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Brr2-IN-3 {[allProObj[0].p_purity_real_show]}

货号:A666053 同义名: Brr2 Inhibitor 9;Brr2 Inhibitor C9

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.

Brr2-IN-3 化学结构 CAS号:2104030-82-0
Brr2-IN-3 化学结构
CAS号:2104030-82-0
Brr2-IN-3 3D分子结构
CAS号:2104030-82-0
Brr2-IN-3 化学结构 CAS号:2104030-82-0
Brr2-IN-3 3D分子结构 CAS号:2104030-82-0
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Brr2-IN-3 纯度/质量文件 产品仅供科研

货号:A666053 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLM636-1298, IC50: 0.97 μM

BLMfull-length, IC50: 2.98 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, IC50: 46.11 nM

Leucyl-tRNA synthetase, Kd: 42.1 nM

98%
SU056 +

YB-1, IC50: 1.73 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Brr2-IN-3 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].

Brr2-IN-3 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.

Brr2-IN-3 实验方案

计算器
存储液制备 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

Brr2-IN-3 技术信息

CAS号2104030-82-0
分子式C24H20N4O3S
分子量 444.506
别名 Brr2 Inhibitor 9;Brr2 Inhibitor C9;GUN30820;Brr2-​IN-​3
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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
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