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BAY-299

CAS No. : 2080306-23-4

MCE 站：BAY-299

产品活性：BAY-299 是一种非常有效的双重抑制剂，抑制 BRPF2 溴结构域 (BD)，TAF1 BD2，和 TAF1L BD2，IC₅₀ 分别为 67 nM，8 nM 和 106 nM。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: BAY-299 is a dual inhibitor of the bromodomain ａnd PHD finger (BRPF) family member BRPF2 ａnd the TATA box binding protein-associated factors TAF1 ａnd TAF1L. TR-FRET assays showed that BAY-299 is a potent inhibitor of BRPF2 BD with an IC₅₀ of 67 nM, ａnd a selectivity of 47- ａnd 83-fold over BRPF1 ａnd BRPF3 BDs. The profile of BAY-299 is further confirmed by AlphaScreen assay, where an IC₅₀ of 97 nM ａnd a selectivity of 23- ａnd 25-fold over BRPF1 ａnd BRPF3 BDs are measured. NanoBRET experiments show that the interaction of BRPF2 BD with histones H4 ａnd H3.3 is blocked by BAY-299 with IC₅₀ values of 575 ａnd 825 nM, respectively. For TAF1 BD2, the IC₅₀ values are 970 ａnd 1400 nM, respectively. No inhibitory effect is observed for the interaction between BRPF1 or BRD4 ａnd histone H4 up to 10 μM for BAY-299. BAY-299 inhibits MOLM-13, MV4-11, 769-P, Jurkat, NCI-H526, CHL-1, ａnd 5637 cells proliferation with GI₅₀s of 1060, 2630, 3210, 3900, 6860, 7400, ａnd 7980 nM, respectively.

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 (t_1/2=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.

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