aldose reductase-in-1

Aldose reductase-IN-1 (AT-001, Caficrestat) is a highly potent inhibitor of aldose reductase with an IC50 value of 28.9 pM, which can target the relaxin hormone signaling pathway in prostate cancer models.

Aldose reductase-IN-4 (compound IIc) is an inhibitor of aldose reductase with IC50 values of 11.70 μM for ALR1 and 0.98 μM for ALR2, respectively [1].

Aldose reductase-IN-6 (Compound 3) is a competitive inhibitor of aldose reductase (AR) with an IC50 of 3.164 μM and a Ki of 0.018 μM. Notably, Aldose reductase-IN-6 demonstrates no cytotoxicity toward normal cells [1].

5α-reductase-IN-1 is a potent inhibitor of the enzyme 5α-reductase. This compound is primarily employed in research studies to investigate its potential efficacy in treating patterned alopecia. It is commonly used in combination with minoxidil, a well-known treatment for hair loss.

Aldose reductase-IN-5 is an inhibitor of aldose reductase (ALR2) that enhances the combination of inhibitory excitability and antioxidant capacity, thereby delaying the diabetes complications progress.

Aldose reductase-IN-3 (Compound 5) is an effective and moderately selective aldose reductase (AR) inhibitor (IC50=3.99 μM) with research potential in sepsis, a molecular target involved in various inflammatory diseases (including sepsis).

Aldose reductase-IN-2 (Compound 5f) is a potent aldose reductase (AR) inhibitor with antioxidant properties, making it a promising drug for anti-diabetic complications.

Aldose 1-epimerase (mutarotases), an essential enzyme for carbohydrate metabolism, facilitates the interconversion between α- and β-anomers of hexose sugars, including glucose and galactose. This enzyme plays a vital role in normal carbohydrate metabolism and the synthesis of complex oligosaccharides [1].

HMG-CoA Reductase-IN-1, an inhibitor of HMG-CoA reductase, demonstrates strong inhibitory activity on HMGR and affinity for OATP1B1, with pIC50 and pKm values of 8.54 and 1.98, respectively. It is utilized in hypercholesterolemia research [1].

3-Isomangostin is a potent human aldose reductase inhibitor with an IC50 of 3.48 uM; it is also an acetylcholinesterase selective inhibitor. 3-Isomangostin has free radical scavenging activity; it shows antiplasmodial activity with IC50 values in the rang

APPA, an aldose reductase inhibitor, demonstrates efficacy in preventing apoptosis and symptoms of Streptozotocin-induced diabetes in rats through inhibition of the polyol pathway. This compound shows promise for research into diabetic nephropathy (DN) [1].

ALR1 2-IN-1 (Compound 6e) is an aldehyde reductase (ALR1) inhibitor (IC50: 3.26 μM) and aldose reductase (ALR2) inhibitor (IC50: 3.06 μM) with anticancer effects.

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].