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Tocris/Dorsomorphin dihydrochloride/3093/10/10 mg

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货号: 3093/10

品牌: Tocris

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Description: Potent AMPK inhibitor

Alternative Names: Compound C, BML-275

Chemical Name: 6-[4-[2-(1-Piperidinyl)ethoxy]phenyl]-3-(4-pyridinyl)-pyrazolo[1,5-a]pyrimidine dihydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent inhibitor of AMP-activated protein kinase (AMPK) (K_i = 109 nM). Displays no significant activity on several structurally related kinases including ZAPK, SYK, PKCθ, PKA and JAK3. Inhibits AMPK activation induced by AICAR (Cat. No. 2840) and metformin (Cat. No. 2864). Also inhibits bone morphogenetic protein (BMP) type I receptors (ALK2, ALK3 and ALK6). Promotes cardiomyogenesis in mouse embryonic stem cells (ESCs) in vitro. Shown to induce autophagy in cancer cell lines via a mechanism independent of AMPK inhibition.

Compound Libraries

Dorsomorphin dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	472.41
Formula	C₂₄H₂₅N₅O.2HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	1219168-18-9
PubChem ID	49761481
InChI Key	RJDVIJJQKMGPMV-UHFFFAOYSA-N
Smiles	C(C=N2)(C4=CC=C(OCCN5CCCCC5)C=C4)=CN1C2=C(C3=CC=NC=C3)C=N1.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	9.45	20mM with gentle warming
	water	47.24	100

Preparing Stock Solutions

The following data is based on the product molecular weight 472.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.12 mL	10.58 mL	21.17 mL
5 mM	0.42 mL	2.12 mL	4.23 mL
10 mM	0.21 mL	1.06 mL	2.12 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Zhou et al (2001) Role of AMP-activated protein kinase in mechanism of metformin action. J.Clin.Invest. 108 1167 PMID: 11602624

Yu et al (2008) Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat.Chem.Biol. 4 33 PMID: 18026094

Vucicevic et al (2011) Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway. Autophagy 7 40 PMID: 20980833

Hao et al (2008) Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells. PLoS ONE 3 2904 PMID: 18682835

Diekmann et al (2015) A reliable and efficient protocol for human pluripotent stem cell differentiation into the definitive endoderm based on dispersed single cells. Stem Cells Dev. 24 190 PMID: 25137387

Keywords: Dorsomorphin dihydrochloride, supplier, Potent, AMPK, inhibitors, inhibits, BMP, type, I, receptor, ALK2, ALK3, ALK6, AMP-Activated, Protein, Kinases, Receptors, Activin, Receptor-like, Receptor, Serine/Threonine, RSTKs, stem, cells, BML275, 866405-64-3, Compound, C, BML-275, BMP, and, Other, Activin, Receptors, AMPK, Autophagy, Cardiomyocyte, Stem, Cells, ESCs, and, iPSC, AMPK, Tocris Bioscience

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