BAY-3827
目录号 : GC67772BAY-3827 是强效的、选择性的 AMPK 抑制剂，IC50 值为 1.4 nM (10 µM ATP) 和 15 nM (2 mM ATP)。BAY-3827 对其他 331 种被测激酶的选择性超过 500 倍相比于 AMPK。AMPK 抑制乙酰 CoA 羧化酶 1 的磷酸化，并在雄激素依赖的前列腺癌细胞株中显示出强效的抗增殖活性。
Cas No.:2377576-35-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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]
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].
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].
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. |
[1]. Lemos C, et al. The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models. Cell Oncol (Dordr). 2021 Jun;44(3):581-594.
| Cas No. | 2377576-35-5 | SDF | Download SDF |
| 分子式 | C27H25FN6O | 分子量 | 468.53 |
| 溶解度 | DMSO : 25 mg/mL (53.36 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | 4°C, protect from light |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.2134 mL | 1.0672 mL | 2.1343 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models
Cell Oncol (Dordr) 2021 Jun;44(3):581-594.PMID:33492659DOI:10.1007/s13402-020-00584-8
Purpose: 5' adenosine monophosphate-activated kinase (AMPK) is an essential regulator of cellular energy homeostasis and has been associated with different pathologies, including cancer. Precisely defining the biological role of AMPK necessitates the availability of a potent and selective inhibitor. Methods: High-throughput screening and chemical optimization were performed to identify a novel AMPK inhibitor. Cell proliferation and mechanistic assays, as well as gene expression analysis and chromatin immunoprecipitation were used to investigate the cellular impact as well as the crosstalk between lipid metabolism and androgen signaling in prostate cancer models. Also, fatty acid turnover was determined by examining lipid droplet formation. Results: We identified BAY-3827 as a novel and potent AMPK inhibitor with additional activity against ribosomal 6 kinase (RSK) family members. It displays strong anti-proliferative effects in androgen-dependent prostate cancer cell lines. Analysis of genes involved in AMPK signaling revealed that the expression of those encoding 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMGCR), fatty acid synthase (FASN) and 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 2 (PFKFB2), all of which are involved in lipid metabolism, was strongly upregulated by androgen in responsive models. Chromatin immunoprecipitation DNA-sequencing (ChIP-seq) analysis identified several androgen receptor (AR) binding peaks in the HMGCR and PFKFB2 genes. BAY-3827 strongly down-regulated the expression of lipase E (LIPE), cAMP-dependent protein kinase type II-beta regulatory subunit (PRKAR2B) and serine-threonine kinase AKT3 in responsive prostate cancer cell lines. Also, the expression of members of the carnitine palmitoyl-transferase 1 (CPT1) family was inhibited by BAY-3827, and this was paralleled by impaired lipid flux. Conclusions: The availability of the potent inhibitor BAY-3827 will contribute to a better understanding of the role of AMPK signaling in cancer, especially in prostate cancer.