| Identification | Back Directory | [Name]
TG003 | [CAS]
300801-52-9 | [Synonyms]
CS-955
CS-1704
(E/Z)-TG003
TG003/TG-003
TG003 USP/EP/BP
Cdc2-Like Kinase Inhibitor, TG003
1-(3-Ethyl-5-methoxy-2(3H)-benzothiazolylidene)-2-propanone
2-Propanone,1-(3-ethyl-5-Methoxy-2(3H)-benzothiazolylidene)-
1-(3-Ethyl-5-methoxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
(1Z)-1-(3-Ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one
(Z)-1-(3-ethyl-5-methoxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one | [Molecular Formula]
C13H15NO2S | [MDL Number]
MFCD00624584 | [MOL File]
300801-52-9.mol | [Molecular Weight]
249.33 |
| Chemical Properties | Back Directory | [Melting point ]
132-132.5 °C | [Boiling point ]
386.0±42.0 °C(Predicted) | [density ]
1.237±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 33 mg/mL | [form ]
solid | [pka]
-1.76±0.20(Predicted) | [color ]
pale yellow | [Sensitive ]
Light Sensitive |
| Hazard Information | Back Directory | [Description]
Cdc2-like kinase (Clk), among a number of other kinases, phosphorylates serine/arginine-rich proteins which play a role in alternative splicing of pre-mRNA. The Clk family consists of four members, which include Clk1/Sty and Clk2-4. TG003 is a novel benzothiazole compound that demonstrates potent inhibition of Clk1/Sty and Clk4 with IC50 values of 20 and 15 nM, respectively. TG003 exhibits considerably weaker inhibition of Clk2 and Clk3 (IC50 = 200 nM and >10 μM, respectively). Through suppression of Clk-mediated phosphorylation, TG003 inhibits SF2/ASF-dependent splicing of β-globin pre-mRNA at 1 μM in vitro. At 10 μM, TG003 rescues the embryonic defects induced by excessive Clk activity in Xenopus. | [Uses]
Cdc2-Like Kinase Inhibitor, TG003 is a benzothiazole agent that acts as a specific and ATP-competitive inhibitor of Clk family members. Reports show that TG003 modifies the regulation of alternative splicing modulated by phosphorylation of SR proteins in vitro, and rescues defects in the development of Xenopus caused by an overabundance of Clk activity. | [Uses]
TG003 can be used as a potent CDC-2 kinase inhibitor, allowing for research into identification of signaling pathways and possible therapeutic treatments.
| [Uses]
TG003 has been used in PAC1 cell culture and in vitro kinase assays. | [Biochem/physiol Actions]
TG003, a CLK (cdc2-like kinase) family inhibitor is used as a drug for duchenne muscular dystrophy. |
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| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
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