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Chemical Structure| 866405-64-3 Chemical Structure| 866405-64-3

Structure of Dorsomorphin
CAS No.: 866405-64-3

Chemical Structure| 866405-64-3

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Dorsomorphin is a selective, ATP-competitive AMPK inhibitor (Ki of 109 nM in the absence of AMP) that selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6, and reverses autophagy activation and anti-inflammatory effects induced by Urolithin A.

Synonyms: Compound C; BML-275

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Product Details of Dorsomorphin

CAS No. :866405-64-3
Formula : C24H25N5O
M.W : 399.49
SMILES Code : C(CN1CCCCC1)OC1=CC=C(C=C1)C1=CN2N=CC(=C2N=C1)C1=CC=NC=C1
Synonyms :
Compound C; BML-275
MDL No. :MFCD08705402
InChI Key :XHBVYDAKJHETMP-UHFFFAOYSA-N
Pubchem ID :11524144

Safety of Dorsomorphin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H332
Precautionary Statements:P280

Related Pathways of Dorsomorphin

epigenetics
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • AMPK

    AMPK, Ki:109 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
U937 cells 5 μM 24 h Enhanced cell death induced by navitoclax, S63845, or A-1155463. PMC11043078
Hep3B cells 10 µM 16 h Dorsomorphin inhibited BMP2- and HJV-induced hepcidin promoter activity. PMC2727650
MRC-5 fetal lung fibroblasts 1 μM 4 days Dorsomorphin synergizes with FSK to promote neuronal survival and maturation, although independently DM has no effect on neuronal conversion. PMC3843951
IMR-90 fetal lung fibroblasts 1 μM 4 days Dorsomorphin synergizes with FSK to promote neuronal survival and maturation, although independently DM has no effect on neuronal conversion. PMC3843951
Clinical acute leukemia isolates 5 μM 24 h Synergized with navitoclax, venetoclax, A-1155463, or S63845 to enhance cell death. PMC11043078
Jurkat cells 5 μM 24 h Inhibited navitoclax- or S63845-induced AMPKα autophosphorylation and substrate phosphorylation, enhancing cell death. PMC11043078
C2C12 cells 4 µM 5 days Dorsomorphin inhibited BMP4- and BMP6-induced alkaline phosphatase activity, indicating inhibition of BMP-induced osteogenic differentiation. PMC2727650
Mouse pulmonary artery smooth muscle cells (PASMCs) 0.47 µM 30 min Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs, without affecting MAPK p38 activation. PMC2727650
Saos2 cells 5 μM 24 h To investigate the effect of Dorsomorphin on the migration and invasion of Saos2 cells, results showed that Dorsomorphin significantly inhibited the migration and invasion induced by TMEM119 overexpression. PMC5454443
FOP fibroblasts 1 μM 25 days Inhibited BMP-SMAD signaling, significantly reducing iPSC generation from FOP fibroblasts PMC5135304
WT-hepatocytes 10 µM 9 h Dorsomorphin completely restored the A23187-mediated inhibition of glycogen deposition, suggesting that the inhibitory effects of A23187 are mediated by AMPK signaling. PMC11060962
WT-hepatocytes 1, 3, or 10 µM 9 h Dorsomorphin reversed the ethanol-mediated inhibition of glycogen levels, indicating that ethanol suppresses glycogen deposition through the AMPK signaling pathway. PMC11060962
3T3-L1 fibroblasts 1 μmol/mL 24 h To verify whether AMPK mediates the anti-fibrotic effect of ORM, results showed that dorsomorphin reversed the inhibitory effect of ORM on fibrotic markers PMC8792011

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c Nude mice Jurkat, U937, or MV-4-11 xenograft models Intraperitoneal injection 25 mg/kg Three times a week for two weeks The combination of dorsomorphin with navitoclax or S63845 significantly inhibited xenograft growth with minimal toxicity to normal tissues. PMC11043078
Zebrafish Adult zebrafish Intraperitoneal injection 23 µg/g Single injection Dorsomorphin inhibited iron-induced hepatic SMAD1/5/8 phosphorylation and hepcidin expression. PMC2727650
Zebrafish Zebrafish embryos Exposure in embryo media 0.312 μM or 0.625 μM Exposure initiated at 0.75 hpf To investigate the effects of DMP on zebrafish embryonic development, particularly on dorsoventral patterning. Results showed that DMP treatment caused dorsalization of embryos, similar to the phenotype induced by TDCIPP. PMC6169527
Rats Streptozotocin-induced diabetic peripheral neuropathy model Intraperitoneal injection 0.2 mg/kg Once daily for 15 days To investigate the effect of Dorsomorphin on the protective role of Empagliflozin in diabetic peripheral neuropathy, results showed that Dorsomorphin almost completely abolished the beneficial effects of Empagliflozin. PMC9325846

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.52mL

2.50mL

1.25mL

25.03mL

5.01mL

2.50mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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