| Bioactivity | 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]. |
| Target | IC50: 0.06 μM (Protein tyrosine phosphatase 1B, PTP1B); 4.3 μM (Aldose reductase, AKR1B1); 9 μM (TC-PTP) |
| Invitro | PTP1B/AKR1B1-IN-1 (化合物 6f) 与 PTP1B 和 AKR1B1 紧密结合，Ki 值分别为 4.6 μM 和 0.08 μM。PTP1B/AKR1B1-IN-1 (20 μM；24 小时) 在分化的小鼠 C2C12 细胞中表现出微不足道的细胞毒性[1]。PTP1B/AKR1B1-IN-1 (20 μM；24 小时) 用胰岛素（10 μM；15 分钟）增强鼠类 C2C12 细胞系中 Akt 磷酸化的增加[1]。PTP1B/AKR1B1-IN-1 (2 μM；24 小时) 导致山梨糖醇在人晶状体上皮细胞系 B3 (HLE) 细胞中的积累显着受损。实验中，可同时用 75 mM D-葡萄糖诱导 24 小时[1]。 Western Blot Analysis[1] Cell Line: |
| Name | PTP1B/AKR1B1-IN-1 |
| Formula | C22H21NO4S2 |
| Molar Mass | 427.54 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |