A3051, is a robust and orally active inhibitor of CXXC5-DVL with an IC 50 of 63.06 nM. Its applications include research into phenotypes associated with obesity, diabetes, and NASH that are induced by high fat diet (HFD) and methionine-choline deficient diet (MCD).

CXXC5-DVL:63.06 nM (IC50)

A3334, at concentrations ranging from 1-10 μM, effectively suppresses the adipogenic differentiation of 3T3-L1 preadipocytes through the Wnt/β-catenin signaling pathway[1]. Additionally, in a 24-hour treatment, A3334 (1-10 μM) increases TOPFlash reporter activity in HEK293-TOP cells[1].

Administering A3334 (25 mg/kg; p.o. once daily) demonstrates significant anti-obesity effects in HFD-fed mice without impacting those on a normal diet, over a period of 16 weeks[1]. Additionally, a 5-day course of the same dosage notably decreases fasting glucose, glucose tolerance (GTT), and insulin tolerance (ITT) in serum[1]. A 3-week regimen eradicates hepatosteatosis and reduces elevated alanine transaminase (ALT) and aspartate transaminase (AST) levels[1]. In a study involving 6-week-old male C57BL/6N mice fed a high-fat diet (HFD) for 16 weeks, the intervention did not result in expected HFD-induced body weight gain and abdominal obesity. It also lowered triglyceride and total cholesterol levels while increasing HDL-cholesterol levels, mitigated adipocyte cell size growth, and suppressed inflammation[1].