TG003

TG003 Basic information
Product Name:TG003
Synonyms:CS-955;CS-1704;Cdc2-Like Kinase Inhibitor, TG003;TG003/TG-003;2-Propanone,1-(3-ethyl-5-Methoxy-2(3H)-benzothiazolylidene)-;(1Z)-1-(3-Ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one;1-(3-Ethyl-5-methoxy-2(3H)-benzothiazolylidene)-2-propanone;(Z)-1-(3-ethyl-5-methoxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
CAS:300801-52-9
MF:C13H15NO2S
MW:249.33
EINECS:
Product Categories:Inhibitors
Mol File:300801-52-9.mol
TG003 Structure
TG003 Chemical Properties
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
pka-1.76±0.20(Predicted)
form solid
color pale yellow
Sensitive Light Sensitive
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26-36
WGK Germany 3
MSDS Information
TG003 Usage And Synthesis
DescriptionCdc2-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.
UsesTG003 has been used in PAC1 cell culture and in vitro kinase assays.
UsesTG003 can be used as a potent CDC-2 kinase inhibitor, allowing for research into identification of signaling pathways and possible therapeutic treatments.
UsesCdc2-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.
Biochem/physiol ActionsTG003, a CLK (cdc2-like kinase) family inhibitor is used as a drug for duchenne muscular dystrophy.
TG003 Preparation Products And Raw materials
PLX4032 Vorinostat PD 0325901 VE-821 ML167 Diethylzinc Y27632 (hydrochloride)

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