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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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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

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 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 Code

11 - Combustible Solids

WGK

WGK 3

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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 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)
Brandon E Aubol et al.
The FEBS journal, 288(2), 566-581 (2020-05-03)
The assembly and activation of the spliceosome rely upon the phosphorylation of an essential family of splicing factors known as the serine-arginine (SR) proteins. Although it has been demonstrated recently that two enzyme families, the SR protein kinases (SRPKs) and
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