BAY 299
BAY 299 Basic information
- Product Name:
- BAY 299
- Synonyms:
-
- BAY-299; BAY 299; BAY299
- 6-(3-hydroxypropyl)-2-(1,3,6-trimethyl-2-oxobenzimidazol-5-yl)benzo[de]isoquinoline-1,3-dione
- BAY 299
- CPD1617
- 6-(3-Hydroxypropyl)-2-(1,3,6-trimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione
- 1H-Benz[de]isoquinoline-1,3(2H)-dione, 2-(2,3-dihydro-1,3,6-trimethyl-2-oxo-1H-benzimidazol-5-yl)-6-(3-hydroxypropyl)-
- 6-(3-Hydroxy-propyl)-2-(1,3,6-trimethyl-2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl)-benzo[de]isoquinoline-1,3-dione
- 6-(3-Hydroxypropyl)-2-(1,3,6-trimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione
- CAS:
- 2080306-23-4
- MF:
- C25H23N3O4
- MW:
- 429.47
- Mol File:
- 2080306-23-4.mol
BAY 299 Chemical Properties
- Boiling point:
- 688.7±55.0 °C(Predicted)
- Density
- 1.377±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:30.0(Max Conc. mg/mL);69.85(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);69.85(Max Conc. mM) - form
- A crystalline solid
- pka
- 14.98±0.10(Predicted)
- color
- Light yellow to yellow
BAY 299 Usage And Synthesis
Description
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM), also known as BRPF2, and the second bromodomain of transcription initiation factor TFIID subunits 1 (TAF1; IC50 = 13 nM). BAY-299 is >30-fold selective over BRPF1, BRPF3, BRD9, and ATAD2 and is >300-fold selective over BRD4. See the Structural Genomics Consortium (SGC) website for more information.
Uses
BAY 299, is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1, also known as BRPF2, and a strong inhibitor of TAF1/TAF1L BD2. These proteins play important roles in transcription regulation.
in vivo
Studies of the in vivo pharmacokinetic properties of BAY-299 in rat reveal that blood clearance is low (ca. 17% of hepatic blood flow), volume of distribution in steady-state high, terminal half-life long to very long (t1/2=10 h), and bioavailability high (F=73%). In vivo blood clearance is as anticipated based on rat liver microsome values but lower than expected based on hepatocyte data[1].
IC 50
BRPF2 BD: 67 nM (IC50); BRPF1 BD: 3150 nM (IC50); BRPF3 BD: 5550 nM (IC50); TAF1 BD2: 8 nM (IC50); TAF1L BD2: 106 nM (IC50)
storage
Store at -20°C
References
[1] MONTSERRAT PéREZ-SALVIA M E. Bromodomain inhibitors and cancer therapy: From structures to applications[J]. Epigenetics, 2016, 12 1: 323-339. DOI: 10.1080/15592294.2016.1265710
BAY 299Supplier
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