WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406434
Description: TG003 is a potent, ATP-competitive inhibitor of Clk-family kinases (IC50 values are 20, 200 and 15 nM for mClk1, 2 and 4 respectively and >10 μ M for mClk3). . TG003 inhibited SF2/ASF-dependent splicing of beta-globin pre-mRNA in vitro by suppression of Clk-mediated phosphorylation. TG003 also suppressed serine/arginine-rich protein phosphorylation, dissociation of nuclear speckles, and Clk1/Sty-dependent alternative splicing in mammalian cells. Consistently, administration of TG003 rescued the embryonic defects induced by excessive Clk activity in Xenopus.
MedKoo Cat#: 406434
Chemical Formula: C13H15NO2S
Exact Mass: 249.08235
Molecular Weight: 249.3287
Elemental Analysis: C, 62.62; H, 6.06; N, 5.62; O, 12.83; S, 12.86
Related CAS #: 300801-52-9 719277-26-6.
Synonym: TG003; TG-003; TG 003.
IUPAC/Chemical Name: (Z)-1-(3-ethyl-5-methoxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
InChi Key: BGVLELSCIHASRV-QPEQYQDCSA-N
InChi Code: 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-
SMILES Code: CC(/C=C1SC2=CC=C(OC)C=C2N\1CC)=O
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 249.3287 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Li P, Carter G, Romero J, Gower KM, Watson J, Patel NA, Cooper DR. Clk/STY (cdc2-like kinase 1) and Akt regulate alternative splicing and adipogenesis in 3T3-L1 pre-adipocytes. PLoS One. 2013;8(1):e53268. doi: 10.1371/journal.pone.0053268. Epub 2013 Jan 4. PubMed PMID: 23308182; PubMed Central PMCID: PMC3537621.
2: Ninomiya K, Kataoka N, Hagiwara M. Stress-responsive maturation of Clk1/4 pre-mRNAs promotes phosphorylation of SR splicing factor. J Cell Biol. 2011 Oct 3;195(1):27-40. doi: 10.1083/jcb.201107093. Epub 2011 Sep 26. PubMed PMID: 21949414; PubMed Central PMCID: PMC3187705.
3: Nishida A, Kataoka N, Takeshima Y, Yagi M, Awano H, Ota M, Itoh K, Hagiwara M, Matsuo M. Chemical treatment enhances skipping of a mutated exon in the dystrophin gene. Nat Commun. 2011;2:308. doi: 10.1038/ncomms1306. PubMed PMID: 21556062; PubMed Central PMCID: PMC3113229.
4: Rosenthal AS, Tanega C, Shen M, Mott BT, Bougie JM, Nguyen DT, Misteli T, Auld DS, Maloney DJ, Thomas CJ. Potent and selective small molecule inhibitors of specific isoforms of Cdc2-like kinases (Clk) and dual specificity tyrosine-phosphorylation-regulated kinases (Dyrk). Bioorg Med Chem Lett. 2011 May 15;21(10):3152-8. doi: 10.1016/j.bmcl.2011.02.114. Epub 2011 Mar 4. PubMed PMID: 21450467; PubMed Central PMCID: PMC3085634.
5: James BP, Staatz WD, Wilkinson ST, Meuillet E, Powis G. Superoxide dismutase is regulated by LAMMER kinase in Drosophila and human cells. Free Radic Biol Med. 2009 Mar 15;46(6):821-7. doi: 10.1016/j.freeradbiomed.2008.12.012. Epub 2008 Dec 24. PubMed PMID: 19135146; PubMed Central PMCID: PMC2699669.
6: Yomoda J, Muraki M, Kataoka N, Hosoya T, Suzuki M, Hagiwara M, Kimura H. Combination of Clk family kinase and SRp75 modulates alternative splicing of Adenovirus E1A. Genes Cells. 2008 Mar;13(3):233-44. doi: 10.1111/j.1365-2443.2008.01163.x. PubMed PMID: 18298798.
7: Muraki M, Ohkawara B, Hosoya T, Onogi H, Koizumi J, Koizumi T, Sumi K, Yomoda J, Murray MV, Kimura H, Furuichi K, Shibuya H, Krainer AR, Suzuki M, Hagiwara M. Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem. 2004 Jun 4;279(23):24246-54. Epub 2004 Mar 8. PubMed PMID: 15010457.