dTRIM24 is a Selective PROTAC Degrader of TRIM24

TRIM24 is a multidomain protein characterized as a co-regulator of transcription. Especially, dTRIM24 acts as a chemical probe of an emerging cancer dependency. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. TRIM24 has been posited as a dependency in numerous cancers,...

DT2216 is a Selective PROTAC Degrader of BCL-XL

BCL-XL is a member of the Bcl-2 protein family and a transmembrane molecule in mitochondria. Specifically, it acts as an anti-apoptotic protein by blocking the release of mitochondrial contents such as cytochrome c. Besides, BCL-XL is a well-validated cancer target and eventually leads to caspase activation and eventually programmed...

Tetrac is a Thyrointegrin Receptor Antagonist

In the angiogenesis process, integrins are members of a family of cell surface transmembrane receptors. They play a critical role particularly in blood vessel formation and the local release of vascular growth factors. Thyroid hormones such as T4 and T3 promote angiogenesis and tumor cell proliferation via integrin αvβ3...

Cilengitide is a Selective Integrin Inhibitor for αvβ3 and αvβ5 Receptor

Integrins are heterodimeric cell surface adhesion receptors that consist of two noncovalently associated alpha and beta subunits. In particular, Integrins are heterodimeric transmembrane proteins composed of one α and one β subunit. Especially, Integrins are crucially important because they are the main receptor proteins that cells use to bind...

E7820 is an α2 Integrin Inhibitor with Anti-Tumor Activity

Vascular endothelial growth factor (VEGF) is a prime contributor to tumor angiogenesis. Most tumor cells produce high levels of VEGF and VEGF receptors associated with tumor endothelial cells. E7820 is an aromatic sulfonamide derivative and an Angiogenesis inhibitor. E7820 inhibits in vitro proliferation and tube formation of human umbilical...

Cyclo(-RGDfK) is a Selective Inhibitor of the αvβ3 Integrin

Increasing evidence indicated that targeting tumor angiogenesis for specific drug transfer into tumor masses and metastasis is a promising approach. On the one hand, integrin poorly expressed on quiescent vessels and selectively overexpressed on activated endothelial cells of growing vessels, on the other hand, integrin αvβ3 frequently overexpresses on...

KB02-SLF is a PROTAC-Based Nuclear FKBP12 Degrader (Molecular Glue)

Conventional small-molecule probes play their roles by perturbing the functions of proteins, including blocking enzyme catalysis or antagonizing receptor signaling. However, a compound only binds to only one of these domains that may can not fully inactivate the protein. There exist a novel strategy, chemical probes, which direct proteins...