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Dorsomorphin dihydrochloride

Catalog No. T6146   CAS 1219168-18-9
Synonyms: BML-275 2HCl, Compound C dihydrochloride, Dorsomorphin (Compound C) 2HCl, Compound C 2HCl, BML-275 dihydrochloride

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Dorsomorphin dihydrochloride Chemical Structure
Dorsomorphin dihydrochloride, CAS 1219168-18-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 64.00
25 mg In stock $ 137.00
50 mg In stock $ 247.00
100 mg In stock $ 447.00
500 mg In stock $ 987.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.89%
Purity: 98.89%
Purity: 98.72%
Purity: 97.74%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.
Targets&IC50 AMPK:109 nM (cell free)
In vitro Dorsomorphin (compound C) is a potent reversible inhibitor that is competitive with ATP, with Ki = 109 ± 16 nM in the absence of AMP. Incubation of cultured hepatocytes with compound C inhibited ACC inactivation by either AICAR or metformin [1]. Compound C suppressed 2-deoxy-D-glucose (2DG)-induced GRP78 promoter activity in a dose-dependent manner but had little effect on tunicamycin-induced GRP78 promoter activity. Compound C also suppressed GRP78 promoter activity induced by glucose withdrawal [2].
In vivo 6 h after dorsomorphin was administered intravenously, hepatic hepcidin mRNA levels were reduced to one-third of that of vehicle-injected mice. Alterations in hepcidin levels affect serum iron concentrations within 24 h via the altered mobilization of intracellular iron by ferroportin33. Administration of dorsomorphin over 24 h led to a 60% increase in total serum iron concentrations [3].
Kinase Assay Liver AMPK was partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture contained 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 was initiated with the addition of the enzyme. After a 30-minute incubation at 30°C, the reaction was stopped by addition of 80 μl 1% H3PO4. Aliquots (100 μl) were transferred to 96-well MultiScreen plates. The plate was 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 — were 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 [1].
Cell Research C2C12 cells were seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. Wells were treated in quadruplicate with BMP ligands and dorsomorphin or vehicle. Cells were harvested after 5 d in culture with 50 μl Tris-buffered saline, 1% Triton X-100. Lysates were added to p-nitro-phenylphosphate reagent in 96-well plates for 1 h, and alkaline phosphatase activity expressed as absorbance at 405 nM. Cell viability and quantity were measured by Cell-titer Glo and binding of nuclear dye CyQuant, respectively, using replicate wells treated identically to those used for alkaline phosphatase measurements [3].
Animal Research 12-week-old C57BL/6 mice raised on a standard diet were injected via the tail vein with 0.2 g kg?1 of dextran (average MW = 5,000) or 0.2 g kg?1 of iron-dextran USP. Dextran was injected with vehicle only, whereas iron-dextran was injected with either vehicle or dorsomorphin (10 mg/kg). 1 h after injection, mice were killed and liver segments were collected in 500 μl of SDS-lysis buffer and mechanically homogenized. 20 μl of liver extracts were resolved by SDS-PAGE and immunoblotted. Total RNA was harvested using Trizol from mechanically homogenized mouse livers (6 h after injection with a single intraperitoneal dose of dorsomorphin (10 mg/kg) or DMSO) [3].
Synonyms BML-275 2HCl, Compound C dihydrochloride, Dorsomorphin (Compound C) 2HCl, Compound C 2HCl, BML-275 dihydrochloride
Molecular Weight 472.41
Formula C24H25N5O·2HCl
CAS No. 1219168-18-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mM, with gentle warming

H2O: 47.2 mg/mL (100 mM)

TargetMolReferences and Literature

1. Zhou G, et al. Role of AMP-activated protein kinase in mechanism of metformin action. J Clin Invest. 2001 Oct;108(8):1167-74. 2. Saito S, et al. Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent of AMPK and BMP signaling. PLoS One. 2012;7(9):e45845. 3. Yu PB, et al. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. Nat Chem Biol. 2008 Jan;4(1):33-41. 5. Fan C, Feng J, Tang C, et al. Melatonin suppresses ER stress-dependent proapoptotic effects via AMPK in bone mesenchymal stem cells during mitochondrial oxidative damage[J]. Stem Cell Research & Therapy. 2020, 11(1): 1-22.

TargetMolCitations

1. Xu J, Ao Y L, Huang C, et al. Harmol promotes α-synuclein degradation and improves motor impairment in Parkinson’s models via regulating autophagy-lysosome pathway. npj Parkinson's Disease. 2022, 8(1): 1-12. 2. Fan C, Feng J, Tang C, et al. Melatonin suppresses ER stress-dependent proapoptotic effects via AMPK in bone mesenchymal stem cells during mitochondrial oxidative damage. Stem Cell Research & Therapy. 2020, 11(1): 1-22 3. Qiu W Q, Pan R, Tang Y, et al. Lychee seed polyphenol inhibits Aβ-induced activation of NLRP3 inflammasome via the LRP1/AMPK mediated autophagy induction. Biomedicine & Pharmacotherapy. 2020, 130: 110575. 4. Cao P, Wang Y, Zhang C, et al.Quercetin ameliorates non-alcoholic fatty liver disease (NAFLD) via the promotion of AMPK-mediated hepatic mitophagy.The Journal of Nutritional Biochemistry.2023: 109414.

Related compound libraries

This product is contained In the following compound libraries:
TGF-beta/Smad Compound Library NO PAINS Compound Library Glycolysis Compound Library Anti-Colorectal Cancer Compound Library Anti-Obesity Compound Library Oxidation-Reduction Compound Library Anti-Fibrosis Compound Library Anti-Diabetic Compound Library Stem Cell Differentiation Compound Library Neuronal Differentiation Compound Library

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Keywords

Dorsomorphin dihydrochloride 1219168-18-9 Autophagy Chromatin/Epigenetic PI3K/Akt/mTOR signaling Stem Cells AMPK TGF-beta/Smad Dorsomorphin (Compound C) Compound C BML 275 BML275 Dihydrochloride Dorsomorphin BMP TGF-β Receptor Compound C Dihydrochloride Dorsomorphin Dihydrochloride inhibit BML-275 2HCl BML-275 Dihydrochloride Compound C dihydrochloride type ATP-competitive BML 275 Dihydrochloride Dorsomorphin (Compound C) 2HCl Transforming growth factor beta receptors receptors Compound C 2HCl BML-275 dihydrochloride pathway BML-275 AMP-activated protein kinase Inhibitor BML275 inhibitor

 

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