Metabolism

Mucidin is an antifungal antibiotic that inhibits electron transfer reactions within the mitochondrial respiratory chain's cytochrome bc1 complex.

Carbonic anhydrase inhibitor 17 (compound 7c) is a pyrazine-based sulfonamide that acts as a carbonic anhydrase II inhibitor, with an IC50 value of 0.63 nM.

Vimirogant is a RORγ inhibitor (Ki: <100 nM).

AZ513 is a reversible FAAH inhibitor, exhibiting an IC50 of 551 nM for human FAAH and 27 nM for rat FAAH. It inhibits the hydrolysis of arachidonoyl ethanolamide in HEK293 cells transfected with human FAAH, with an IC50 of 360 nM.

JTT-553 is a DGAT1 inhibitor with an IC50 of 2.38 nM. It effectively reduces plasma levels of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and liver triglycerides (TG). JTT-553 enhances insulin-dependent glucose absorption and glucose intolerance in the adipose tissue of diet-induced obese (DIO) mice. In KK-Ay mice, it lowers TNF-α mRNA levels and elevates GLUT4 mRNA levels in adipose tissue. By contributing to weight loss, JTT-553 improves insulin resistance in adipose tissue and overall glucose metabolism. This compound is useful for research on obesity and type 2 diabetes mellitus (T2DM).

ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) (IC50: 218.9 μM) that lacks inhibitory activity against LPAR1.

COTC is an anticancer bacterial metabolite; inhibits glyoxalase with GSH, halts HeLa cell growth, and fights tumor in Ehrlich murine model.

CIT-ALD is an aldehyde intermediate formed during the metabolism of Citalopram. It has potential applications in the research of neurological disorders.

PNPLA3 Modifier 1 (Compound 10), a modifier of patatin-like phospholipase domain-containing protein 3 (pnpla3), exhibits a geometric mean EC50 of 4.9 nM.

NPD10084 is an inhibitor of pyruvate kinase PKM2 that blocks non-glycolytic signaling in cancer cells by disrupting PKM2's interaction with β-catenin or STAT3, thus inhibiting downstream pathways. It demonstrates antiproliferative effects against colorectal cancer cells both in vitro and in vivo [1].

DS44470011 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) with oral bioavailability. It enhances the release of erythropoietin (EPO) from cells and is utilized in research related to renal anemia.

Falecalcitriol is an analog of calcitriol. It has a higher potency both in vivo and in vitro systems, which is longer duration of action in vivo.

ABT-046 is an orally active, selective, and highly efficient Diacylglycerol Acyltransferase 1 (DGAT-1) inhibitor that can be used in metabolic disease research.

ICMT-IN-55 (compound 31) acts as an ICMT inhibitor, exhibiting an IC50 value of 90 nM [1].

DEL-I25 is an effective activator of GPX4 that protects cells from ferroptosis (iron-dependent cell death).

Compound LE-77, known as FXR/CES2 modulator 1, functions as a dual regulator that activates FXR and inhibits CES2. It effectively mitigates the intestinal toxicity of irinotecan.

Nampt-IN-15 (Example 3) is a Nampt inhibitor that exhibits cytotoxic effects on various cell lines, including BxPC-3, HepG2, L540cy, and MOLM-13. The respective IC50 values for these cell lines are 38.5 nM, 8 nM, 8.5 nM, and 7 nM.

MolPort-010-778-422 is a high-affinity inhibitor targeting the ACE2 receptor of the SARS-CoV-2 virus. It demonstrates remarkable antiviral activity with an IC50 of 8.9 nM and holds promise for use in studies related to SARS-CoV-2.

4-Acetylphenylboronic acid acts as an effective inhibitor targeting carbonic anhydrase II (CAII), displaying inhibitory concentrations (IC50) of 246 μM for bovine CAII (bCA II) and 281.40 μM for human CAII (hCA II).