Dorsomorphin NEW
| Price | $48 | $74 | $249 |
| Package | 5mg | 10mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Dorsomorphin | CAS No.: 866405-64-3 |
| Purity: 99.3% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Dorsomorphin |
| Description | Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity. |
| Cell Research | Dorsomorphin is dissolved in DMSO (10 mM) and stored,and then diluted with appropriate media (DMSO 0.5%) before use[2].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[2]. |
| Kinase Assay | HT1080 cells are seeded in 24-well plates (2×104 cells per well) and treated with Dorsomorphin in the presence or absence of glucose or 10 mM 2DG for 2 h. HT1080 cells that overexpressed the wild-type and dominant negative AMPKα1 are prepared by transfecting plasmid DNA (pAMPKα1-wt, pAMPKα1-D168A and pcFlag as a control) in 6-well plates, seeding in 24-well plate and treating with UPR inhibitors. Cells are lysed with cell lysis buffer (20 mM Tris-HCl, pH 7.5, 250 mM NaCl, 10% glycerol, 0.5% NP-40, 1 mM EDTA, 1 mM EGTA, 0.2 mM PMSF, 1 μg/mL pepstatin, 0.5 μg/mL leupeptin, 5 mM NaF, 2 mM Na3Vo4, 2 mM β-glycerophosphate, 1 mM DTT). Relative AMPK kinase activity (mean±SD of duplicate determinations) to control sample (vehicle or pcFlag under normal growth conditions) is determined using the CycLex AMPK kinase assay kit[2]. |
| 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. [1] 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. [2] |
| 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. [2] 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. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 10% DMSO+90% Saline : 0.13 mg/mL (0.33 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 1.33 mg/mL (3.34 mM), Sonication and heating are recommended. |
| Keywords | BML275 | AMP-activated protein kinase | inhibit | ATP-competitive | Inhibitor | Dorsomorphin | BMP | Transforming growth factor beta receptors | Autophagy | AMPK | type | receptors | BML 275 | TGF-β Receptor |
| Inhibitors Related | Stavudine | Xylitol | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib | Chitosan oligosaccharide |
| Related Compound Libraries | Bioactive Compound Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Fibrosis Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library | TGF-beta/Smad Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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