A cell-permeable allosteric inhibitor of PTP1B
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PTP1B Inhibitor

Item No. 15782

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-[(2-thiazolylamino)sulfonyl]phenyl]-6-benzofuransulfonamide
CAS Number
765317-72-4
Synonyms
  • Protein Tyrosine Phosphatase 1B Inhibitor
  • PTPN1 Inhibitor
  • Tyrosine-protein Phosphatase Non-Receptor Type 1 Inhibitor
Molecular Formula
C26H19Br2N3O7S3
Formula Weight
741.5
Purity
≥70%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/ml
SMILES
O=S(NC1=CC=C(S(NC2=NC=CS2)(=O)=O)C=C1)(C3=CC=C(C(C(C4=CC(Br)=C(O)C(Br)=C4)=O)=C(CC)O5)C5=C3)=O
InChi Code
InChI=1S/C26H19Br2N3O7S3/c1-2-21-23(24(32)14-11-19(27)25(33)20(28)12-14)18-8-7-17(13-22(18)38-21)41(36,37)30-15-3-5-16(6-4-15)40(34,35)31-26-29-9-10-39-26/h3-13,30,33H,2H2,1H3,(H,29,31)
InChi Key
SXKBTDJJEQQEGE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Protein tyrosine phosphatase 1B (PTP1B) has critical roles in cell signaling relevant to diabetes, obesity, and cancer.1,2 PTP1B inhibitor is a cell-permeable allosteric inhibitor of PTP1B (IC50s = 4 and 8 µM for 403 and 298 residue PTP1B forms, respectively).3 It binds reversibly and non-competitively, altering the conformation of the catalytic pocket.3,4 PTP1B inhibitor selectively increases the phosphorylation of the insulin receptor, insulin receptor substrate 1, and Akt, mimicking the action of insulin.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, S., and Zhang, Z.Y. PTP1B as a drug target: Recent developments in PTP1B inhibitor discovery. Drug Discov. Today 12(9-10), 373-381 (2007).

    2. Tonks, N.K. Protein tyrosine phosphatases - from housekeeping enzymes to master regulators of signal transduction. FEBS J. 280(2), 346-378 (2013).

    3. Wiesmann, C., Barr, K.J., Kung, J., et al. Allosteric inhibition of protein tyrosine phosphatase 1B. Nat. Struct. Mol. Biol. 11(8), 730-737 (2004).

    4. Li, S., Zhang, J., Lu, S., et al. The mechanism of allosteric inhibition of protein tyrosine phosphatase 1B. PLoS One 9(5), e97668 (2014).