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Brr2-IN-3

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Chemical Structure| 2104030-82-0 同义名 : Brr2 Inhibitor 9;Brr2 Inhibitor C9;GUN30820;Brr2-​IN-​3
CAS号 : 2104030-82-0
货号 : A666053
分子式 : C24H20N4O3S
纯度 : 99%+
分子量 : 444.506
MDL号 : MFCD32857110
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(112.48 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
动物实验配方：
生物活性
靶点

  • helicase
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL
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.