I-BRD9

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Chemical Structure| 1714146-59-4 同义名 : GSK602
CAS号 : 1714146-59-4
货号 : A178532
分子式 : C22H22F3N3O3S2
纯度 : 99%+
分子量 : 497.55
MDL号 : MFCD28952791
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(24.12 mM)，配合低频超声助溶，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
生物活性
靶点

  • BET

    BRD4, pIC50:5.3

    BRD9, pIC50:7.3
描述 BRD9 (Bromodomain Containing 9) plays a role in chromatin remodeling and regulation of transcription. It acts as a chromatin reader that recognizes and binds acylated histones. BRD9 is also component of SWI/SNF chromatin remodeling subcomplex GBAF that carries out key enzymatic activities, changing chromatin structure by altering DNA-histone contacts within a nucleosome in an ATP-dependent manner[2]. I-BRD9 is a selective BRD9 inhibitor. According to data obtained by TR-FRET assays, the pIC50s of I-BRD9 against BRD9 and BRD4 were 7.3 and 5.3, respectively, suggesting 100-fold selectivity for BRD9. A nanoBRET assay revealed that the pIC50 of I-BRD9 agianst BRD9 was 6.8. In a BROMOscan profiling against 34 bromodomains, the pKd of I-BRD9 binding BRD9 was 8.7 and good selectivity over other bromodomians was revealed[3]. According data obtained by MTT cytotoxicity assays, the inhibitory IC50s of I-BRD9 against cell proliferation of Rhabdoid tumor cell lines BT12, BT16, Chla266, G401 and KD were 21.2 μM, 11.2 μM, 13.3 μM, 13.4 μM and 8.1 μM, respectively[4]. Kasumi-1 cells were treated by 10 μM I-BRD9 for 6h and results obtained by qPCR assays suggested that I-BRD9 suppressed the genes of CLEC1, DUSP6, FES and SAMSN1[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.05mL

2.01mL

1.00mL

20.10mL

4.02mL

2.01mL
参考文献

[1]Theodoulou NH, Bamborough P, et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39.

[2]Alpsoy A, Dykhuizen EC. Glioma tumor suppressor candidate region gene 1 (GLTSCR1) and its paralog GLTSCR1-like form SWI/SNF chromatin remodeling subcomplexes. J Biol Chem. 2018 Mar 16;293(11):3892-3903.

[3]Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon AM, Molnar J, Robson SC, Tomkinson NC, Kouzarides T, Prinjha RK, Humphreys PG. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39.

[4]Krämer KF, Moreno N, Frühwald MC, Kerl K. BRD9 Inhibition, Alone or in Combination with Cytostatic Compounds as a Therapeutic Approach in Rhabdoid Tumors. Int J Mol Sci. 2017 Jul 16;18(7):1537.