产品说明书

PFI-4

Print
Chemical Structure| 900305-37-5 同义名 : -
CAS号 : 900305-37-5
货号 : A157158
分子式 : C21H24N4O3
纯度 : 99%+
分子量 : 380.44
MDL号 : MFCD14744412
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(65.71 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BRPF

    BRPF2, IC50:7.9 μM

    BRPF1, IC50:80 nM
描述 BRPF1 belong to the the BRPF (bromodomain and PHD finger-containing) family. BRPF1 is a component of the MOZ/MORF histone acetyltransferase complexes which function as a transcriptional regulators[2]. BRPF1 also links the catalytic HATs to the other subunits ING5 and hEAF6.8. BRPF1 is important for maintaining skeletal development and Hox gene expression[3]. PFI-4 is a selective BRPF1 inhibitor. According to data obtained by TR-FRET competition binding, the pIC50s of PFI-4 against BRPF1, BRPF2, BRPF3, BRD4 BD1 and BRD4 BD2 were 7.1, 5.1, <4.0, <4.3, <4.3, respectively. A nanoBRET assay revealed that the pIC50 of PFI-4 agianst BRPF1 was 6.0. In a BROMOscan panel of 35 bromodomain binding assays, the pKd of PFI-4 binding BRPF1 was 8.0 and good selectivity over other bromodomians was revealed. In a cellular protein interaction assay measuring disruption of chromatin binding, PFI-4 exhibited a dose-response curve with micromolar IC50[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.29mL

5.26mL

2.63mL
参考文献

[1]Demont EH, Bamborough P, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.

[2]Yan K, Rousseau J, Littlejohn RO, Kiss C, Lehman A, Rosenfeld JA, Stumpel CTR, Stegmann APA, Robak L, Scaglia F, Nguyen TTM, Fu H, Ajeawung NF, Camurri MV, Li L, Gardham A, Panis B, Almannai M, Sacoto MJG, Baskin B, Ruivenkamp C, Xia F, Bi W; DDD Study; CAUSES Study, Cho MT, Potjer TP, Santen GWE, Parker MJ, Canham N, McKinnon M, Potocki L, MacKenzie JJ, Roeder ER, Campeau PM, Yang XJ. Mutations in the Chromatin Regulator Gene BRPF1 Cause Syndromic Intellectual Disability and Deficient Histone Acetylation. Am J Hum Genet. 2017 Jan 5;100(1):91-104.

[3]Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932.