1. Epigenetics
    PI3K/Akt/mTOR
    Autophagy
  2. AMPK
    Autophagy

Dorsomorphin (Synonyms: BML-275; Compound C)

Cat. No.: HY-13418A Purity: 99.32%
Handling Instructions

Dorsomorphin is a potent and selective AMPK inhibitor, that is competitive with ATP, with Ki=109±16 nM in the absence of AMP.

For research use only. We do not sell to patients.

Dorsomorphin Chemical Structure

Dorsomorphin Chemical Structure

CAS No. : 866405-64-3

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5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Dorsomorphin:

Customer Validation

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61.

    Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

    Dorsomorphin purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 May 19;18(5). pii: E1063.

    Inhibition of sirt1 and AMPK blocked Rb2-induced hepatic autophagy. HepG2 cells are pretreated with 50 µM Rb2 for 4 h in the presence or absence of the sirt1 inhibitor EX-528 (EX) and the specific AMPK inhibitor Compound C (CC), and then subjected to OA (1 mM for HepG2 and 2 mM for primary mouse hepatocytes) exposure for 12 h. For lipid content determination, intracellular TG are stained by Oil red O (ORO). ORO is then eluted with isopropanol and the optical absorbance of the eluate is measured

    Dorsomorphin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Autophagy is involved in Rg1-inhibited apoptosis in macrophages Macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in the absence or presence of 3-MA (5 mM). The protein expression level of cleaved caspase-3 determined by western blot analysis in Raw264.7 macrophages.

    Dorsomorphin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages with serum deprivation are treated with 50 μM Rg1 for 48 h in absence or presence of compound C (10 mM) or AICAR (250 μM). Western blots of the protein expressions of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Dorsomorphin purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Dorsomorphin purchased from MCE. Usage Cited in: Free Radic Biol Med. 2016 Nov 9;101:401-412.

    Effect of EsA on AMPK activation is necessary for AKT/GSK3β-mediated Nrf2 activity and cytoprotection. Cells are treated with 3 μM Compound C for 18 h, followed by treatment with EsA for 6 h, and then cell lysates are immunoblotted to assess the phosphorylation of AMPK, Akt and GSK3β and Nrf2.

    Dorsomorphin purchased from MCE. Usage Cited in: Oncotarget. 2016 Apr 5;7(14):18085-94.

    MACC1 is up-regulated by ACh through p-AMPK. A. ACh stimulates AMPK phosphorylation via M3R. B. Inhibition of AMPK activity by Dorsomorphin (8 μM) suppresses the induction of MACC1 expression by ACh. p-AMPK levels increase after ACh stimulation, and pretreatment of Darifenacin attenuates the ACh-induced increase of p-AMPK.

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Aug 15;138:49-60.

    Dose-dependent effects of Cantharidin on AMPK-related signaling in three HCC cell lines. The phosphorylation of AMPK is markedly upregulated, and so is its downstream effector phospho-ULK1, whereas PP5 expression is not affected after Cantharidin treatment.

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Aug 15;138:49-60.

    Blockade of AMPK signals by AMPK α2 siRNA or AMPK inhibitor (Dorsomorphin; 2.5 μM, pretreatment 2 hours) treatment counteracts the apoptotic effects of Cantharidin at 2.5 μM. Data are representative of at least two independent experiments. Blocking AMPK signaling by knockdown of AMPK or Dorsomorphin (AMPK kinase inhibitor) treatment markedly reverses the apoptotic effect of Cantharidin, indicating that AMPK activation is required for the anti-HCC activity of Cantharidin.

    Dorsomorphin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Aug 15;138:49-60.

    PP5 overexpression suppresses AMPK-Thr172 phosphorylation induced by AMPK activators, AICAR and metformin. Hep3B cells are transfected with indicated plasmids and treated with AICAR (2 mM; 3 h) or Metformin (3 mM; 16 h) to simulate AMPK phosphorylation.

    Dorsomorphin purchased from MCE. Usage Cited in: Cell Death Dis. 2017 May 18;8(5):e2798.

    Involvement of the AMPK/AKT/GSK3β pathway in Nrf2 nuclear translocation by Betulin. Cells are treated with 3 μM compound C (Comp.C) for 18 h before treatment with betulin (36 μM) for 6 h. Cell lysates are immunoblotted for the phosphorylation of AMPK, Akt, GSK3β and Nrf2.

    Dorsomorphin purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Effects of Palbociclib on CDK4/6-Rb pathway. HCC cells are treated with different doses of Palbociclib for 24 h, and then, the cells are subjected to western blot analysis.

    Dorsomorphin purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Inhibition of AMPK reverses Palbociclib-induced autophagy and apoptosis. Hep3B cells are incubated with AMPK inhibitor (Compound C, 2.5 μM) for 4 h and then treated with Palbociclib for 24 h. Apoptotic cells are determined by flow cytometry.

    Dorsomorphin purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Effects of CDK4/6 inhibitors on AMPK phosphorylation and apoptosis-related signals. After 24 h of drug treatment, the cells are subjected to western blot analysis. AMPK phosphorylation level is quantified by the ratio of band intensities of phospho-AMPKα vs. AMPKα.

    Dorsomorphin purchased from MCE. Usage Cited in: Mol Oncol. 2017 Aug;11(8):1035-1049.

    Co-treatment of Metformin and Ribociclib induces cell death in Hep3B cells. Cells are exposed to Ribociclib at 25 μM and/or Metformin at 10 mM for 72 h.

    Dorsomorphin purchased from MCE. Usage Cited in: Am J Chin Med. 2017 Aug 22:1-17.

    Activity of MMP-2 and MMP-9 in water extract (WAF)- and ethanol extract (EtAF)-treated CT26 cells after CC (20 μM) pretreatment for 4 h.

    Dorsomorphin purchased from MCE. Usage Cited in: Lung Cancer. 2017 Oct;112:81-89.

    Dose-and time-dependent effects of Cantharidin on p-AMPK, PARP, and Caspase 9. Cells are treated with Cantharidin at indicated concentrations for 24 hours or 2.5 μM Cantharidin for different time durations. The protein levels are analyzed with indicated antibodies.

    Dorsomorphin purchased from MCE. Usage Cited in: J Cell Physiol. 2018 May;233(5):3945-3954.

    Fraxinellone-prompted phosphorylation of AMPK is blocked by Compound C (CC).

    Dorsomorphin purchased from MCE. Usage Cited in: Mol Cell. 2017 Oct 19;68(2):336-349.e6.

    AMPK DKO SV40-immortalized MEFs are electroporated with plasmids encoding Myc-tagged AMPK α1, Myc-tagged AMPK α2 and Myc-tagged AMPK α2 S > A. 48 hr later, MEFs are starved for 3 hr and treated for 2 hr with DMSO or 50 mM A769662 before protein extraction. Western blot analysis shows the A769662-induced ACC phosphorylation in transfected cells.

    Dorsomorphin purchased from MCE. Usage Cited in: Zhongguo Sheng Wu Hua Xue Yu Fen Zi Sheng Wu Xue Bao. 2017;8,33(8):781-788.

    Western blotting for AMPKα, p-AMPKα and CCS.C13 cells are exposed to 10 μM Compound C 12 hours. The cell lysates are prepared and AMPKα, p-AMPKα and CCS are examined by Western blotting with specific antibodies. The data are representative of three independent experiments.

    Dorsomorphin purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Feb 19;100:417-425.

    HaCaT cells are pre-incubated with Compound C (CC) (10 μM) and U0126 (10 μM), pharmacological inhibitors of AMPKα, ERK, respectively, for 1 h before treatment with DA8 and DA14 (DAs).

    Dorsomorphin purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Mar 21;66(11):2758-2764.

    Effect of D-fagomine on the expression of phosphorylated LKB1, AMPK, SIRT1, and PGC-1α in HUVECs. Cultured HUVECs are treated with D-fagomine (0.1, 1, or 10 μM) for 24 h. Cell lysates are prepared and subjected to Western blotting analyses.

    Dorsomorphin purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Feb 5;9:68.

    CT26 cells are treated with CC for 4 h and detected phosphorylation levels of AMPK.

    Dorsomorphin purchased from MCE. Usage Cited in: Biotechnol Appl Biochem. 2018 Mar 25.

    The mTOR inhibitor Rapamycin augments the autophagy induced by GEM. (A, B) Beclin-1 and LC3B expression is analyzed by western blot after treatment of the cells with GEM (5 μM) and Rapamycin (0, 1, and 2.5 μM) for 48 (A) or 72 (B) h.

    Dorsomorphin purchased from MCE. Usage Cited in: Redox Biol. 2018 Apr 18;17:180-191.

    MDA-MB-231 cells are cultured in poly-HEMA coated dishes and treated with Compound C or GL-V9 for 36 h. The expression of AMPK and p-AMPK in Compound C treated cells are assayed by Western blotting.

    Dorsomorphin purchased from MCE. Usage Cited in: Liver Int. 2018 May 24.

    Cells are treated with 5 μM Dorsomorphin dihydrochloride (Compound C) for 3 hours to inhibit AMPK activity. Next, 2.5 μM CTD is applied for 24 hours. Cells are then collected for apoptosis assays and western blotting.

    Dorsomorphin purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jul 5;66(26):6772-6781.

    Effects of Compound C on capsiate-treated HepG2 cells in high fat environment. The expressions of key metabolic regulators and lipid metabolism-related proteins are quantified by densitometry, and the relative intensities are expressed in the bar chart.

    Dorsomorphin purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jul 5;66(26):6772-6781.

    Effects of Compound C on capsiate-treated HepG2 cells in high fat environment. The expressions of glucose metabolism-related proteins are quantified by densitometry, and the relative intensities are expressed in the bar chart.

    Dorsomorphin purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018 Jul 13;48(1):227-236.

    Inhibition of AMPK with Compound C (CC) attenuates the protective effects of FNDC5 on the oxLDL-induced AMPK dephosphorylation and fibrosis in LX-2 cells.

    Dorsomorphin purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Aug 5.

    HUVECs are pretreated with Compound C (5, 10, or 20 μM) for 18 hr or AICAR (1, 2, or 4 mM) for 1 hr, and then exposed to LSS for 30 min.

    Dorsomorphin purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jul 16;9:761.

    Epithelial cells from colon tissue are extracted from mice in each group (n=6-8 per group) and protein level of p-AMPK (Thr172) and AMPKα1/2 are measured by western blot.

    Dorsomorphin purchased from MCE. Usage Cited in: Med Sci Monit. 2018 Jul 25;24:5168-5177.

    The levels of p-S6K and S6K in 16HBE cells after treatment of Rosiglitazone/Troglitazone or/and Compound C are detected by western blot. The levels of p62 and LC3 in 16HBE cells after treatment of Rosiglitazone/Troglitazone or/and Compound C are detected by western blot.

    Dorsomorphin purchased from MCE. Usage Cited in: PLoS One. 2018 Aug 1;13(8):e0200897.

    Phosphorylation of AMPK (Thr172) in HTOZ cells pretreated with Compound C at different concentrations (0-20 μM) for 1 hour prior to the presence of norUDCA at 200 μM for additional 1 hour is determined by western blotting analyses.

    Dorsomorphin purchased from MCE. Usage Cited in: J Immunol Res. 7 August 2018.

    Western blot assays show that 3-MA abrogates the Alda-1 induced expression increases in LC3BⅡ and Bcl2 and decreases in P62 and Bax.

    Dorsomorphin purchased from MCE. Usage Cited in: J Immunol Res. 7 August 2018.

    Western blot analysis of p-AMPK, AMPK, Bcl2 and Bax, LC3B and P62 expression in liver tissues.

    Dorsomorphin purchased from MCE. Usage Cited in: Redox Biol. 2018 Oct;19:339-353.

    Western blotting assay of AMPK, p-AMPK, PGC-1α, p-PGC-1α levels in nucleus pulposus (NP) cells stimulated with AGEs (200 μg/mL) in the presence or absence of A-769662 (50 μM), RAGE antibody (10 μg/mL), nicotinamide mononucleotide (NMN, 100 μM) or Compound C (50 uM).

    Dorsomorphin purchased from MCE. Usage Cited in: Redox Biol. 2018 Oct;19:339-353.

    Representative western blotting assay and quantitation of the level of Cyt-c in mitochondrial and cytoplasmic extracts from human NP cells with MitoTEMPO or SKQ1 pre-treatment.

    Dorsomorphin purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Aug 29;9:986.

    AMPK and p38 phosphorylation is confirmed after Compound C (CC) and SB203580 treatment of Gomisin A (G.A)-treated CT26 cells.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dorsomorphin is a potent and selective AMPK inhibitor, that is competitive with ATP, with Ki=109±16 nM in the absence of AMP.

    IC50 & Target[1]

    AMPK

    109 nM (Ki)

    Autophagy

     

    In Vitro

    HT1080 cells are treated with 10 μM Dorsomorphin for 2 h under 2DG stress. Immunoblot analysis reveals that phosphorylation levels of the catalytic α subunit of AMPK are increased by exposure of HT1080 cells to 2DG, whereas both basal and 2DG-induced phosphorylation levels are clearly reduced when Dorsomorphin is added. Measurements of cellular kinase activity using an ELISA-based assay system confirmed that Dorsomorphin does reduce the endogenous AMPK activity regardless of cell culture conditions[2].

    In Vivo

    Administration of Dorsomorphin over 24 h leads to a 60% increase in total serum iron concentrations. Dorsomorphin treatment is therefore effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice[3].

    Solvent & Solubility
    In Vitro: 

    Ethanol : 3.33 mg/mL (8.34 mM; Need ultrasonic)

    DMSO : 2 mg/mL (5.01 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5032 mL 12.5160 mL 25.0319 mL
    5 mM 0.5006 mL 2.5032 mL 5.0064 mL
    10 mM 0.2503 mL 1.2516 mL 2.5032 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [2]

    HT1080 cells are seeded in 24-well plates (2×104 cells per well) and treated with Dorsomorphin in the presence or absence of glucose or 10 mM 2DG for 2 h. HT1080 cells that overexpressed the wild-type and dominant negative AMPKα1 are prepared by transfecting plasmid DNA (pAMPKα1-wt, pAMPKα1-D168A and pcFlag as a control) in 6-well plates, seeding in 24-well plate and treating with UPR inhibitors. Cells are lysed with cell lysis buffer (20 mM Tris-HCl, pH 7.5, 250 mM NaCl, 10% glycerol, 0.5% NP-40, 1 mM EDTA, 1 mM EGTA, 0.2 mM PMSF, 1 µg/mL pepstatin, 0.5 µg/mL leupeptin, 5 mM NaF, 2 mM Na3Vo4, 2 mM β-glycerophosphate, 1 mM DTT). Relative AMPK kinase activity (mean±SD of duplicate determinations) to control sample (vehicle or pcFlag under normal growth conditions) is determined using the CycLex AMPK kinase assay kit[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    HeLa and 786-O cells are treated with various concentrations of Dorsomorphin (0, 0.3, 1, 3, 10 µM ), Versipelostatin and Phenformin in the presence or absence of 10 mM 2DG or 1 µg/mL of Tunicamycin as a stressor for 30 h in 96-well plates. For the combination study, 786-O cells are treated with various concentrations of UPR inhibitors in the presence or absence of 10 mM 2DG for 24 h. The medium is then replaced with fresh growth medium, and cells are cultured for a further 15 h. Subsequently, MTT is added to the culture medium, and the absorbance of each well is determined. For the viability assay under glucose-withdrawal conditions, HT1080 cells are treated with various concentrations of Dorsomorphin and phenformin in 12-well plates in the presence or absence of glucose for 18 h, seeded in 96-well plates with growth medium, and then cultured for a further 48 h before MTT is added. Relative cell survival (mean±SD of quadruplicate determinations) is calculated by setting each control absorbance from untreated cells as 100%. The effects of drug combinations at concentrations producing 80% cell growth inhibition (IC80) are analyzed using the isobologram method[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    12-week-old C57BL/6 mice raised on a standard diet are injected via the tail vein with 0.2 g/kg of Dextran or 0.2 g/kg of iron-dextran USP. Dextran is injected with vehicle only, whereas iron-dextran is injected with either vehicle or Dorsomorphin (10 mg/kg). 1 h after injection, mice are killed and liver segments are collected in 500 µL of SDS-lysis buffer and mechanically homogenized. 20 µL of liver extracts are resolved by SDS-PAGE and immunoblotted. Total RNA is harvested using Trizol from mechanically homogenized mouse livers (6 h after injection with a single intraperitoneal dose of Dorsomorphin (10 mg/kg) or DMSO).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    399.49

    Formula

    C₂₄H₂₅N₅O

    CAS No.

    866405-64-3

    SMILES

    C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2

    Storage

    4°C, protect from light

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.32%

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    Product Name:
    Dorsomorphin
    Cat. No.:
    HY-13418A
    Quantity:

    Dorsomorphin

    Cat. No.: HY-13418A