- LDN-212854
- Imperatorin
- ML347
- PD 169316
| DMH-1Selective BMP ALK2 receptor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.68%
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- Datasheet
Chemical structure
| Description | DMH1 is a selective inhibitor of BMP receptor with IC50 of 107.9 nM for ALK2. | |||||
| Targets | BMP signaling | ALK2 | ||||
| IC50 | 100 nM | 107.9 nM | ||||
| Kinase experiment [1]: | |
Inhibitory activities | DMH1, a small molecule inhibitor of BMP Type I receptors, potently reduced lung cell proliferation, promoted cell death, and decreased cell migration and invasion in NSCLC cells by blocking BMP signaling, It suppressed Smad 1/5/8 phosphorylation and gene expression of Id1, Id2 and Id3. |
| Cell experiment [1]: | |
Cell lines | A549 and H460 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | Cell scratch-wound Assay: 24 h DMH1 at 1 μM and 3μM concentrations.Cell Proliferation Assay：incubated for 48 hours and 96 hours |
Applications | DMH1 blocked BMP signaling in NSCLC cells and decreased NSCLC cell migration and invasion, DMH1 reduces NSCLC cell proliferation and induces cell death |
| Animal experiment [1]: | |
Animal models | Xenograft model |
Dosage form | 5 mg/kg DMH1 every other day. |
Preparation method | dissolved in 12.5% 2-hydroxypropyl-b-cyclodextrin |
Application | The rate for doubling tumor size in DMH1-treated mice was about one day longer than the controls (5.6 versus 4.7 days in the DMH1 treated and control mice, respectively). MH1 treatment resulted in a statistically significant reduction in tumor volumes by about 50% compared to the vehicle control group. In a word , DMH1 attenuated xenograft lung tumor growth in mice |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Jijun Hao, Rachel Lee, Andy Chang, et al. DMH1, a Small Molecule Inhibitor of BMP Type I Receptors, Suppresses Growth and Invasion of Lung Cancer. 2014, 9(3): e90748. | |
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| Cas No. | 1206711-16-1 | SDF | Download SDF |
| Canonical SMILES | CC(C)OC1=CC=C(C=C1)C2=CN3C(=C(C=N3)C4=CC=NC5=CC=CC=C45)N=C2 | ||
| Formula | C24H20N4O | M.Wt | 380.44 |
| Solubility | ≥9.511mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
DMH1 is a small molecule inhibitor of bone morphogenetic protein (BMP) signaling with IC50 value of 107.9nM against ALK2 [1].
DMH1 is an analog of dorsomorphin. It exclusively targets BMP and has no effect on VEGF signaling. DMH1 shows potent and specific inhibitory activity against purified human BMP type-I receptor ALK2 with IC50 value of 107.9nM. It shows no significant inhibition of purified KDR, ALK5, AMPK and PDGFRβ. In cells respectively transfected with the active forms of ALK2, ALK3 and ALK6, DMH1 effectively inhibits signaling by ALK2 and ALK3 with IC50 values of both less than 0.5μM. In addition, DMH1 has no effect on the p38/MAP kinase signaling or the Activin A-induced Smad2 activation [1].
Moreover, DMH1 is found to have antitumor effect in lung cancer through blocking BMP signaling. In the NSCLC cell line A549 cells, DMH1 inhibits the phosphorylation of Smad 1/5/8 and decreases the expression of Id1, Id2 and Id3 genes. It decreases cell migration and invasion in A549 and H460 cell line. Besides that, DMH1 reduces cell proliferation and induces cell death in A549 cells. In the A549 tumor xenograft in mice, treatment of DMH1significantly suppresses tumor growth [2].
References:[1] Hao J, Ho J N, Lewis J A, et al. In vivo structure- activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. ACS chemical biology, 2010, 5(2): 245-253.[2] Hao J, Lee R, Chang A, et al. DMH1, a Small Molecule Inhibitor of BMP Type I Receptors, Suppresses Growth and Invasion of Lung Cancer. PloS one, 2014, 9(3): e90748.
