874594-37-3
Chemical Structure
BET-IN-18
- CAS No.: 874594-37-3
- Formula:C18H17N3O4
- Molecular Weight:339.35
IUPAC Name: 1-ethyl-5-(p-tolyl)-5,9-dihydrofuro[3',4':5,6]pyrido[2,3-d]pyrimidine-2,4,6(1H,3H,8H)-trione
InChIKey: MUOCQMZJLRQTRD-UHFFFAOYSA-N
SMILES: O=C1OCC=2NC3=C(C(=O)NC(=O)N3CC)C(C4=CC=C(C=C4)C)C12
Biological Activity: BET-IN-18 (Compound 3) is a pan-BET bromodomain small-molecule inhibitor, with Ki values of 0.69 μM and 0.37 μM, and Kd values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 (HY-13030) to Brd4 (1) and BrdT (1), with IC50 values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) (IC50 = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma[1].
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BET-IN-18 | BET-IN-18 (Compound 3) is a pan-BET bromodomain small-molecule inhibitor, with Ki values of 0.69 μM and 0.37 μM, and Kd values of 1.6 μM and 8.4 μM against BrdT (1) and Brd4 (1) bromodomains, respectively. BET-IN-18 potently and competitively inhibits the binding of the known BET inhibitor (+)-JQ1 (HY-13030) to Brd4 (1) and BrdT (1), with IC50 values of 1.0 μM and 2.3 μM, respectively. BET-IN-18 also competitively inhibits the binding of acetylated histone substrates to Brd4 (1) (IC50 = 0.90 μM). BET-IN-18 can be used in the research of multiple myeloma. | |||||||||||||||||||||
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Keywords
