Stemcell, 100-1644, CPI-203

Influence the expression of key oncogenes and anti-apoptotic proteins with CPI-203 (Filippakopoulos & Knapp. Nat Rev Drug Discov, 2014), a JQ1 analog and bromodomain-containing protein 4 inhibitor (BRD4; IC50 = 26 nM ). BRD4 is a protein in the bromodomain and extra-terminal (BET) family involved in transcriptional regulation. CPI-203 inhibits BRD4-mediated phosphorylation of serine 2 on the C-terminal domain of RNA polymerase II (Devaiah et al. Proc Natl Acad Sci USA, 2012), through which this epigenetic modifier modulates the expression of oncogenes and anti-apoptotic proteins.

CPI-203 has been used for:

DIFFERENTIATION

· Represses Myc expression, resulting in hematopoietic stem cell (HSC) maintenance in a mouse model (Knudsen et al. Genes Dev, 2015).

· Promote expansion of human umbilical cord blood HSCs and increase proportion of megakaryocyte differentiation (Hua et al. Blood, 2020).

CANCER RESEARCH

· Enhance the effect of immunotherapy in a mouse model of liver cancer by inhibiting programmed death receptor 1 expression (Niu et al. Cancer Sci, 2022).