Panobinostat is a Potent and Orally Active Non-selective HDAC Inhibitor
HDACs (Histone deacetylases) are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone, allowing the histones to wrap the DNA more tightly. This is important because acetylation and de-acetylation can regulate DNA expression. Acetylation is controlled by two antagonistic enzyme families:...
AUTAC4 is a Mitochondria-targeting Autophagy-targeting Chimera (AUTAC).
AUTAC4 is a Mitochondria-targeting Autophagy-targeting Chimera (AUTAC). Besides, AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy. Autophagy-targeting chimera (AUTAC) degrades target proteins via a lysosomal pathway rather than the common proteasome pathway. Besides, One end of AUTAC is a target protein-ligand, the other end is a...
Henatinib is an Orally Active Multikinase Inhibitor with Broad Antitumor Activities
Tumor growth and development involve many complex pathways, such as malignant cell proliferation and angiogenesis. Kinases are the enzymes that control signal transduction in these pathways, including VEGF, PDGFR, c-kit, and so on. They are present in stromal vascular or cell-matrix, and when they are dysfunctional (such as overactivation), they...
PSB-SB-487 is a Potent GPR55 Antagonist
GPR55 (G protein-coupled receptor 55) is a G protein-coupled receptor that in humans is encoded by the GPR55 gene. GPR55, along with GPR119 and GPR18, are novel cannabinoid receptors. Like the CB receptors, GPR55 belongs to the rhodopsin-like seven transmembranes G protein-coupled receptor (GPCR) superfamily. GPR55 and CB2 receptors...
Tiragolumab is An Immune Checkpoint Inhibitor Binding to T-cell Immunoglobulin and TIGIT
Tiragolumab is a potent TIGIT inhibitor. Tiragolumab alone or in combination with the PD-L1 inhibitor Atezolizumab has effects on solid cancers. Additionally, at two recent medical meetings, the agent achieves statistically significant results in multiple solid malignancies. Especially in small cell lung cancer (NSCLC). Lung cancer is the most...
Pulrodemstat is a Potent, Selective, Reversible and Orally Active Inhibitor of LSD1
Lysine-specific histone demethylase 1A (LSD1) also known as lysine (K)-specific demethylase 1A (KDM1A) is a protein in humans that is encoded by the KDM1A gene. LSD1 is a member of a broad family of monoamine oxidases that requires FAD as a cofactor to catalyze demethylase activity. In addition, LSD1...
LDN-211904 is a Potent and Selective EphB3 Inhibitor for Colorectal Cancer Research
LDN-211904 is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. Besides, LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. What’s more, LDN-211904 oxalate with cetuximab could effectively inhibit STAT3-activated CSC stemness and cetuximab resistance in colorectal cancer. LDN-211904 oxalate is a potent EphB3 inhibitor. Besides,...