TCS 401, 10 mg

TCS 401 is a potent and selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B). The structure is a derivate of 2-(oxalyl-amino)-benzoic acid (OBA), a general inhibitor of PTPs, targeting the highly conserved phosphate binding loop. TCS 401 shows a remarkable selectivity for PTP1B vs. other PTPs (Ki values are 0.29, 59, 560, 1100, > 2000, > 2000 and > 2000 μM for PTP1B, CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1 and LAR D1D2 at the pH optimum of PTP1B at pH 5.5). 

Solubility: DMSO to 5 mM, Molecular Weight:  306.7 g/mol

Formula: C₁₀H₁₀N₂O₅S.HCl �

Product specific literature references:

Andersen HS, Olsen OH, Iversen LF, S�rensen AL, Mortensen SB, Christensen MS, Branner S, Hansen TK, Lau JF, Jeppesen L, Moran EJ, Su J, Bakir F, Judge L, Shahbaz M, Collins T, Vo T, Newman MJ, Ripka WC, M�ller NP. (2002) "Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B." J Med Chem.;45(20):4443-59

Iversen LF, Andersen HS, Branner S, Mortensen SB, Peters GH, Norris K, Olsen OH, Jeppesen CB, Lundt BF, Ripka W, M�ller KB, M�ller NP. (2000) "Structure-based design of a low molecular weight, nonphosphorus, nonpeptide, and highly selective inhibitor of protein-tyrosine phosphatase 1B." J Biol Chem.;275(14):10300-7

Pedersen AK, Branner S, Mortensen SB, Andersen HS, Klausen KM, M�ller KB, M�ller NP, Iversen LF.(2004) " Affinity purification of recombinant protein-tyrosine phosphatase 1B using a highly selective inhibitor." J Chromatogr B Analyt Technol Biomed Life Sci. 799(1):1-8.