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-146471
    EGFR-IN-51
    		Inducer
    EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis.
    EGFR-IN-51
  • HY-170565
    CHD-1
    		Inhibitor
    CHD-1 is a a hypoxia-activated antitumor prodrug. CHD-1 impairs mitochondrial morphology and membrane potential in hypoxic tumor cells, further triggering excessive mitophagy and inducing apoptosis. CHD-1 inhibits the growth of hypoxic tumor cells in vitro and the growth of HeLa xenograft in vivo.
    CHD-1
  • HY-134985
    Thalidomide-NH-PEG1-NH2
    		Inducer
    Thalidomide-NH-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-PEG1-NH2
  • HY-178466
    Tubulin polymerization/P-gp-IN-1
    		Inducer
    Tubulin polymerization/P-gp-IN-1 is a Tubulin polymerization/P-gp dual inhibitor. Tubulin polymerization/P-gp-IN-1 inhibits tubulin polymerization and induces G2/M arrest and apoptosis. Tubulin polymerization/P-gp-IN-1 reverses MDR by inhibiting P-gp efflux function. Tubulin polymerization/P-gp-IN-1 has dual functions: direct antitumor activity and reversal of P-gp-mediated Cisplatin (HY-17394) resistance. Tubulin polymerization/P-gp-IN-1 stable binds to the tubulin CBS (ΔG = −12.4 kcal/mol) and the P-gp hydrophobic lumen (ΔG = −10.8 kcal/mol). Tubulin polymerization/P-gp-IN-1 can be used for the study of drug-resistant cervical cancer.
    Tubulin polymerization/P-gp-IN-1
  • HY-173493
    ALK-IN-31
    		Inducer
    ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor (IC50: 1135 nM). ALK-IN-31 exhibits excellent antiproliferative activity against lung cancer H2228 cells with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation in the G0/G1 phase by affecting mitochondrial function. ALK-IN-31 exerts its anti-tumor effect by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. ALK-IN-31 can be used in the study of non-small cell lung cancer (NSCLC).
    ALK-IN-31
  • HY-159589
    BTK-IN-37
    		Inducer
    BTK-IN-37 (compound 8d) is a BTK inhibitor that can induce apoptosis in cancer cells. BTK-IN-37 targets BTK with Ki and IC50 of 5.07 nM and 3.6 nM, respectively. BTK-IN-37 can also selectively induce enrichment of genes involved in necroptosis and pyroptosis.
    BTK-IN-37
  • HY-146163
    Topoisomerase II inhibitor 7
    		Inducer
    Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis.
    Topoisomerase II inhibitor 7
  • HY-120600
    Sibiriline
    		Inhibitor
    Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis..
    Sibiriline
  • HY-172620
    LIB3S0280
    		Inducer 99.89%
    LIB3S0280 is a potent TBK1 inhibitor with an IC50 value of 493.9 nM. LIB3S0280 exhibits better anticancer effects in pancreatic cancer cell lines with high TBK1 expression. LIB3S0280 inhibits TBK1 downstream signaling pathways, including PI3K/AKT and NF-κB. LIB3S0280 induces G2/M arrest, apoptosis and cellular senescence. LIB3S0280 can be used for pancreatic ductal adenocarcinoma (PDAC) research.
    LIB3S0280
  • HY-161855
    VEGFR-2-IN-50
    		Inducer
    VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases.
    VEGFR-2-IN-50
  • HY-170842
    TDK-HCPT
    		Inducer
    TDK-HCPT is a small-molecule conjugate that links glutathione-sensitive thiamine disulfide to the chemotherapy drug 10-Hydroxycamptothecin (HY-N0095) via a thioketal bond. TDK-HCPT can target tumor cells and prolong the retention of chemotherapy agents within tumor cells. TDK-HCPT can inhibit tumor growth, induce apoptosis of tumor cells, and has anti-tumor activity.
    TDK-HCPT
  • HY-N1381R
    Periplocin (Standard)
    		Inducer
    Periplocin (Standard) is the analytical standard of Periplocin. This product is intended for research and analytical applications. Periplocin is a cardiotonic steroid isolated from root-bark Periploca sepium Bunge. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase.
    Periplocin (Standard)
  • HY-138008
    WX-132-18B
    		Inducer
    WX-132-18B is a tubulin inhibitor with an IC50 of 0.45-0.99 nM. WX-132-18B selectively binds to the colchicine-binding site on tubulin, reduces microtubule content via depolymerization, and inhibits tubulin polymerization. WX-132-18B induces tumor cell cycle arrest, apoptosis and changes in nuclear membrane permeability, and decreases mitochondrial membrane potential. WX-132-18B exhibits antiproliferative activity against endothelial cells and human tumor cells, and inhibits the proliferation and growth of xenograft tumors in mice. WX-132-18B can be used in research related to sarcoma, non-small cell lung cancer, gastric cancer and breast cancer.
    WX-132-18B
  • HY-174855
    PI3K/mTOR-IN-17
    		Inducer
    PI3K/mTOR-IN-17 is a dual PI3K and mTOR inhibitor with IC50 values of 1.21 μM (PI3K), and 0.21 μM (mTOR). PI3K/mTOR-IN-17 induces cells caspase-mediated apoptosis by arresting their growth in the G1-phase. PI3K/mTOR-IN-17 upregulates the levels of caspases-3, 7, 8, and 9, p53 expression and Bax/Bcl-2 ratio. PI3K/mTOR-IN-17 suppresses the PI3K/mTOR signaling pathway. PI3K/mTOR-IN-17 can be used for research of cancer, such as non-small cell lung cancer (NSCLC).
    PI3K/mTOR-IN-17
  • HY-103086
    INU-152
    INU-152 is a potent and selective B-Raf inhibitor. INU-152 reduces tumor cell proliferation, enhances autophagy, and induces apoptosis by inhibiting B-Raf activity. INU-152 exhibits significant cytotoxicity against cancer cells transformed with v-Ha-ras (Ras-NIH 3T3). INU-152 can be utilized in cancer research.
    INU-152
  • HY-161153
    Microtubule inhibitor 9
    		Inducer
    Microtubule inhibitor 9 (Compound O-7) is a 2-Aryl-1H-benzo [d] imidazole derivative with in vitro anticancer activity. Microtubule inhibitor 9 can induce cell cycle arrest at the G2/M phase and early apoptosis. Microtubule inhibitor 9 inhibits cancer cell migration by inhibiting wound healing and colony formation.
    Microtubule inhibitor 9
  • HY-163506
    Ebselen derivative 1
    		Inhibitor
    Ebselen derivative 1 (Compound 19) is a glutathione peroxidase (GPx) mimic with oral activity. Ebselen derivative 1 demonstrates significant protective effects against cisplatin (HY-17394)-induced hair cell (HC) damage both in vitro and in vivo, effectively reducing oxidative stress, apoptosis, and ferroptosis in hair cells. Ebselen derivative 1 can be utilized in the research of cisplatin (HY-17394)-induced hearing loss .
    Ebselen derivative 1
  • HY-B1448AS
    (Rac)-Benidipine-d7
    (Rac)-Benidipine-d7 is the deuterium labeled Benidipine. Benidipine is a potent and orally active calcium channel antagonist. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats.
    (Rac)-Benidipine-d<sub>7</sub>
  • HY-179032
    VEGFR-2-IN-77
    		Inducer
    VEGFR-2-IN-77 (Compound 10) is a VEGFR-2 inhibitor with an IC50 value of 139 nM. VEGFR-2-IN-77 inhibits the PI3K/AKT/mTOR pathway. VEGFR-2-IN-77 exhibits selective cytotoxicity, being particularly sensitive to leukemia and prostate cancer cells. VEGFR-2-IN-77 causes cell cycle arrest and apoptosis, inhibiting cell migration and invasion. VEGFR-2-IN-77 can be used for the study of leukemia and prostate cancer.
    VEGFR-2-IN-77
  • HY-183591
    CAIX/XII-IN-18
    		Inducer
    CAIX/XII-IN-18 is a selective human carbonic anhydrase IX/XII (CA IX/XII) inhibitor with Ki values of 28.1 nM (hCA IX) and 11.6 nM (hCA XII). CAIX/XII-IN-18 induces apoptosis in breast cancer cells. CAIX/XII-IN-18 can be used for the research of breast cancer, pancreatic cancer.
    CAIX/XII-IN-18
Cat. No. Product Name / Synonyms Application Reactivity