PTP1B/AKR1B1-IN-1 

PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC₅₀s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC₅₀ value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels^[1].

IC50: 0.06 μM (Protein tyrosine phosphatase 1B, PTP1B); 4.3 μM (Aldose reductase, AKR1B1); 9 μM (TC-PTP)^[1]

PTP1B/AKR1B1-IN-1 (compound 6f) tightly binds to PTP1B and AKR1B1 with K_i values of 4.6 μM, and 0.08 μM, respectively^[1].
PTP1B/AKR1B1-IN-1 (20 μM; 24 h) shows insignificant cytotoxicity in differentiated murine C2C12 cells^[1].
PTP1B/AKR1B1-IN-1 (20 μM; 24 h) enhances the increases of Akt phosphorylation in murine C2C12 cell line with insulin (10 μM; 15 min)^[1].
PTP1B/AKR1B1-IN-1 (2 μM; 24 h) results significant impairment of sorbitol accumulation in human lens epithelial line B3 (HLE) cells, induced with 75 mM d-glucose for 24 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

427.54

C₂₂H₂₁NO₄S₂

O=C(CN1C(/C(SC1=S)=C/C2=CC=CC(OCCCCC3=CC=CC=C3)=C2)=O)O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Maccari R, et al. Designed multiple ligands for the treatment of type 2 diabetes mellitus and its complications: Discovery of (5-arylidene-4-oxo-2-thioxothiazolidin-3-yl)alkanoic acids active as novel dual-targeted PTP1B/AKR1B1 inhibitors. Eur J Med Chem. 2023 Apr 5;252:115270.  [Content Brief]