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BAY-3827
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY-3827图片
CAS NO:2377576-35-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
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。
生物活性

BAY-3827 is a potent and selectiveAMPKinhibitor withIC50values 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 ofacetyl-CoA carboxylase1 and shows strongest anti-proliferative activity in androgen-dependent prostatecancercell 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]

体外研究
(In Vitro)

BAY-3827 (0-200 μM) inhibits AMPK kinase activity with IC50values 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 IC50values 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 IC50values of 0.28 and 1.71 nM, respectily. Inhibited proliferation of 22Rv1 cells with an IC50value of 5.55 nM.
分子量

468.53

性状

Solid

Formula

C27H25FN6O

CAS 号

2377576-35-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°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℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1343 mL10.6717 mL21.3434 mL
5 mM0.4269 mL2.1343 mL4.2687 mL
10 mM0.2134 mL1.0672 mL2.1343 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。