Stemcell, 100-1657, SGC-CBP30

Influence gene expression and cellular responses including cell proliferation and inflammation, with SGC-CBP30, a potent inhibitor of CREB-binding protein (CBP; IC50 = 21 - 69 nM) and p300 (IC50 = 38 nM) bromodomains (Gallenkamp et al. ChemMedChem, 2014). CBP and p300 are histone acetyltransferases that can act as transcriptional co-activators to regulate gene expression. The bromodomain of these proteins facilitate acetylation of lysine residues, and mutations in CBP and p300 have been associated with cancer and inflammatory responses (Raisner et al. Cell Rep, 2018; Zhu et al. Cancers, 2023). Through the inhibition of CBP and p300, SGC-CBP30 impacts gene expression and cellular processes.

SGC-CBP30 has been used for:

IMMUNOLOGY

· Reduce inflammatory cell infiltration in the lungs, liver, colon, and kidney of a septic mouse model (Bi et al. Front Immunol, 2021).

CANCER RESEARCH

· Inhibit cell proliferation and induce apoptosis by downregulating uridine phosphorylase 1 expression in human lung adenocarcinoma cells (Wang et al. Aging Dis, 2022).

· Diminish the viability of human pancreatic cancer cells when used in combination with the bromodomain and extra-terminal domain (BET) inhibitors (Principe et al. Proc Natl Acad Sci U S A, 2022).