BAY-3827
目录号 : KP12714 CAS No. : 2377576-35-5

BAY-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。

规格 价格 是否有货 数量
5mg
¥1380.00
In-stock
10mg
¥2180.00
In-stock
25mg
¥4150.00
In-stock
50mg
¥6780.00
In-stock

Other Forms of Rapamycin:

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生物活性

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.

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)

体外研究

BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC50 values of 1.4 nM and 15 nM, respectively, under low (10 μM) and high (2 mM) ATP conditions. BAY-3827 (0-200 μM) inhibited the activity of Aurora A, Flt3, c-Met, and Rsk4 under 10 μM ATP conditions, with IC50 values of 1324 nM, 124 nM, 788 nM, and 36 nM, respectively. BAY-3827 (overnight) significantly reduced the phosphorylation of ACC1 Ser79 in LNCaP and VCaP cells, with weaker effects in IMR-32 and Colo320 cells [1].
BAY-3827 (0-10 nM; 6 days) showed significant inhibitory effects on LNCaP and VCaP cells [1].
BAY-3827 (1 and 5 μM; Inhibiting LIPE gene expression at 24 and 48 hours, reducing the expression of serine/threonine kinase AKT3, and blocking the expression of several genes in the mitochondrial carnitine palmitoyltransferase (CPT) family involved in acylcarnitine formation in VCaP cells [1].
BAY-3827 (5 μM; 2-4 days) significantly increased lipid droplet formation in VCaP cells compared to androgen treatment alone [1].

 

Cell Proliferation Assay

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.
分子式
C27H25FN6O
分子量
468.53
CAS号
2377576-35-5
中文名称
BAY-3827
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, protect from light

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

溶解性数据
In Vitro: 

DMSO: 25 mg/mL (53.36 mM; ultrasonic and warming and heat to 60°C)

配制储备液
                                           
浓度 溶剂体积 质量 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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

[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.

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