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PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].
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50 mg | Inquiry | Backorder |
Description | PTP1B/AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1]. |
In vitro | PTP1B/AKR1B1-IN-1 exhibits tight binding affinity to PTP1B and AKR1B1 with K_i values of 4.6 μM and 0.08 μM, respectively. At 20 μM for 24 hours, this compound shows negligible cytotoxicity in differentiated murine C2C12 myoblasts [1]. It also enhances insulin (10 μM, 15 minutes)-stimulated Akt phosphorylation in the C2C12 cell line at the same concentration and duration [1]. Additionally, PTP1B/AKR1B1-IN-1 (2 μM, 24 hours) significantly reduces sorbitol accumulation in the human lens epithelial cell line B3 (HLE) when co-incubated with 75 mM D-glucose for 24 hours [1]. |
Molecular Weight | 427.54 |
Formula | C22H21NO4S2 |
Storage | Shipping with blue ice. |
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