Dorsomorphin (BML275)

Alias:

BML-275,Compound C; BML275; BML-275; BML 275; CpdC;Dorsomorphin

Cat No.:V0251 Purity: ≥98%
Dorsomorphin(BML-275) is a reversible and selective AMPK (AMP-activated protein kinase) inhibitor with a Ki of 109 nM in cell-free assays, exhibiting little effects against closely related kinases such as ZAPK, SYK, PKCθ, PKA, and JAK3.
Dorsomorphin (BML275) Chemical Structure CAS No.: 866405-64-3
Product category: AMPK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Dorsomorphin (BML275):

  • Dorsomorphin 2HCl (BML275)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
Dorsomorphin (BML-275), a selective and reversible AMPK (AMP-activated protein kinase) inhibitor, has a Ki of 109 nM in cell-free assays and has negligible effects on other closely related kinases like ZAPK, SYK, PKC, PKA, and JAK3. Inhibiting BMP signaling, which encourages cardiomyogenesis in embryonic stem cells, is another function of dorsomorphin. By suppressing the signaling of bone morphogenetic protein, dorsomorphin changes the mesenchymal phenotype of breast cancer-causing cells.
Biological Activity I Assay Protocols (From Reference)
Targets
AMPK (Ki = 109 nM); ACVR1; BMPR1A; ALK6; Autophagy
ln Vitro
Dorsomorphin reduces the ability of AICAR and metformin to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes, as well as their ability to inactivate ACC. [1]
In HT-29 cells, Dorsomorphin almost entirely prevents autophagic proteolysis by inhibiting AMPK activity.[2]
Dorsomorphin additionally blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription, and osteogenic differentiation by selectively inhibiting the BMP type I receptors ALK2, ALK3 and ALK6.[3]
ln Vivo
Dorsomorphin (10 mg/kg) increases serum iron levels and lowers basal levels of hepcidin expression in adult mice. [3]
Dorsomorphin (0.2 mg/kg, i.v.) significantly lowers VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4]
Enzyme Assay
Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPKinhibitor, with aKiof 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3 and ALK6.
Cell Assay
Dorsomorphin (compound C) (0-10 μM, 18 h) suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunicamycin-induced GRP78 promoter activity. Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells.
Animal Protocol
Iron-replete mice; Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin.
10 mg/kg.
Intravenously once.
References

[1]. J Clin Invest. 2001 Oct;108(8):1167-74.

[2]. J Biol Chem. 2006 Nov 17;281(46):34870-9.

[3]. Nat Chem Biol. 2008 Jan;4(1):33-41.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H25N5O
Molecular Weight
399.49
Exact Mass
399.2059
Elemental Analysis
C, 72.16; H, 6.31; N, 17.53; O, 4.00
CAS #
866405-64-3
Appearance
Solid powder
SMILES
C12=C(C3=CC=NC=C3)C=NN1C=C(C4=CC=C(OCCN5CCCCC5)C=C4)C=N2
InChi Key
XHBVYDAKJHETMP-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H25N5O/c1-2-12-28(13-3-1)14-15-30-22-6-4-19(5-7-22)21-16-26-24-23(17-27-29(24)18-21)20-8-10-25-11-9-20/h4-11,16-18H,1-3,12-15H2
Chemical Name
6-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine
Synonyms

BML-275,Compound C; BML275; BML-275; BML 275; CpdC;Dorsomorphin

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~3 mg/mL (7.5 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (5.0 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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