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

Dorsomorphin dihydrochloride (Synonyms: BML-275 dihydrochloride; Compound C dihydrochloride)

Cat. No.: HY-13418 Purity: 99.73%
Handling Instructions

Dorsomorphin dihydrochloride (BML-275 dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109±16 nM.

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

Dorsomorphin dihydrochloride Chemical Structure

Dorsomorphin dihydrochloride Chemical Structure

CAS No. : 1219168-18-9

Size Price Stock Quantity
10 mM * 1 mL in Water USD 66 In-stock
Estimated Time of Arrival: December 31
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 dihydrochloride:

Customer Validation

    Dorsomorphin dihydrochloride 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 dihydrochloride 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 dihydrochloride purchased from MCE. Usage Cited in: Redox Biol. 2018 Jul;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 dihydrochloride purchased from MCE. Usage Cited in: Liver Int. 2018 Dec;38(12):2248-2259.

    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 dihydrochloride purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Nov 7;66(44):11757-11766.

    The number of GFP-LC3 dots are reduced significantly after inhibiting STAT3 (AG-490) signaling.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1390-1395.

    Effect of atorvastatin and Compound C on cell viability, cell surface area, and apoptosis in Ang II-treated H9c2 cells.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1390-1395.

    Effect of atorvastatin and Compound C on the AMPK/Foxo1/miR-143-3p axis in Ang II-treated H9c2 cells.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018 Nov 5;50(5):1891-1902. 

    AMPK inhibitor dorsomorphin treatment reduces the protein expression of PGC-1α.

    Dorsomorphin dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride purchased from MCE. Usage Cited in: Am J Chin Med. 2017;45(6):1309-1325.

    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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):428-435.

    Western blotting showing AMPK/m-TOR/ULK1 pathway relative protein (AMPK, p-AMPK, mTOR, p-mTOR, ULK1 and p-ULK1) levels in low glucose (LG), LG+Compound C (CC), HG and HG+CC groups.

    Dorsomorphin dihydrochloride 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 dihydrochloride purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Dec;233(12):9701-9715.

    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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride purchased from MCE. Usage Cited in: J Immunol Res. 2018; 2018: 9807139

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

    Dorsomorphin dihydrochloride 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 dihydrochloride 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.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: Int J Mol Med. 2018 May;41(5):2535-2544.

    Cells are treated with AICAR and AICAR (A++, 10 μM) + Compound C (C++, 1 μM) for 24 h, after which western blot analysis is performed.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: J Cardiovasc Pharmacol. 2018 Oct;72(4):167-175.

    Foam cells are incubated with or without Compound C (10 μM) before the addition of CTRP9. According to the Western blot, the relative protein levels of p-AMPK, p-mTOR, LC3 II, and p62 are analyzed, respectively.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: J Am Heart Assoc. 2018 Jun 12;7(12). 

    Representative immunoblots of LC3 in Hippo and cortical brain tissue after CA/CPR. β-Actin serves as a loading control. J, Optical densities of LC3-II and LC3-I protein bands are quantitated. Cc indicates compound C.

    Dorsomorphin dihydrochloride purchased from MCE. Usage Cited in: J Am Heart Assoc. 2018 Jun 12;7(12). 

    Representative photomicrographs of immunohistochemistry for MAP2, Nissl, Iba-1, and GFAP in the hippocampal CA1 region of the sham-operated, sham-treated with Met (Met-a), and the experimental groups (Veh, Mettreated group, compound C [Cc]–treated group, Met+Cc-treated group, chloroquine [CQ]–treated group, and Met+CQ-treated group) at 7 days after return of spontaneous circulation.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dorsomorphin dihydrochloride (BML-275 dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109±16 nM.

    IC50 & Target

    Ki: 109±16 nM (AMPK)[1]

    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: 

    H2O : ≥ 50 mg/mL (105.84 mM)

    DMSO : 5.2 mg/mL (11.01 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1168 mL 10.5840 mL 21.1681 mL
    5 mM 0.4234 mL 2.1168 mL 4.2336 mL
    10 mM 0.2117 mL 1.0584 mL 2.1168 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Dorsomorphin dihydrochloride is dissolved in saline[4].

    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

    472.41

    Formula

    C₂₄H₂₇Cl₂N₅O

    CAS No.

    1219168-18-9

    SMILES

    [H]Cl.[H]Cl.C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.73%

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    Product Name:
    Dorsomorphin dihydrochloride
    Cat. No.:
    HY-13418
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    Dorsomorphin dihydrochloride

    Cat. No.: HY-13418