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BAY-299
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY-299图片
CAS NO:2080306-23-4
规格:≥98%
包装与价格:
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

产品介绍
理化性质和储存条件


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 InformationSynonym: 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
实验参考方法

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.    

These protocols are for reference only. InvivoChem does not independently validate these methods.