Antibodies
Dorsomorphin 2HCl
- 貨號 Cat. No.
- S7306
- 規格 Size
- 10mgã€50mg
- 品牌 Brand
- Selleckchem
Description
Dorsomorphin 2HCl
Catalog No.S7306
Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3.
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Biological Activity
| Description | Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. | |||||
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| Targets | AMPK | |||||
| IC50 | 109 nM [1] | |||||
| In vitro | Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformins effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] in addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. [3] | |||||
| In vivo | Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4] | |||||
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Protocol(Only for Reference)
Kinase Assay: [1]
| AMPK partial purification and in vitro kinase assay. | Liver AMPK is partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture contains 100 μM AMP, 100 μM ATP (0.5 μCi 33P-ATP per reaction), and 50 μM SAMS in a buffer (40 mM HEPES, pH 7.0, 80 mM NaCl, 0.8 mM EDTA, 5 mM MgCl2, 0.025% BSA, and 0.8 mM DTT). The reaction is initiated with addition of the enzyme. After 30-minute incubation at 30°C, the reaction is stopped by addition of 80 μl 1% H3PO4. Aliquots (100 μl) are transferred to 96-well MultiScreen plates. The plate is washed three times with 1% H3PO4 followed by detection in a Top-count. The in vitro AMPK inhibition data obtained with compound C — (6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo[1,5-a] pyrimidine — are fit to the following equation for competitive inhibition by nonlinear regression using a least-squares Marquardt algorithm in a computer program written by N. Thornberry of Merck Research Laboratories: Vi/Vo = (Km + S)/[S + Km × (1 + I/Ki)], where Vi is the inhibited velocity, Vo is the initial velocity, S is the substrate (ATP) concentration, Km is the Michaelis constant for ATP, I is the inhibitor (compound C) concentration, and Ki is the dissociation constant for compound C. |
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Animal Study: [3]
| Animal Models | Iron-replete mice |
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| Dosages | ~10 mg/kg |
| Administration | i.v. |
| Solubility | 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL |
References
Chemical Information
Download Dorsomorphin 2HCl SDF
| Molecular Weight (MW) | 472.41 |
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| Formula | C24H25N5O.2HCl |
| CAS No. | 1219168-18-9 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | BML-275,Compound C |
| Solubility (25°C) * | In vitro | DMSO | <1 mg/mL (<1 mM) |
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| Water | 94 mg/mL (198 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 1% DMSO/30% polyethylene glycol/1% Tween 80, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 6-[4-[2-(1-Piperidinyl)ethoxy]pheny​l]-3-(4-pyridinyl)-pyrazolo[1,5-a]pyrimidine dihydrochloride |
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