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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 CAS No. Information
GY06767

Flavokawain B

1775-97-9

Flavokawain B is a natural chalcone that can induce apoptosis in androgen receptor-negative, hormone-refractory prostate cancer cell lines (IC50=3-50 uM), via up-regulation of death-receptor 5 and Bim expression; induces apoptosis in human myeloid leukemic cells by modifying NF-κB, possesses potential anti-inflammation and anti-cancer activities; also exhibits significant inhibition of the neurogenic nociceptive induced by intraplantar injections of glutamate and capsaicin in mice.

GY02181

Ecteinascidin 770

114899-80-8

A tetrahydroisoquinoline alkaloid with potent anticaner activities; shows cytotoxicity against human cell lines HCT116, QG56, and DU145 with IC50 of 0.60, 2.4, and 0.81 nM, respectively; sensitizes H23 the cells by activating the p53 protein, down-regulates MCL1 and up-regulates BAX proteins, with no effect on Bcl-2; enhances anoikis response of human lung cancer H23 and H460 cells.

GY02097

JPH203

1037592-40-7

JPH203 (KYT-0353) is a potent, selective L-type amino acid transporter 1 (LAT1, SLC7A5) inhibitor with IC50 of 60 nM (leucine uptake inhibition), but not LAT2; inhibits cell growth in HT-29 cells with IC50 of 4.1 uM, also inhibits (14)C-leucine uptake in mouse renal proximal tubule cells expressing LAT1 and inhibits cell growth with IC50 of 0.14 and 16.4 uM, respectively; significant inhibits HT-29 tumor growth in vivo.

GY03765

Silvestrol aglycone

960365-65-5

Silvestrol is a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in cancer cells through the mitochondrial/apoptosome pathway; effectively targets the cyclin/CDK/Rb pathway, and additionally induces cytotoxicity via intrinsic apoptosis, exhibits low nanomolar potency both in MCL cell lines and primary MCL tumor cells; demonstrates B-cell selective activity in chronic lymphocytic leukemia and acute lymphoblastic leukemia in vitro and in vivo.

GY03493

Silvestrol

697235-38-4

Silvestrol is a potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in cancer cells through the mitochondrial/apoptosome pathway; effectively targets the cyclin/CDK/Rb pathway, and additionally induces cytotoxicity via intrinsic apoptosis, exhibits low nanomolar potency both in MCL cell lines and primary MCL tumor cells; demonstrates B-cell selective activity in chronic lymphocytic leukemia and acute lymphoblastic leukemia in vitro and in vivo.

GY03405

Imexon

59643-91-3

Imexon is a 2-cyanoaziridine derivative with antitumor activity in some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma; induces mitochondrial oxidation and induces apoptosis via a pathway involving cleaved caspase-3, caspase-9, and/or caspase-8; an apoptosis inducer agent.

GY03322

Iberin

505-44-2

Iberin is an isothiocyanate compound from horseradish that exhibits anticancer activity, a quorum-sensing inhibitor (QSI) of the bacterial pathogen Pseudomonas aeruginosa, and significantly induces Nrf2 nuclear translocation in NIH3T3 fibroblasts; induces cell cycle arrest and apoptosis in human neuroblastoma cells associated with inhibition of expression of Cdk2, Cdk4, and Cdk6 proteins.

GY03309

Hinokitiol

499-44-5

Hinokitiol (4-Isopropyltropolone;β-Thujaplicin) is a tropolone-related natural compound that can induces apoptosis and cell cycle arrest, exhibits anti-inflammatory and anti-tumor activities; inhibits the proliferation of Chlamydia trachomatis with MIC of 32 ug/mL; also can harness such gradients to restore iron transport into, within, and/or out of cells.

GY03251

Kinetin riboside

4338-47-0

Kinetin riboside is a cytokinin analog that displays potent antiproliferative activity against various human cancer cell lines; inhibits MiPaCa-2 cell proliferation with IC50 of 0.27 uM; induceds marked suppression of CCND2 transcription and rapidly suppresses cyclin D1 and D2 protein expression in primary myeloma cells and tumor lines, causing cell cycle arrest, tumor cell-selective apoptosis, and inhibition of myeloma growth in xenografted mice; also can activate PINK1 in cells independent of mitochondrial depolarization.

GY01624

Apoptosis Activator 2

79183-19-0

Apoptosis Activator 2 is an apoptosis activator that strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation; leads to the destruction of cells (Apaf-1 dependent) with IC50 of 4 uM; exert cytostatic and cytotoxic effects on a variety of cancer cell lines while having little or no activity against the normal cell lines tested.

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