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Chemical Structure| 719277-26-6 Chemical Structure| 719277-26-6

Structure of TG003
CAS No.: 719277-26-6

Chemical Structure| 719277-26-6

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TG003 is a potent inhibitor of Clk1/Sty and Clk4 with IC50 of 15-20 nM, less potency on Clk2 (IC50= 200 nM).

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Product Details of TG003

CAS No. :719277-26-6
Formula : C13H15NO2S
M.W : 249.33
SMILES Code : CC(/C=C1SC2=CC=C(OC)C=C2N\1CC)=O
MDL No. :MFCD00624584
InChI Key :BGVLELSCIHASRV-QPEQYQDCSA-N
Pubchem ID :1893668

Safety of TG003

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of TG003

Hedgehog

Isoform Comparison

Biological Activity

Description
TG003 is a potent inhibitor of Clk1/Sty, which inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 5 µM and 20 µM 1 hour Evaluate the inhibitory effect of TG693 on SR protein phosphorylation Sci Rep. 2017 May 30;7:46126
H1299 cells 10 µM to 100 µM 24 hours TG003 treatment promoted alternative splicing of TP53 intron 9, increasing β and γ spliced products Cell Death Differ. 2014 Sep;21(9):1377-87.
MCF7 cells 10 µM to 100 µM 24 hours TG003 treatment increased endogenous p53β and p53γ protein expression by modulating alternative splicing of TP53 intron 9 Cell Death Differ. 2014 Sep;21(9):1377-87.
HeLa cells 20 µM 24 hours TG003 induced widespread changes in alternative splicing of cancer-associated genes Sci Rep. 2021 Apr 12;11(1):7963
293T cells 10 µM or 50 µM 24 hours To evaluate the compensatory effect of TG003 on the transcriptional suppression defect of NR0B1 Q408X mutation. Results showed that TG003 significantly alleviated the impaired transcriptional suppressive activity of the NR0B1 Q408X mutation. J Endocr Soc. 2022 Apr 22;6(6):bvac068
HeLa cells 50 µM 30 minutes TG003 treatment reduced the nuclear signal for intron 4 of Clk1. J Cell Biol. 2011 Oct 3;195(1):27-40
NIH-3T3 cells 5, 10, 20 µM 30 minutes TG003 treatment reduced the amount of intron 3/4-retaining Clk1 RNA and increased the amount of mature Clk1 mRNA. J Cell Biol. 2011 Oct 3;195(1):27-40
PC3 prostate cancer cells 10–50 µM 48 hours Inhibition of CLK1 increased expression of the anti-apoptotic isoform caspase 9b BMC Cancer. 2018 Apr 2;18(1):355
MCF-7 cells 10 µM 48 hours To evaluate the effect of TG003 on SOD1 and SOD2 protein expression. Results showed that TG003 treatment led to an approximate 2-fold increase in SOD1 protein levels in MCF-7 cells, but no significant change in SOD2 protein levels. Free Radic Biol Med. 2009 Mar 15;46(6):821-7.
HeLa cells 10 µM 48 hours To evaluate the effect of TG003 on SOD1 and SOD2 protein expression. Results showed that TG003 treatment led to an approximate 2-fold increase in SOD1 protein levels in HeLa and MCF-7 cells, and a 3-fold increase in SOD2 protein levels in HeLa cells. Free Radic Biol Med. 2009 Mar 15;46(6):821-7.
Human neurons 20 µM 5 weeks TG003 treatment exacerbated dendrite length increases in R841X neurons Nat Neurosci. 2019 Apr;22(4):556-564.
CP-CML CD34+ cells 20 µM 72 hours Evaluate the effect of TG003 on CP-CML CD34+ cell viability, results showed reduced cell viability Cancers (Basel). 2022 Sep 27;14(19):4695
KCL22 cells 54.0 µM (IC50) 72 hours Evaluate the effect of TG003 on KCL22 cell viability, results showed IC50 of 54.0 μM Cancers (Basel). 2022 Sep 27;14(19):4695
K562 cells 51.4 µM (IC50) 72 hours Evaluate the effect of TG003 on K562 cell viability, results showed IC50 of 51.4 μM Cancers (Basel). 2022 Sep 27;14(19):4695
PNT2 cells 1 µM, 10 µM, 50 µM 72 hours TG003 reduced cell proliferation and increased apoptosis, but with lower sensitivity Sci Rep. 2021 Apr 12;11(1):7963
DU145 cells 1 µM, 10 µM, 50 µM 72 hours TG003 reduced cell proliferation and increased apoptosis Sci Rep. 2021 Apr 12;11(1):7963
PC3 cells 1 µM, 10 µM, 50 µM 72 hours TG003 reduced cell proliferation and increased apoptosis Sci Rep. 2021 Apr 12;11(1):7963
3T3-L1 pre-adipocytes 50 nM From day 3 to day 8 of differentiation TG003 treatment reduced lipid droplet size, increased mitochondrial number, and induced UCP1 and PGC1α expression, indicating a shift of 3T3-L1 cells towards beige adipocytes. J Cell Mol Med. 2022 Aug;26(15):4183-4194

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ICR mice Oral 30 mg/kg Single dose Evaluate the bioavailability of TG693 in mouse skeletal muscle and its inhibitory effect on SR protein phosphorylation Sci Rep. 2017 May 30;7:46126
CD1 nude mice PC3 cell xenograft model Intraperitoneal injection 50 µM Twice a week for 29 days TG003 significantly inhibited the growth of xenograft tumors Sci Rep. 2021 Apr 12;11(1):7963

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.05mL

4.01mL

2.01mL

40.11mL

8.02mL

4.01mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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