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CAS No.: 1714146-59-4

I-BRD9 Catalog No. CSN17207

Synonyms: GSK602

I-BRD9 is a BRD9 bromodomain inhibitor with pIC50 value of 7.3 and pKd of 8.7. BRD9 fuctions as part of the SWI/SNF complex in chromatin remolding .

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技术信息

生物活性

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0098 mL
- 10.0492 mL
- 20.0983 mL
- 5 mM
- 0.4020 mL
- 2.0098 mL
- 4.0197 mL
- 10 mM
- 0.2010 mL
- 1.0049 mL
- 2.0098 mL

技术信息

CAS号

1714146-59-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H22F3N3O3S2

运输

蓝冰

分子量

497.55

别名

GSK602

溶解度

DMSO	16.0 mg/mL (32.2 mM) warming
Water	insoluble

动物实验配方

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I-BRD9 Catalog No. CSN17207

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