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CAS No.: 2104030-82-0

Brr2-IN-3 Catalog No. CSN20324

Synonyms: Brr2 Inhibitor 9;Brr2 inhibitor C9;GUN-30820

Brr2 inhibitor C9 is an allosteric inhibitor targeting the spliceosomal RNA helicase Brr2, which implicated in autosomal-dominant retinitis pigmentosa, a group of progressive retinal degenerative disorders.

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描述Brr2 is an RNA helicase that belongs to the Ski2-like subfamily. It serves as an essential component of spliceosome by catalyzing the unwinding of the U4/U6 RNA duplex. Brr2 Inhibitor C9 is a potent and selective allosteric inhibitor of Brr2 helicase with an IC50 value of 1.3μM. It also exhibits excellent inhibitory activity against Brr2 ATPase with an IC50 value of 79nM. Brr2 Inhibitor C9 showed no inhibitory activity against single-cassette RNA helicases, such as DEAD box-family RNA helicase and DEAH box-family RNA helicase^[2].
参考文献

[1] Iwatani-Yoshihara M, Ito M, et al. Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2. J Med Chem. 2017 Jun 20.
[2] Iwatani-Yoshihara M, Ito M, Klein MG, Yamamoto T, Yonemori K, Tanaka T, Miwa M, Morishita D, Endo S, Tjhen R, Qin L, Nakanishi A, Maezaki H, Kawamoto T. Discovery of Allosteric Inhibitors Targeting the Spliceosomal RNA Helicase Brr2. J Med Chem. 2017 Jul 13;60(13):5759-5771.

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
- 2.2497 mL
- 11.2485 mL
- 22.4969 mL
- 5 mM
- 0.4499 mL
- 2.2497 mL
- 4.4994 mL
- 10 mM
- 0.2250 mL
- 1.1248 mL
- 2.2497 mL

技术信息

CAS号

2104030-82-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H20N4O3S

运输

蓝冰

分子量

444.51

别名

Brr2 Inhibitor 9;Brr2 inhibitor C9;GUN-30820

溶解度

DMSO	89.0 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (4.5 mM)

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