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Purity: ≥98%
DMH1 (DMH-1; DMH 1) is a selective and 2nd-generation small molecule inhibitor of BMP (bone morphogenetic protein) receptor inhibitor with potential antitumor activity. It inhibits ALK2 with an IC50 of 107.9 nM and exhibits no effects against other kinases such as AMPK, ALK5, KDR (VEGFR-2) or PDGFR.
| ln Vitro |
The expression of OCT4, Nanog, and PAX6 proteins is regulated by DMH-1 (0.5 μM). In SM3 and CA6 cells, DMH-1 dramatically decreased the proportion of cells expressing the pluripotency marker proteins OCT4 and Nanog. On days 5 and 7, respectively, there was a substantial upregulation of PAX6 expression in CA6 and SM3 cells. DMH-1 controls the mRNA for the neural precursor marker and causes pluripotency. During the neural induction process of hiPSCs, PAX6 can independently control the expression of SOX1 by controlling the concentration of DMH-1 [2]. In HeLa cells, DMH-1 (5 μM and 10 μM) inhibits autophagy induced by CDDP and increases CDDP's capacity to reduce cell viability; in MCF-7 cells, it inhibits autophagy induced by Tamoxifen and increases Tamoxifen's capacity to reduce MCF-7 cell viability; in MCF-7 and HeLa cells, it inhibits autophagy induced by 5-FU, but it has no effect on the inhibitory effect of 5-FU on the viability of MCF-7 and HeLa cells. After 24 hours of treatment, DMH-1 increased the effect of CDDP on HeLa cells that causes apoptosis. HeLa and MCF-7 cell growth is inhibited by DMH-1 [3]. Smads 1, 5, and 9 had less canonical phosphorylation when exposed to DMH-1 (20 μM). In OVCAR8 cells, the combination of DMH-1 and cisplatin dramatically decreased Ki-67 positive staining. In OVCAR8 and NCI-RES cells, DMH-1 (20 μM) upregulates JAG1, decreases CYP1B1, and enhances HAPLN1 expression [4].
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| ln Vivo |
Treatment with DMH1 (5 mg/kg, ip) dramatically inhibited the growth of tumors in a human lung cancer xenograft model [5].
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| References |
[1]. Engers DW, et al. Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of mL347 as an ALK2 versus ALK3 selective mLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52.
[2]. Sheng Y, et al. DMH1 (4-[6-(4-isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline) inhibits chemotherapeutic drug-induced autophagy. Acta Pharm Sin B. 2015 Jul;5(4):330-6. [3]. Neely MD, et al. DMH1, a highly selective small molecule BMP inhibitor promotes neurogenesis of hiPSCs: comparison of PAX6 and SOX1 expression during neural induction. ACS Chem Neurosci. 2012 Jun 20;3(6):482-91. [4]. Hover LD, et al. Small molecule inhibitor of the bone morphogenetic protein pathway DMH1 reduces ovarian cancer cell growth. Cancer Lett. 2015 Nov 1;368(1):79-87. [5]. Hao J, et al. DMH1, a small molecule inhibitor of BMP type i receptors, suppresses growth and invasion of lung cancer. PLoS One. 2014 Mar 6;9(6):e90748 |
| Molecular Formula |
C24H20N4O
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| Molecular Weight |
380.44
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| Exact Mass |
380.16371
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| CAS # |
1206711-16-1
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| Related CAS # |
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| SMILES |
O(C([H])(C([H])([H])[H])C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])C1C([H])=NC2=C(C([H])=NN2C=1[H])C1=C([H])C([H])=NC2=C([H])C([H])=C([H])C([H])=C12
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| Chemical Name |
4-(6-(4-isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6285 mL | 13.1427 mL | 26.2854 mL | |
| 5 mM | 0.5257 mL | 2.6285 mL | 5.2571 mL | |
| 10 mM | 0.2629 mL | 1.3143 mL | 2.6285 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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