tumoral cell

BI-1347 is a potent, selective inhibitor of CDK8 cyclinC (IC50: 1 nM). It shows tumor growth inhibition in an in vivo xenograft model.

FB49 is a selective Bcl-2-associated athanogene 3 (BAG3) inhibitor with a Ki of 45 μM. It inhibits the proliferation of human tumoral cells without affecting the viability of human peripheral mononuclear cells. Additionally, FB49 arrests the cell cycle at the G1 phase and induces apoptosis and autophagy in treated medulloblastoma HD-MB03 cells [1].

SIAIS039 is an orally active PROTAC specifically targeting c-ros oncogene 1 (ROS1), demonstrating DC50 values of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, Ba F3 cells expressing CD74-ROS1 fusion, and Ba F3 cells expressing SDC4-ROS1 fusion, respectively. This compound inhibits proliferation, induces cell cycle arrest, and triggers apoptosis in ROS1-positive cells, while also inhibiting colony formation. In vivo, SIAIS039 exhibits potent anti-tumoral activity against ROS1-driven tumor growth. The composition of SIAIS039 includes the ALK inhibitor Brigatinib, linker EM-12, and VHL E3 ubiquitin ligase ligand.

Keap1-Nrf2-IN-21 (compound 4d) acts as an inhibitor of glucose metabolism with anti-tumoral properties. It targets the glycolytic pathway by affecting the Keap1-Nrf2 signaling pathway, which in turn suppresses glycolytic activity in cancer cells and inhibits tumor growth. Additionally, Keap1-Nrf2-IN-21 exhibits cytotoxic effects on the HEC1A cell line with an IC50 value of 2.60 μM.

Cyclo(-RGDfK) is a selective αvβ3 integrin inhibitor(IC50 : 0.94 nM).

CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).

Cyclo(-RGDfK) is a potent and selective inhibitor of integrin αvβ3 with IC50 of 0.94 nM. Cyclo specifically targets tumor microvasculature and cancer cells by binding to αvβ3 integrin on the cell surface.