CAS NO: | 2080306-23-4 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Name: BAY-299 CAS#: 2080306-23-4 Chemical Formula: C25H23N3O4 Exact Mass: 429.1689 Molecular Weight: 429.476 | |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Technical Information | Synonym: BAY299; BAY 299; BAY-299. Chemical Name: 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 InChi Key: OFWWWKWUCDUISA-UHFFFAOYSA-N InChi Code: InChI=1S/C25H23N3O4/c1-14-12-20-21(27(3)25(32)26(20)2)13-19(14)28-23(30)17-8-4-7-16-15(6-5-11-29)9-10-18(22(16)17)24(28)31/h4,7-10,12-13,29H,5-6,11H2,1-3H3 SMILES Code: O=C1N(C2=C(C)C=C(N3C)C(N(C)C3=O)=C2)C(C4=CC=C(CCCO)C5=CC=CC1=C45)=O |
Bromodomains (BD) are readers of lysine acetylation marks present in
numerous proteins associated with chromatin. Here we describe a dual
inhibitor of the bromodomain and PHD finger (BRPF) family member BRPF2
and the TATA box binding protein-associated factors TAF1 and TAF1L.
These proteins are found in large chromatin complexes and play important
roles in transcription regulation. The substituted
benzoisoquinolinedione series was identified by high-throughput
screening, and subsequent structure-activity relationship optimization
allowed generation of low nanomolar BRPF2 BD inhibitors with strong
selectivity against BRPF1 and BRPF3 BDs. In addition, a strong
inhibition of TAF1/TAF1L BD2 was measured for most derivatives. The best
compound of the series was BAY-299, which is a very potent, dual
inhibitor with an IC50 of 67 nM for BRPF2 BD, 8 nM for TAF1
BD2, and 106 nM for TAF1L BD2. Importantly, no activity was measured for
BRD4 BDs. Furthermore, cellular activity was evidenced using a BRPF2-
or TAF1-histone H3.3 or H4 interaction assay.