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Merck
CN

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:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Technical Service
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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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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
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

SKUGTIN
T5575-5MG04061833265741
T5575-25MG04061833265734