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この商品について
実験式(ヒル表記法):
C24H25N5O
CAS番号:
分子量:
399.49
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
製品名
AMPK Inhibitor, Compound C, AMPK Inhibitor, Compound C, CAS 866405-64-3, is a cell-permeable compound that inhibits KDR/VEGFR2, ALK2/BMPR-I, and AMPK kinase activities (IC50 = 25.1, 148, and 234.6 nM, respectively).
SMILES string
[n]21ncc(c2ncc(c1)c4ccc(cc4)OCCN5CCCCC5)c3ccncc3
InChI
1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2
InChI key
XHBVYDAKJHETMP-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light yellow
solubility
2% HCl: 10 mg/mL
2% acetic acid: 10 mg/mL
methanol: 3 mg/mL
DMSO: 4 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
EC100 = 2.5 µM against BMP pathway-dependent dorsoventral development; EC50 = 5 µM against VEGF signaling-dependent intersomitic vessel formation in zebrafish embryo in vivo
Primary Target
AMPK
AMPK
Product competes with ATP.
Reversible: yes
Target IC50: 25.1, 148, and 234.6 nM, against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity, respectively
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC50 = 25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFβR-I, ZAPK, Syk, PKCθ, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC100 = 2.5 µM) and VEGF signaling-dependent intersomitic vessel formation (EC50 = 5 µM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR (Cat. No. 123040) and/or Metformin (Cat. No. 317240) for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo. Also available as a 10 mM solution in DMSO (Cat. No. 171261).
Other Notes
Hao, J., et al. 2010. ACS Chem.Biol.5, 245.
Yu, P.B., et al. 2008. Nat. Chem. Biol4, 33.
Kim, E.K., et al. 2004. J. Biol. Chem.279, 19970.
Lee, M., et al. 2003. J. Biol. Chem.278, 39653.
Inoki, K., et al. 2003. Cell115, 577.
Fryer, L.G., 2002. FEBS Lett.531, 189.
Zhou, G., et al. 2001. J. Clin. Invest.108, 1167.
Yu, P.B., et al. 2008. Nat. Chem. Biol4, 33.
Kim, E.K., et al. 2004. J. Biol. Chem.279, 19970.
Lee, M., et al. 2003. J. Biol. Chem.278, 39653.
Inoki, K., et al. 2003. Cell115, 577.
Fryer, L.G., 2002. FEBS Lett.531, 189.
Zhou, G., et al. 2001. J. Clin. Invest.108, 1167.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
保管分類
11 - Combustible Solids
wgk
WGK 3
試験成績書(COA)
製品のロット番号・バッチ番号を入力して、試験成績書(COA) を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Xi Mei et al.
Behavioural brain research, 379, 112344-112344 (2019-11-11)
The pathogenesis of postoperative cognitive impairment of obstructive sleep apnea-hypopnea syndrome (OSAHS) individuals remains unclear. AMP activated protein kinase (AMPK) is a ubiquitous sensor/effector of cell stresses. Thus we detected the role and underlying mechanisms of AMPK in postoperative cognitive
Mohamadreza Savaee et al.
Reports of biochemistry & molecular biology, 11(1), 157-165 (2022-06-30)
Prostate cancer is known as one of the most prevalent health disorders in the male population globally. The aim of the current study was to evaluate the effects of separate and concomitant use of MK-2206 and salinomycin on prostate cancer
Charles B Trelford et al.
Frontiers in cell and developmental biology, 9, 712124-712124 (2021-11-12)
The mechanism(s) in which transforming growth factor beta 1 (TGFβ) modulates autophagy in cancer remain unclear. Here, we characterized the TGFβ signaling pathways that induce autophagy in non-small cell lung cancer cells, using cells lines stably expressing GFP-LC3-RFP-LC3ΔG constructs that
Mahesh Pandit et al.
Experimental & molecular medicine, 54(8), 1214-1224 (2022-08-24)
Allergic inflammation is a T helper 2 (Th2) cell-driven pathophysiological phenomenon, but the mechanism by which the metabolic cascade affects Th2 cell differentiation remains unclear. In this study, we investigated the roles of AMP-activated protein kinase (AMPK) and intracellular energy
Jumi Kim et al.
Microorganisms, 10(3) (2022-03-27)
Ca2+/calmodulin-dependent protein kinase II (CaMKII), which is involved in the calcium signaling pathway, is an important regulator of cancer cell proliferation, motility, growth, and metastasis. The effects of CaMKII on hepatitis B virus (HBV) replication have never been evaluated. Here
グローバルトレードアイテム番号
| カタログ番号 | GTIN |
|---|---|
| 171260-5MGCN | 04055977207163 |
| 171260-1MGCN | 04055977207149 |
| 171260-10MGCN | 04055977207156 |
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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