BAY-3827

SKU: orb1744239

Description

BAY-3827 is a selective AMPK inhibitor that blocks acetyl-CoA carboxylase 1 phosphorylation. It demonstrates antiproliferative effects in vitro and shows potential antitumor activity in vivo, specifically in androgen-dependent prostate cancer models, making it a valuable research tool for oncology and metabolic studies.

Research Area

Epigenetics & Chromatin, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 2377576-35-5
• MW: 468.53
• Purity: 99.90% (May vary between batches)
• Formula: C₂₇H₂₅FN₆O
• SMILES: C(#N)C=1C(C(C#N)=C(C)N(C)C1C)C=2C=C3C(=C(C)C2F)NN=C3NC(=O)C4=C(CC)C=CC=C4
• Target: Acyltransferase,AMPK
• Solubility: DMSO:29.44 mg/mL (62.83 mM)

Bioactivity

• Target IC50:
  c-Met:788 nM|Rsk4:36 nM|AMPK,10 µM ATP:1.4 nM|Flt3:124 nM|Aurora A:1324 nM|AMPK, 2 mM ATP:15 nM
• In Vitro:
  BAY-3827, in the concentration range of 0-200 μM, inhibits AMPK kinase activity with IC50 values of 1.4 nM at low ATP concentration (10 µM) and 15 nM at high ATP concentration (2 mM).In the concentration range of 0-200 μM, BAY-3827 inhibits Aurora A, Flt3, c-Met, and Rsk4 with IC50 values of 1324, 124, 788, and 36 nM, respectively, at 10 µM ATP concentration.After overnight treatment, BAY-3827 strongly reduces ACC1 Ser79 phosphorylation in LNCaP and VCaP cells, with a lesser extent in IMR-32 and especially in Colo320 cells.At concentrations of 0-10 nM over 6 days, BAY-3827 exhibits strong inhibitory effects on LNCaP and VCaP cells.At concentrations of 1 and 5 μM over 24 and 48 hours, BAY-3827 represses LIPE gene expression, reduces serine/threonine kinase AKT3, and blocks the expression of several genes from the mitochondrial carnitine palmitoyltransferase (CPT) family, which is involved in acyl carnitine formation in VCaP cells. At a concentration of 5 μM over 2-4 days, BAY-3827 significantly increases the formation of lipid droplets compared to androgen treatment only.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMPK, acyl-CoA oxidase-1

Compound Identifiers

PubChem CID

134817183