Apoptosis
Apoptosis, also known as programmed cell death, is rigorously controlled process of cell death that leads to phagocytosis of unwanted cell. It is triggered after sufficient cellular damage and activated through extrinsic or intrinsic pathways. The intrinsic pathway is mainly occurs via release of cytochrome c from the mitochondria and regulates mitochondrial outer membrane permeabilization by Bcl-2 family proteins. The extrinsic pathway is induced by ligand binding to death receptor, such as Fas, TNFαR, DR3, DR4, and DR5. Caspases then cleave target proteins and nuclear lamins to promote DNA degradation, resulting apoptotic cells undergo phagocytosis. In addition, p53 has the ability to activate intrinsic and extrinsic pathways of apoptosis by inducing transcription of several proteins like Puma, Bid, Bax, TRAIL-R2, and CD95.
Some Inhibitors of apoptosis proteins (IAPs), such as XIAP/BIRC4 and Bruce/BIRC6, can block casapse activity through direct binding, while other IAPs, such as cIAP1/BIRC2, cIAP2/BIRC3, act as ubiquitin ligases that target caspases for ubiquitin-mediated degradation. Apoptosis is essential for growth, development and aging in multicellular organisms. Any alterations or abnormalities occurring in apoptotic processes contribute to development of human diseases, including cancer.
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BA7727 FOXO1-IN-3Summary: FOXO1-IN-3 is a highly selective and orally active inhibitor. - BA7858 NHI-2Summary: NHI-2 is a potent inhibitor.
- BA7918 CirsiliolSummary: Cirsiliol is a potent and selective inhibitor of 5-lipoxygenase.
- BA7927 5-LOX-IN-2Summary: 5-LOX-IN-2 is a 5-lipoxygenase inhibitor.
- BA7948 YamogeninSummary: Yamogenin (Neodiosgenin) is the diastereoisomer of Diosgenin.
- BA7994 S3QEL-2Summary: S3QEL-2 is an inhibitor of superoxide production by mitochondrial complex III. S3QEL-2 selectively inhibits superoxide production at the IIIQo site (=1.7 μM).
- BA7997 DX3-213BSummary: DX3-213B is a potent orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (=3.6 nM).
- BA8103 HKB99Summary: HKB99 is a variant inhibitor of phosphoglycerate mutase 1.
- BA8137 SHP389Summary: SHP389 is a metastable inhibitor.
- BA8210 TanimilastSummary: Tanimilast (CHF-6001) is a novel potent and selective inhibitor (=0.026±0.006nM) with potent anti-inflammatory activity suitable for topical pulmonary administration.