所有图片(1)
About This Item
经验公式(希尔记法):
C13H15NO2S
CAS号:
分子量:
249.33
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
mp
132-132.5 °C
溶解性
DMSO: 33 mg/mL
储存温度
2-8°C
SMILES字符串
CCN1\C(Sc2ccc(OC)cc12)=C\C(C)=O
InChI
1S/C13H15NO2S/c1-4-14-11-8-10(16-3)5-6-12(11)17-13(14)7-9(2)15/h5-8H,4H2,1-3H3/b13-7-
InChI key
BGVLELSCIHASRV-QPEQYQDCSA-N
应用
TG003已被用于PAC1细胞培养和体外激酶检测中。
TG003已被用于开发可影响mRNA剪接1的筛选底物的检测体系。
生化/生理作用
Cdc2样激酶(Clk)的有效、特异、可逆及ATP竞争性抑制剂。对于mClk1/Sty的Ki = 10 nM;对于mClk4、mClk1、mClk2和mClk3分别的IC50 = 15 nM、20 nM、200 nM和> 10 mM。
TG003可调节可变剪接并降低SF2/ASF1的磷酸化。
TG003,一种CLK(cdc2样激酶)家族抑制剂,可用作杜氏肌营养不良症的药物。
包装
在氮气保护下封装。
制备说明
TG003可以33 mg/ml溶于DMSO。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
David O Bates et al.
Pharmacological reviews, 69(1), 63-79 (2016-12-31)
More than 95% of genes in the human genome are alternatively spliced to form multiple transcripts, often encoding proteins with differing or opposing function. The control of alternative splicing is now being elucidated, and with this comes the opportunity to
Deciphering targeting rules of splicing modulator compounds: case of TG003
Sakuma M, et al.
BMC Molecular Biology, 16(1), 16-16 (2015)
Brandon E Aubol et al.
The FEBS journal, 288(2), 566-581 (2020-05-03)
The assembly and activation of the spliceosome rely upon the phosphorylation of an essential family of splicing factors known as the serine-arginine (SR) proteins. Although it has been demonstrated recently that two enzyme families, the SR protein kinases (SRPKs) and
Yukiya Sako et al.
Scientific reports, 7, 46126-46126 (2017-05-31)
Duchenne muscular dystrophy (DMD) is a fatal progressive muscle-wasting disease. Various attempts are underway to convert severe DMD to a milder phenotype by modulating the splicing of the dystrophin gene and restoring its expression. In our previous study, we reported
The alternative splicing program of differentiated smooth muscle cells involves concerted non-productive splicing of post-transcriptional regulators
Llorian M, et al.
Nucleic Acids Research, 44(18), 8933-8950 (2016)
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