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Merck

T5575

Sigma-Aldrich

TG003

≥98% (HPLC)

Sinónimos:

(Z)-1-(3-Ethyl-5-methoxy-2,3-dihydrobenzothiazol-2-ylidene)propan-2-one

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About This Item

Fórmula empírica (notación de Hill):
C13H15NO2S
Número de CAS:
Peso molecular:
249.33
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

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 regulates alternative splicing and reduces the phosphorylation of SF2/ASF1.
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.

Packaging

Packaged under nitrogen.

Preparation Note

TG003 is soluble in DMSO at 33 mg/ml.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves


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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
The TORC1-Regulated CPA Complex Rewires an RNA Processing Network to Drive Autophagy and Metabolic Reprogramming
Tang H W, et al.
Cell Metabolism, 27(5), 1040-1054 (2018)
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)
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
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

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