T5575
TG003
≥98% (HPLC)
Synonym(s):
(Z)-1-(3-Ethyl-5-methoxy-2,3-dihydrobenzothiazol-2-ylidene)propan-2-one
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About This Item
Empirical Formula (Hill Notation):
C13H15NO2S
CAS Number:
Molecular Weight:
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 has been used in PAC1 cell culture and in vitro kinase assays.
TG003 has been used to develop assays for screening substances that affect mRNA splicing1.
Biochem/physiol Actions
TG003, a CLK (cdc2-like kinase) family inhibitor is used as a drug for duchenne muscular dystrophy.
Potent, specific, reversible, and ATP-competitive inhibitor of Cdc2-like kinase (Clk). Ki = 10 nM for mClk1/Sty; IC50 = 15 nM, 20 nM, 200 nM, and > 10 mM for mClk4, mClk1, mClk2, and mClk3, respectively.
TG003 regulates alternative splicing and reduces the phosphorylation of SF2/ASF1.
Packaging
Packaged under nitrogen.
Preparation Note
TG003 is soluble in DMSO at 33 mg/ml.
Storage Class
11 - Combustible Solids
wgk
WGK 3
ppe
dust mask type N95 (US), Eyeshields, Gloves
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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)
Ken-ichi Fujita et al.
Bioscience, biotechnology, and biochemistry, 76(6), 1248-1251 (2012-07-14)
A number of proteins complete mRNA processing in the nucleus, thus, inhibitor of mRNA processing is worth finding to analyze the mechanism of mRNA maturation in detail. Here, we established a monitoring system for mRNA processing using a test compound
Global Trade Item Number
| SKU | GTIN |
|---|---|
| T5575-5MG | 04061833265741 |
| T5575-25MG | 04061833265734 |