BRD4-IN-41

BRD4-IN-41 is a BRD4 inhibitor with an IC₅₀ of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC₅₀ values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia^[1]. In Vitro:BRD4-IN-41 (Compound 3) potently inhibits the BRD4 bromodomain with an IC₅₀ of 34 nM in an Alpha Screen binding assay^[1].
BRD4-IN-41 (100 μM) binds to the BRD4-1 bromodomain, increasing the protein's melting temperature by 11.0 °C in a DSF assay^[1].
BRD4-IN-41 potently inhibits purified JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC₅₀ values ranging from 0.9 nM to 43 nM in a ³³P-ATP radiolabeled assay^[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) potently inhibits the growth of human multiple myeloma MM1.S cells with an IC₅₀ of 0.15 μM in a 72 h CellTiter Blue viability assay^[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) potently inhibits the growth of human JAK2^V617F mutant myeloproliferative neoplasm UKE-1 cells, MM1.S cells and HCC78 cells with IC₅₀ values of 0.08, 0.1 and 0.66 μM in a 72 h CellTiter Blue viability assay^[1].
BRD4-IN-41 (6 h) induces dose-dependent inhibition of JAK2 (via reduced phospho-STAT3) and BRD4 (via reduced c-MYC, increased p21Cip1) signaling, and triggers apoptosis (via cleaved PARP) in human multiple myeloma MM1.S cells after 6 h of treatment^[1].
BRD4-IN-41 (0.5 μM; 24 h) induces G1 phase arrest^[1].
BRD4-IN-41 (6 h) induces dose-dependent inhibition of JAK2 (via reduced phospho-STAT3) and BRD4 (via reduced c-MYC) signaling in human JAK2^V617F mutant myeloproliferative neoplasm UKE-1 cells after 6 h of treatment^[1].
BRD4-IN-41 (25 nM-500 nM; 14 days) potently inhibits erythroid colony formation in primary JAK2^V617F-positive MPN cells, with IC₅₀ values <50 nM^[1].
BRD4-IN-41 (96 h) inhibits growth across 931 human cancer cell lines with a mean IC₅₀ of 0.51 μM, showing highest potency against bone and blood cancer cell lines (mean IC₅₀ values 0.18 μM and 0.25 μM, respectively)^[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) inhibits the growth of human erythroleukemia HEL cells with an IC₅₀ of 0.37 μM in a 72 h CellTiter Blue viability assay^[1].
BRD4-IN-41 (1 nM-10 μM; 72 h) potently inhibits the growth of JAK2^V617F transformed BaF3 cells with an IC₅₀ of 0.04 μM in a 72 h CellTiter Blue viability assay^[1].