Glutamic acid monosodium salt is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid monosodium salt has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid monosodium salt can be used in the study of neurological diseases.
    L-Glutamic acid monosodium salt (Standard)
  • HY-128393S2
    Trilinolein-d5
    Trilinolein-d5 is the deuterium labeled Trilinolein (HY-128393). Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.
    Trilinolein-d<sub>5</sub>
  • HY-143328
    PROTAC BRD4 Degrader-17
    		Inducer
    PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
    PROTAC BRD4 Degrader-17
  • HY-175236
    SF-9-2
    		Inducer
    SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research.
    SF-9-2
  • HY-W040329S
    2'-Deoxyadenosine-13C10,15N5
    		Inducer
    2'-Deoxyadenosine-13C10,15N5 is 13C and 15N-labeled 2'-Deoxyadenosine (HY-W040329). 2′-Deoxyadenosine is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine inhibits the growth of various cells. 2'-Deoxyadenosine has an anticancer effect on colon cancer.
    2'-Deoxyadenosine-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub>
  • HY-107796
    Metamizole magnesium
    		Inducer
    Metamizole magnesium is an orally active cyclooxygenase (COX) inhibitor. Metamizole magnesium can inhibit cell proliferation and promote cell apoptosis. Metamizole magnesium has anti-inflammatory and antioxidant activities. Metamizole magnesium is an antipyretic, analgesic and spasmolytic agent.
    Metamizole magnesium
  • HY-151980
    Mps1-IN-5
    		Inducer
    Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage.
    Mps1-IN-5
  • HY-N2447R
    Amarogentin (Standard)
    		Inducer
    Amarogentin (Standard) is the analytical standard of Amarogentin. This product is intended for research and analytical applications. Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
    Amarogentin (Standard)
  • HY-178176
    PROTAC CB1R Degrader-1
    		Inducer
    PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)).
    PROTAC CB1R Degrader-1
Cat. No. Product Name / Synonyms Application Reactivity