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T5575

Sigma-Aldrich

TG003

≥98% (HPLC)

Synonym(s):

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

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$191.90
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$800.00

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5 MG
$191.90
25 MG
$800.00

About This Item

Empirical Formula (Hill Notation):
C13H15NO2S
CAS Number:
300801-52-9
Molecular Weight:
249.33
MDL number:
MFCD00624584
UNSPSC Code:
12352200
PubChem Substance ID:
24278611
NACRES:
NA.77

$191.90

List price$202.00
Web-Only Promotion

Available to ship onApril 08, 2025Details

Request a Bulk Order

Quality Level

100

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[1] and in vitro kinase assays.[2]
TG003 has been used to develop assays for screening substances that affect mRNA splicing1.

Biochem/physiol Actions

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.
TG003, a CLK (cdc2-like kinase) family inhibitor is used as a drug for duchenne muscular dystrophy.[3]

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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Certificates of Analysis (COA)

Lot/Batch Number
0000405753
0000405752
0000405753
0000405752
056M4620V

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Deciphering targeting rules of splicing modulator compounds: case of TG003
Sakuma M, et al.
BMC Molecular Biology, 16(1), 16-16 (2015)
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
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)
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)
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
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