171261

Dorsomorphin

≥95% (HPLC), liquid, AMPK inhibitor, Calbiochem

• Synonim(y): Dorsomorfina, inhibitor AMPK I, inhibitor BMP I, Inhibitor AMPK InSolution, związek C
• Wzór empiryczny (zapis Hilla): C₂₄H₂₅N₅O
• Numer CAS: 866405-64-3
• Masa cząsteczkowa: 399.49
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD08705402
• Assay: ≥95% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Właściwości

• Nazwa produktu: Inhibitor AMPK, związek C, InSolution, ≥95%, 10 mM, AMPK Inhibitor
• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, desiccated (hygroscopic), protect from light
• shipped in: wet ice
• storage temp.: 2-8°C
• 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

Opis

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.

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

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

Packaging

Packaged under inert gas

Physical form

Supplied as a 10 mM (1 mg/250 µl) solution of AMPK Inhibitor, Compound C (Cat. No. 171260) in DMSO.

Preparation Note

Following initial use, aliquot and freeze (-20°C). Once opened, stock solutions are stable for up to 3 months at -20°C.

Other Notes

Hao, J., et al. 2010. ACS Chem.Biol.5, 245.
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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Irritant (B)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 10 - Combustible liquids
• wgk: WGK 2
• flash_point_f: 188.6 °F - closed cup - (Dimethylsulfoxide)
• flash_point_c: 87 °C - closed cup - (Dimethylsulfoxide)