Dorsomorphin 2HCl, IC-02113615
Product Introduction
AMP-activated protein kinase (AMPK) is a central regulator of cellular energy homeostasis and metabolism, implicated in diabetes, inflammation, and cancer. Dorsomorphin dihydrochloride is a potent, reversible, and selective AMPK inhibitor (Ki = 109 nM in cell-free assays). In hepatocytes, dorsomorphin (5-10 ¦ÌM) blocks AICAR-induced AMPK activation and ACC phosphorylation, thereby inhibiting fatty acid oxidation and lipogenic gene expression. In HT-29 cells, dorsomorphin (10 ¦ÌM) completely suppresses AMPK-dependent autophagic proteolysis. In vivo, dorsomorphin (10 mg/kg, i.p.) reduces basal hepcidin expression and elevates serum iron in mice. Additionally, dorsomorphin inhibits BMP type I receptors (ALK2, ALK3, ALK6) and blocks SMAD1/5/8 phosphorylation. Note: The compound also inhibits VEGFR2 (Flk1/KDR) and disrupts angiogenesis at higher concentrations.
Product Features
1. Potent AMPK Inhibitor: Selective and reversible inhibition of AMP-activated protein kinase with Ki of 109 nM in cell-free assays.
2. Dual BMP Receptor Antagonism: Inhibits BMP type I receptors (ALK2, ALK3, ALK6) and blocks SMAD1/5/8 phosphorylation.
3. Metabolic Regulation: Suppresses fatty acid oxidation and lipogenic gene expression in hepatocytes.
4. Autophagy Inhibition: Completely blocks AMPK-dependent autophagic proteolysis in cellular models.
5. In Vivo Activity: Effectively reduces hepcidin expression and modulates iron homeostasis in mouse models.
Specifications
Size: Available in 10 mg, 25 mg, and 50 mg
CAS Number: 1219168-18-9
Molecular Weight: 472.41
Molecular Formula: C24H27Cl2N5O
Purity: ¡Ý99%
Solubility: DMSO: 5 mg/mL
Storage and Stability
Storage Conditions: Store at -80¡ãC for up to 2 years or -20¡ãC for up to 1 year in solvent. Protect from light.
Shelf Life: The product is stable as indicated when stored under recommended conditions. Avoid repeated freeze-thaw cycles.
Protocol (For Reference Only)
Important: Protect compound from light during handling and storage. Prepare stock solutions in DMSO and aliquot to avoid repeated freeze-thaw cycles.
1. Stock Solution Preparation: Dissolve Dorsomorphin 2HCl in DMSO to prepare a concentrated stock solution (e.g., 5-50 mM), aliquot into single-use volumes, and store at -20¡ãC or -80¡ãC protected from light.
2. Working Solution Preparation: Immediately before use, dilute the DMSO stock solution into aqueous buffer or culture medium to the desired final concentration; typical working concentrations range from 1-20 ¦ÌM depending on cell type and experimental endpoint.
3. Cellular Treatment: Add the working solution to cultured cells and incubate for the desired duration; for AMPK inhibition studies, a 30-60 minute pretreatment before AMPK activation is recommended.
4. In Vivo Administration: For animal studies, prepare compound in an appropriate vehicle; typical doses range from 10-30 mg/kg via intraperitoneal or intravenous injection.
5. Analysis: Monitor AMPK phosphorylation status by Western blotting, assess metabolic parameters, or evaluate downstream signaling pathways including ACC phosphorylation and autophagy markers.
Precautions
1. Protect from light during handling and storage to prevent compound degradation.
2. Prepare fresh working solutions daily as the compound may lose activity upon prolonged storage in aqueous buffers.
3. Use appropriate vehicle controls in all experiments as DMSO concentrations above 0.1% may affect cellular responses.
4. Dorsomorphin exhibits off-target effects on BMP receptors and VEGFR2 at higher concentrations; confirm target specificity using appropriate controls and alternative inhibitors.
5. For research use only. Not for use in diagnostic or therapeutic procedures.
FAQ (Simplified)
Q1: What is the recommended starting concentration for in vitro studies?
A1: For AMPK inhibition in hepatocytes and most cell lines, 5-10 ¦ÌM is an effective starting concentration. Titration experiments are recommended to determine the optimal concentration for specific cell types and endpoints.
Q2: How should I store the compound after reconstitution?
A2: Prepare concentrated stock solutions in DMSO, aliquot into single-use volumes, and store at -20¡ãC for short-term use (up to 1 month) or -80¡ãC for long-term storage (up to 2 years). Protect from light at all times.
Q3: Does Dorsomorphin affect other signaling pathways?
A3: Yes. At concentrations above 10 ¦ÌM, Dorsomorphin also inhibits BMP type I receptors (ALK2/3/6) and VEGFR2. Include appropriate controls and consider using more selective AMPK inhibitors if off-target effects are a concern.
Q4: Can Dorsomorphin be used in vivo?
A4: Yes. Intraperitoneal administration at 10-30 mg/kg has been shown to effectively reduce hepcidin expression and modulate iron metabolism in mouse models. Optimize dosing and vehicle based on specific experimental requirements.
Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions using a small-scale pilot experiment is strongly recommended before processing valuable samples.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages, including loss of samples or data.
4. Wear appropriate protective clothing and gloves when handling this product.
Ordering Information
Catalog Number: IC-02113615
Product Name: Dorsomorphin 2HCl
Size: 10 mg / 25 mg / 50 mg
Price:
10 mg: CNY ¥1350.00 / USD $135.00 / EUR €162.00 / JPY ¥24300.00
25 mg: CNY ¥2450.00 / USD $245.00 / EUR €294.00 / JPY ¥44100.00
50 mg: CNY ¥4300.00 / USD $430.00 / EUR €516.00 / JPY ¥77400.00
2023 Version
