Dorsomorphin (Compound C) 2HCl

Catalog No.S7306 Synonyms: BML-275 2HCl,Compound C 2HCl

Dorsomorphin (Compound C) 2HCl Chemical Structure

Molecular Weight(MW): 472.41

Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity.

Size Price Stock Quantity  
USD 147 In stock
USD 470 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 242 Publications

Purity & Quality Control

Choose Selective AMPK Inhibitors

Biological Activity

Description Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity.
Targets
AMPK [1]
(Cell-free assay)
109 nM(Ki)
In vitro

Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformin’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] in addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse C2C12 cells NF[wWW1HfW6ldHnvckBie3OjeR?= MnW1OEDPxE1? NEDRRZlKdmirYnn0bY9vKG:oIFLNVHIyNW2nZHnheIVlKG:|dHXvZoxie3RiZHnm[oVz\W62aXH0bY9vKGmwIFLNVFQue3SrbYXsZZRm\CCvb4Xz[UBEOkNzMjDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBidGujbHnu[UBxcG:|cHjheIF{\SCuZY\lcEBifCB2IIXNJIJ6KHOyZXP0do9xcG:2b33leJJ6 M2TURlE5ODJ4MEm0

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-SMAD / SMAD; 

PubMed: 30808965     


SMAD phosphorylation was assessed by Western blot after cells were treated with dorsomorphin (0 µM to 10 µM) from day 1 to day 3 or from day 3 to day 4.

Id1 / Id2 / Id3 ; 

PubMed: 25010525     


Dorsomorphin dramatically inhibited the expression of Ids. KMM cells were treated with 5 µM Dorsomorphin for 24 hours before harvesting. Expressions of Ids were detected by immunoblotting.

pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α ; 

PubMed: 29531259     


PC-3 and LNCaP cells were treated with vehicle, 25 µM compound 8c, 25 µM compound 8c + 5 μM Dorsomorphin (8c + D) or 5 μM Dorsomorphin (D), for 1 hour or 24 hours and levels of the phosphorylated AMPK (pAMPK), phosphorylated ACC (pACC), phosphorylated Raptor (pRaptor) forms and HIF1α were determined by Western blot. Upper panel, representative Western blot of three different experiments. β-tubulin (β-Tub) serves as a loading control. Lower panel, densitometric analyses of bands represented as the mean of the ratio pAMPK/AMPK or pACC/ACC.

p-ERK / ERK / Bcl2 / BAX / Cleaved caspase-3; 

PubMed: 30155931     


Western blot analysis of the protein expression of ERK, p‐ERK, Bcl2, BAXand cleaved caspase‐3 in T98 cells stimulated by Compound C (0, 1, 5, 10 μmol/L) for 24 h.

LC3B I/ LC3B II; 

PubMed: 30155931     


The representative western blot analysis showed that stimulation by Compound C for 24 h decreased the ratio of LC3BI/IIin T98 cells in a dose-dependent manner. 

30808965 25010525 29531259 30155931
Immunofluorescence
MyHC; 

PubMed: 20689554     


Satellite cell-derived myoblasts were plated at high cell density (80–90% confluency) and cultured in proliferation medium for 2 days with or without Dorsomorphin. Immunostaining for MyHC showed that Dorsomorphin promoted myogenic differentiation and fusion in a dose-dependent manner. 

Id1 / MyoD ; 

PubMed: 20689554     


(a) Exposure to 3 μM Dorsomorphin for 6 h to inhibit BMP signalling resulted in a downregulation of Id1 expression in satellite cells associated with a myofibre. (b) Similarly, immunostaining of plated satellite cells after exposure to 3 μM Dorsomorphin for 18 h in proliferation medium also resulted in downregulation of Id1 protein. Scale bar equals 20 μm.

20689554
Growth inhibition assay
Cell viability (MM cells); 

PubMed: 25010525     


Dorsomorphin showed preferential toxicity to KMM (KSHV-transformed MM cells) cells. KMM cells or MM cells were seeded 4000 cells/well. 24 hours after seeding, medium was replaced with Dorsomorphin medium as indicated. Cell viability was measured by MTT assay 48 hours post Dorsomorphin treatment. Data were shown as mean ± s.e.m., n = 3. 

Cell viability (glioma cell lines); 

PubMed: 24419061     


Histogram showing the dose-dependent effect of Compound C (1, 2.5, 5 and 10μM) on the viability of three glioma cell lines. Numbers inside bars represent % dead cells.

25010525 24419061
In vivo Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4]

Protocol

Animal Research:[3]
- Collapse
  • Animal Models: Iron-replete mice
  • Formulation: DMSO
  • Dosages: ~10 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro Water 94 mg/mL (198.97 mM)
DMSO Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
PBS
For best results, use promptly after mixing. 		15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 472.41
Formula

C24H25N5O.2HCl
CAS No. 1219168-18-9
Storage powder
in solvent
Synonyms BML-275 2HCl,Compound C 2HCl

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Is there any information you may provide as to WHICH AMPK SUBUNIT is this drug targeting in the AMPK complex?

  • Answer:

    According to the reference （see link below), Dorsomorphin(Compound C) should target the AMPK alpha subunit through ALCAR or metformin. http://www.ncbi.nlm.nih.gov/pubmed/20844250

selleck catalog

AMPK Signaling Pathway Map

Related AMPK Products

  • HTH-01-015 New

    HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

  • Dorsomorphin (Compound C) New

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

  • AICAR (Acadesine)

    AICAR (Acadesine), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

    Features:A potential first-in-class adenosine regulating agent (ARA).

  • Phenformin HCl

    Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

  • A-769662

    A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

  • WZ4003

    WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2 in cell-base assays, respectively, without significant inhibition on 139 other kinases.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

  • MK-2206 2HCl

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

    Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

  • CHIR-99021 (CT99021) HCl

    CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2.

Tags: buy Dorsomorphin (Compound C) 2HCl | Dorsomorphin (Compound C) 2HCl supplier | purchase Dorsomorphin (Compound C) 2HCl | Dorsomorphin (Compound C) 2HCl cost | Dorsomorphin (Compound C) 2HCl manufacturer | order Dorsomorphin (Compound C) 2HCl | Dorsomorphin (Compound C) 2HCl distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID