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关于此项目
经验公式(希尔记法):
C13H15NO2S
化学文摘社编号:
分子量:
249.33
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
mp
132-132.5 °C
solubility
DMSO: 33 mg/mL
storage temp.
2-8°C
SMILES string
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
Application
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。
Biochem/physiol Actions
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。
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。
Packaging
在氮气保护下封装。
Preparation Note
TG003可以33 mg/ml溶于DMSO。
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
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)
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)
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| T5575-5MG | 04061833265741 |
| T5575-25MG | 04061833265734 |