Dorsomorphin (Compound C)

Dorsomorphin (Compound C)

Catalog Number:
L002370473APE
Mfr. No.:
APE-B3252
Price:
$180
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      • Overview
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          Background

          Dorsomorphin is a cell-permeable and reversible ATP-competitive inhibitor of AMP-activated protein kinase (AMPK) with Ki value of 109nM [1].
          Dorsomorphin is highly selective against AMPK over other structure related kinases such as protein kinase A, protein kinase C and Janus kinase 3. As an AMPK inhibitor, dorsomorphin is found to reverse the anti-proliferation induced by AMPK signaling in glucose-deprived mouse neural stem cells. It also shows inhibition of adipogenic differentiation in mouse 3T3-L1 fibroblasts [2].
          Dorsomorphin is also reported to be an inhibitor of BMP signaling. It inhibits the phosphorylation of Smad 1/5/8, resulting in a reduction of heterotopic ossification. It also decreases the gene transcription of hepatic hepcidin and leads to increased iron levels subsequently. Moreover, the inhibition of BMP caused by dorsomorphin promotes self-renewal and neural induction of human ESC [2]

          [1] Lu Y, Akinwumi BC, Shao Z, Anderson HD. Ligand Activation of Cannabinoid Receptors Attenuates Hypertrophy of Neonatal Rat Cardiomyocytes. J Cardiovasc Pharmacol. 2014 Jun 26.
          [2] Kudo T, Kanetaka H, Mizuno K, et al. Effects of the Small Molecule Dorsomorphin on Intracellular Signaling. Interface Oral Health Science 2011. Springer Japan, 2012: 131-133.

      • Properties
        • Alternative Name
          Compound C; 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine
          CAS Number
          866405-64-3
          Molecular Formula
          C24H25N5O
          Molecular Weight
          399.49
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥8.49 mg/mL in DMSO with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
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          2. Xiuyan Wang, Bin Song, et al. "LOC100996425 acts as a promoter in prostate cancer by mediating hepatocyte nuclear factor 4A and the AMPK/mTOR pathway." J Cell Mol Med. 2021 Sep;25(17):8174-8186. PMID:34309216
          3. Jingui Hu, Ling Zhang, et al. "Cardioprotective effect of ginsenoside Rb1 via regulating metabolomics profiling and AMP-activated protein kinase-dependent mitophagy." Journal of Ginseng Research.Available online 3 July 2021.
          4. Weipeng Hu, Shan Jiang, et al. "High phosphate impairs arterial endothelial function through AMPK‐related pathways in mouse resistance arteries." Acta Physiologica.
          5. Si-wei Wang, Wen Wang, et al. "Hesperetin, a SIRT1 activator, inhibits hepatic inflammation via AMPK/CREB pathway." Int Immunopharmacol. 2020 Oct 14;89(Pt B):107036. PMID:33068864
          6. Lei L, Chai Y, et al. "Dihydroquercetin Activates AMPK/Nrf2/HO-1 Signaling in Macrophages and Attenuates Inflammation in LPS-Induced Endotoxemic Mice." Front Pharmacol. 2020;11:662. PMID:32508636
          7. Yang PM, Hong YH, et al. "Progressive Rotavirus Infection Downregulates Redox-Sensitive Transcription Factor Nrf2 and Nrf2-Driven Transcription Units." Oxid Med Cell Longev. 2020 Apr 4;2020:7289120. PMID:32322337
          8. Su K, Yi B, et al. "Liraglutide attenuates renal tubular ectopic lipid deposition in rats with diabetic nephropathy by inhibiting lipid synthesis and promoting lipolysis." Pharmacol Res. 2020;156:104778. PMID:32247822
          9. Xie B, Zhao M, et al. "Induction of autophagy and suppression of type I IFN secretion by CSFV." Autophagy. 2020;1-23. PMID:32160078
          10. Lu Q, Liu J, et al. "Empagliflozin attenuates ischemia and reperfusion injury through LKB1/AMPK signaling pathway." Mol Cell Endocrinol. 2019 Nov 20:110642. PMID:31759100
          11. Xiao J, Yang R, et al. "A role of AMPK and connexin 43 in the suppression of CoCl(2)-induced apoptosis of spiral modiolar artery smooth muscle cells by adiponectin." Life Sci. 2019 Oct 23:116876. PMID:31655194
          12. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758
          13. Wei Q, Zhang B, et al. "Maslinic Acid Inhibits Colon Tumorigenesis by the AMPK-mTOR Signaling Pathway." J Agric Food Chem. 2019 Apr 17;67(15):4259-4272. PMID:30913881
          14. Tian L, Cao W, et al. "Pretreatment with Tilianin improves mitochondrial energy metabolism and oxidative stress in rats with myocardial ischemia/reperfusion injury via AMPK/SIRT1/PGC-1 alpha signaling pathway." J Pharmacol Sci. 2019 Apr;139(4):352-360. PMID:30910451
          15. Liu Y, Hu X, et al. "Rosiglitazone metformin adduct inhibits hepatocellular carcinoma proliferation via activation of AMPK/p21 pathway." Cancer Cell Int. 2019 Jan 11;19:13. PMID:30651718
          16. Li X, Liu J, et al. "Dichloroacetate ameliorates cardiac dysfunction caused by ischemic insults through AMPK signal pathway- not only shifts metabolism." Toxicol Sci. 2018 Oct 29. PMID:30371859
          17. He GR, Lin XK, et al. "Dexmedetomidine impairs P glycoprotein mediated efflux function in L02 cells via the adenosine 5' monophosphate activated protein kinase/nuclear factor κB pathway." Mol Med Rep.2018 Apr;17(4):5049-5056. PMID:29393492

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