2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. BAY-3827

BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines.

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BAY-3827 Chemical Structure

BAY-3827 Chemical Structure

CAS No. : 2377576-35-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 155 In-stock
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10 mM * 1 mL in DMSO USD 155 In-stock
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10 mg USD 240 In-stock
25 mg USD 450 In-stock
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Based on 2 publication(s) in Google Scholar

BAY-3827 Related Antibodies

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View All AMPK Isoform Specific Products:

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

  • Biological Activity

  • Purity & Documentation

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Description

BAY-3827 is a potent and selective AMPK inhibitor with IC50 values of 1.4 nM at low (10 µM ATP concentration) and 15 nM at high (2 mM ATP concentration). BAY-3827 shows over 500-fold selectivity for most of the 331 kinases. BAY-3827 prevents phosphorylation of acetyl-CoA carboxylase 1 and shows strongest anti-proliferative activity in androgen-dependent prostate cancer cell lines[1].

IC50 & Target

IC50: 1.4 nM (AMPK kinase,10 µM ATP), 15 nM (AMPK kinase, 2 mM ATP), 1324 nM (Aurora A), 124 nM (Flt3), 788 nM (c-Met), 36 nM (Rsk4)[1]
In Vitro

BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC50 values of 1.4 nM at low, 10 µM ATP concentration and 15 nM at high, 2 mM ATP concentration[1].
BAY-3827 (0-200 μM) inhibits Aurora A, Flt3, c-Met and Rsk4 with IC50 values of 1324, 124, 788 and 36 nM , respectively with 10 µM ATP concentration[1].
BAY-3827 (overnight) strongly reduces ACC1 Ser79 phosphorylation in LNCaP and VCaP cells, and shows a lesser extent in IMR-32 and especially in Colo320 cells[1].
BAY-3827 (0-10 nM; 6 d) shows strong inhibitory effects to LNCaP and VCaP cells[1].
BAY-3827 (1 and 5 μM; 24 and 48 h) 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[1].
BAY-3827 (5 μM; 2-4 d) significantly increases the formation of lipid droplets in comparison to androgen treatment only[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BAY-3827 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: LNCaP, VCaP, 22Rv1, C4-2B, PC-3 and DU-145 prostate cancer cell lines
Concentration: 0-10 nM
Incubation Time: 6 d
Result: Showed strong inhibitory effects for LNCaP and VCaP cells, two prostate cancer cell lines with IC50 values of 0.28 and 1.71 nM, respectily. Inhibited proliferation of 22Rv1 cells with an IC50 value of 5.55 nM.
Molecular Weight

468.53

Formula

C27H25FN6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCC1=CC=CC=C1C(NC2=NNC3=C2C=C(C4C(C#N)=C(C)N(C)C(C)=C4C#N)C(F)=C3C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (53.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1343 mL 10.6717 mL 21.3434 mL
5 mM 0.4269 mL 2.1343 mL 4.2687 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 98.36%

COA (257 KB) HNMR (263 KB) LCMS (105 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1343 mL 10.6717 mL 21.3434 mL 53.3584 mL
5 mM 0.4269 mL 2.1343 mL 4.2687 mL 10.6717 mL
10 mM 0.2134 mL 1.0672 mL 2.1343 mL 5.3358 mL
15 mM 0.1423 mL 0.7114 mL 1.4229 mL 3.5572 mL
20 mM 0.1067 mL 0.5336 mL 1.0672 mL 2.6679 mL
25 mM 0.0854 mL 0.4269 mL 0.8537 mL 2.1343 mL
30 mM 0.0711 mL 0.3557 mL 0.7114 mL 1.7786 mL
40 mM 0.0534 mL 0.2668 mL 0.5336 mL 1.3340 mL
50 mM 0.0427 mL 0.2134 mL 0.4269 mL 1.0672 mL
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BAY-3827 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY-38272377576-35-5BAY3827BAY 3827AMPKAMP-activated protein kinaseATPAurora AFlt3c-MetRsk4phosphorylationLNCaPVCaPLIPEAKT3lipid dropletInhibitorinhibitorinhibit

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