Dorsomorphin

SKU: orb1306886

Description

Dorsomorphin (BML-275) is a selective, ATP-competitive AMPK inhibitor (Ki=109 nM) that also blocks BMP receptors ALK2, ALK3, and ALK6. It is widely used in research to study autophagy, bone morphogenetic protein signaling, and tumor biology in both cellular and animal models due to its antitumor properties.

Research Area

Cell Biology, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 866405-64-3
• MW: 399.49
• Purity: >98%
• Formula: C₂₄H₂₅N₅O
• SMILES: C(CN1CCCCC1)Oc1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccncc1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 3 mg/ml).

Bioactivity

• Target IC50:
  MP46 cells:10.13 µM|A2780 cells:0.9 μM (EC50)|MCF-7 cells:4.9 μM (EC50)|OMM2.5 cells:31.45 µM|92-1 cells:6.526 µM|HeLa cells:10.71 μM|AMPK:109 nM (Ki)|Mel 270 cells:8.39 µM|HCT116 cells:11.34 μM
• In Vivo:
  METHODS: To test the antitumor activity in vivo, Dorsomorphin (10 mg/kg) was administered intraperitoneally to NOD/SCID mice bearing human tumor S1T once daily for 28 days. RESULTS: Dorsomorphin inhibited the growth of human ATL tumor xenografts in NOD/SCID mice. METHODS: To examine the effect on SMAD activity in vivo, Dorsomorphin (10 mg/kg) was administered as a single intraperitoneal injection to iron-dextran-treated C57BL/6 mice. RESULTS: Dorsomorphin eliminated iron-dextran-induced iron-mediated increase in hepatic SMAD1/5/8 phosphorylation.
• In Vitro:
  METHODS: Human tumor cells HeLa and HCT116 were treated with Dorsomorphin (1.25-80 μM) for 24 h, and cell viability was measured by CCK-8. RESULTS: Dorsomorphin inhibited the viability of HeLa and HCT116 cells with IC50 values of 10.71 μM and 11.34 μM, respectively. METHODS: ATL patient-derived PBMCs cells were treated with Dorsomorphin (5-25 μM) for 24 h. Apoptosis was detected by Flow Cytometry. RESULTS: Dorsomorphin increased the frequency of early apoptotic cells in PBMCs from patients with acute and chronic forms of ATL in a dose-dependent manner.
• Cell Research:
  Dorsomorphin is dissolved in DMSO (10 mM) and stored,and then diluted with appropriate media (DMSO 0.5%) before use.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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Compound C

Compound Identifiers

PubChem CID

11524144