Dorsomorphin

SKU: orb1306886

Description

Dorsomorphin

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 866405-64-3
• MW: 399.49
• Purity: 98.00%
• Formula: C₂₄H₂₅N₅O
• SMILES: C(CN1CCCCC1)Oc1ccc(cc1)-c1cnc2c(cnn2c1)-c1ccncc1
• Target: TGF-beta/Smad,AMPK,Autophagy
• Solubility: 1M HCI:255 mg/mL (638.31 mM);DMSO:1.33 mg/mL (3.33 mM);10% DMSO+90% Saline:0.13 mg/mL (0.33 mM)

Bioactivity

• Target IC50:
  MP46 cells:10.13 µM|A2780 cells:0.9 μM (EC50)|MCF-7 cells:4.9 μM (EC50)|OMM2. 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 tes 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 inhibite the growth of human ATL tumor xenografts in NOD/SCID mice. METHODS: To examin the effect on SMAD activity in vivo Dorsomorphin (10 mg/kg) was administered as a Single intraperitoneal injection to iron-dextran-treated C57B-/- 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 inhibite 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 increase 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 us. eLa and 786-O cells are treated with various concentration 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.Fo the combination study,786-O cells are treated with various concentration 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 an the absorbance of Each well is determined.Fo the viability assay under glucose-withdrawal conditions,HT1080 cells are treated with various concentration 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 (mea ± D of quadruplicate determinations) is calculated by setting Each control absorbance from untreated cells as 100%.The effects of drug combinations at concentration producing 80% cell growth Inhibition (IC80) are analyzed usin the isobologram metho.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, AMPK, AMP-activated protein kinase, ATP-competitive, Autophagy, BML 275, BML275, BML-275, BMP, Dorsomorphin, Compound C, Transforming growth factor beta receptors, TGFβ, TGF-β Receptor, TGF-β/Smad, type, receptors, Smad, TGFb, TGF-b/Smad, TGFbeta/Smad, TGFbeta, TGF-beta

Compound Identifiers

PubChem CID

11524144