Dorsomorphin dihydrochloride

Biological Activity

Dorsomorphin (BML-275; Compound C) dihydrochloride is a potent inhibitor of AMP-activated protein kinase (AMPK) (Ki = 109 nM) and bone morphogenic protein (BMP) signaling. Dorsomorphin dihydrochloride inhibits AMPK activation induced by AICAR and metformin. Dorsomorphin dihydrochloride also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), BMPR-IA (ALK3), and BMPR-IB (ALK6). Dorsomorphin dihydrochloride induces autophagy in cancer cell lines via a mechanism independent of AMPK inhibition. Dorsomorphin dihydrochloride induces autophagy.

Product Citations

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  Biomed Pharmacother. 2024 May 23;176:116760.

  Identification of a novel hypoglycemic small molecule, trans-2, 4-dimethoxystilbene by rectifying gut microbiota and activating hepatic AMPKα-PPARγ pathway through gut-liver axis
  Dorsomorphin dihydrochloride purchased from AbMole

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  Int J Mol Sci. 2023 Jan 5;24(2):1070.

  Sulforaphane Suppresses H2O2-Induced Oxidative Stress and Apoptosis via the Activation of AMPK/NFE2L2 Signaling Pathway in Goat Mammary Epithelial Cells
  Dorsomorphin dihydrochloride purchased from AbMole

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  PLoS One. 2023 Dec 1;18(12):e0294566.

  Silencing of topical proline hydroxylase domain 2 promotes the healing of rat diabetic wounds by phosphorylating AMPK
  Dorsomorphin dihydrochloride purchased from AbMole

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  J Appl Toxicol. 2023 Feb 27.

  AMP‐activated protein kinase‐farnesoid X receptor pathway contributes to oleanolic acid‐induced liver injury
  Dorsomorphin dihydrochloride purchased from AbMole

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  Italian Journal of Food Science. 2023 Apr 17;35 (2): 13–21.

  Pretreatment of kaempferol-3-O-rutinoside protects H9c2 cells against LPS-induced inflammation through the AMPK/SIRT1 pathway
  Dorsomorphin dihydrochloride purchased from AbMole

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  Adv Sci (Weinh). 2022 Nov 22;10(1):e2204463.

  Genetic and Pharmacological Inhibition of Astrocytic Mysm1 Alleviates Depressive-Like Disorders by Promoting ATP Production
  Dorsomorphin dihydrochloride purchased from AbMole

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  Int J Biol Sci. 2022 Jan 31;18(4):1594-1611.

  Atractylenolide III ameliorates Non-Alcoholic Fatty Liver Disease by activating Hepatic Adiponectin Receptor 1-Mediated AMPK Pathway
  Dorsomorphin dihydrochloride purchased from AbMole

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  J Food Biochem. 2022 Aug 5;e14351.

  Liquiritin inhibits H2O2-induced oxidative stress injury in H9c2 cells via the AMPK/SIRT1/NF-κB signaling pathway
  Dorsomorphin dihydrochloride purchased from AbMole

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  Acta Histochem. 2022 Aug;124(6):151931.

  Fibroblast-derived exosomal miRNA-133 promotes cardiomyocyte-like differentiation
  Dorsomorphin dihydrochloride purchased from AbMole

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  Indian J Pharm Sci. 2022;2022:84(3)284-293.

  Gallic acid Inhibits M1 Macrophage Polarization via Adenosine 5'-Monophosphate-Activated Protein Kinase/Signal Transducers and Activators of
  Dorsomorphin dihydrochloride purchased from AbMole

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  Front Pharmacol. 2021 May 17;12:589273.

  Dapagliflozin Alleviates Hepatic Steatosis by Restoring Autophagy via the AMPK-mTOR Pathway
  Dorsomorphin dihydrochloride purchased from AbMole

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  J Cell Physiol. 2021 Mar;236(3):1889-1902.

  Icariin ameliorates endothelial dysfunction in type 1 diabetic rats by suppressing ER stress via the PPARα/Sirt1/AMPKα pathway
  Dorsomorphin dihydrochloride purchased from AbMole

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  Front Oncol. 2021 Jan 29;10:614067.

  Solasonine Suppresses the Proliferation of Acute Monocytic Leukemia Through the Activation of the AMPK/FOXO3A Axis
  Dorsomorphin dihydrochloride purchased from AbMole

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  BMC Cancer. 2021 Feb 25;21(1):195.

  Blockage of AMPK-ULK1 pathway mediated autophagy promotes cell apoptosis to increase doxorubicin sensitivity in breast cancer (BC) cells: an in vitro study
  Dorsomorphin dihydrochloride purchased from AbMole

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  Cell Physiol Biochem. 2018;50(6):2341-2364.

  Peperomin E Induces Promoter Hypomethylation of Metastatic-Suppressor Genes and Attenuates Metastasis in Poorly Differentiated Gastric Cancer.
  Dorsomorphin dihydrochloride purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Hum Mol Genet (2016). Figure 2. Dorsomorphin dihydrochloride
	Method	RT-qPCR
	Cell Lines	iPSC lines
	Concentrations	1 μM
	Incubation Time	72 h
	Results	We generated cortical neurons using a well-established protocol with small molecule dual SMAD inhibition for neural induction followed by plating of neuroepithelial cells for final differentiation

Protocol (for reference only)

Cell Experiment
Cell lines	Spermatogonial Cell
Preparation method	Dorsomorphin was added to the medium at a final concentration of 0, 1, 2, 4, or 8 µM (in final 0.4% dimethyl sulfoxide). The cells were maintained at 28.5°C in an atmosphere of 3% carbon dioxide and the medium was replaced every 3–4 days.
Concentrations	0, 1, 2, 4, or 8 µM
Incubation time	3 weeks

Animal Experiment
Animal models	C57BL/6 mice
Formulation	DMSO
Dosages	10 mg/kg
Administration	i.p.

Chemical Information

Molecular Weight	472.41
Formula	C24H25N5O.2HCl
CAS Number	1219168-18-9
Solubility (25°C)	Water 45 mg/mL DMSO 5 mg/mL (Need ultrasonic)
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

References

[1] Wong TT, et al. PLoS One. Dorsomorphin promotes survival and germline competence of zebrafish spermatogonial stem cells in culture.

[2] Hyeon Ung Park, et al. Mol Cancer Ther. AMP-activated protein kinase promotes human prostate cancer cell growth and survival

[3] Yu PB, et al. Nat Chem Biol. Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.