| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
BMP type I receptors: ALK6, ALK3, and ALK2. Ki values: <1 nM (ALK6), 5.4 nM (ALK3), and 43 nM (ALK2).
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|---|---|
| ln Vitro |
Three lung cancer cell lines with K-Ras mutations (A549, H157, H727) and three lung cancer cell lines without K-Ras mutations (H1299, H865, U1752) exhibit growth impairment due to reduced expression of Id1 and Id3. Display[1]. The combination of DMH2 and PP2 significantly reduced Id1 promoter activity and inhibited growth in A549 cells more than either drug did alone [1].
DMH2 is a potent antagonist of BMP type I receptors with Ki values of <1 nM for ALK6, 5.4 nM for ALK3, and 43 nM for ALK2. It downregulates the expression of Id1 and Id3 proteins. The compound inhibits proliferation and induces cell death of lung cancer cell lines. It causes cell growth reduction and apoptosis in H1299 non-small cell lung cancer cells in vitro. |
| ln Vivo |
At a dosage of 2 mg/kg, DMH2 (0–2 mg/kg, IP, twice daily, 2 days prior to PH (partial hepatectomy), 2 days subsequent to PH) enhanced hepatocyte proliferation from 13.7% to 26.9% [2].
DMH2 decreases growth and induces cell death of lung cancer cell lines in vivo. As a BMP type I receptor antagonist, the compound inhibits BMP signaling, which plays a role in cancer progression. The compound's antiproliferative and pro-apoptotic effects in lung cancer models support its potential as an anticancer agent. |
| Enzyme Assay |
In vitro BMP receptor binding assays for DMH2 measure its affinity for BMP type I receptors (ALK2, ALK3, ALK6). Radioligand binding studies using membrane preparations from cells expressing recombinant receptors and radiolabeled BMP ligands or selective antagonists are conducted. Competition binding experiments determine Ki values for each receptor subtype.
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| Cell Assay |
In vitro cell-based assays for DMH2 evaluate its antiproliferative and pro-apoptotic effects in cancer cell lines. H1299 non-small cell lung cancer cells and other lung cancer cell lines are treated with varying concentrations of the compound. Cell viability is assessed using standard assays, and apoptosis is confirmed by measuring caspase activity or annexin V staining. Id1 and Id3 protein levels are measured by Western blot.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (7-8 weeks, male) [2]
Doses: 0.5, 1, 2 mg/kg Route of Administration: IP twice (two times) daily, 2 days before PH, 2 days after PH (partial Hepatectomy) Experimental Results: Hepatocyte proliferation increased from 13.7% to 26.9% at the 2 mg/kg dose. In vivo animal studies for DMH2 have been conducted in mouse models of lung cancer. The compound is administered systemically, and tumor growth inhibition is monitored. Endpoints include tumor volume, tumor weight, and histopathological analysis. Biomarkers of BMP signaling such as Id1 and Id3 expression are assessed in tumor tissue. |
| ADME/Pharmacokinetics |
DMH2 has a molecular weight of 451.52 g/mol. Detailed pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion are not extensively reported in the provided literature. The compound is soluble in DMSO and other organic solvents. Storage conditions are typically -20°C.
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| Toxicity/Toxicokinetics |
Specific toxicity data for DMH2 is not extensively reported. As a BMP receptor antagonist, its safety profile would need to be established through comprehensive toxicology studies. The compound is classified as a research-grade chemical and is not intended for human use.
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| References |
[1]. Langenfeld J E, Langenfeld E. Src inhibition enhances BMP receptor antagonists downregulation of Id1 and growth suppression of lung cancer cells with a K-Ras mutation. 2013:5263.
[2]. Tsugawa D, Oya Y, Masuzaki R, et al. Specific activin receptor-like kinase 3 inhibitors enhance liver regeneration. J Pharmacol Exp Ther. 2014;351(3):549-558. |
| Additional Infomation |
DMH2 (CAS# 1206711-14-9) is a potent antagonist of BMP type I receptors with Ki values of <1 nM for ALK6, 5.4 nM for ALK3, and 43 nM for ALK2. It downregulates Id1 and Id3 expression and inhibits proliferation and induces cell death in lung cancer cell lines. It causes cell growth reduction and apoptosis in H1299 non-small cell lung cancer cells. It has not received FDA approval.
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| Molecular Formula |
C27H25N5O2
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|---|---|
| Molecular Weight |
451.53
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| Exact Mass |
451.2
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| CAS # |
1206711-14-9
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| PubChem CID |
50997748
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.689
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| LogP |
2.09
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
639
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCN(CCOC2C=CC(=CC=2)C2C=NC3=C(C=NN3C=2)C2C=CN=C3C=CC=CC=23)CC1
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| InChi Key |
DXLXRNZCYAYUED-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H25N5O2/c1-2-4-26-24(3-1)23(9-10-28-26)25-18-30-32-19-21(17-29-27(25)32)20-5-7-22(8-6-20)34-16-13-31-11-14-33-15-12-31/h1-10,17-19H,11-16H2
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| Chemical Name |
4-[2-[4-(3-quinolin-4-ylpyrazolo[1,5-a]pyrimidin-6-yl)phenoxy]ethyl]morpholine
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| Synonyms |
DMH 2 DMH-2 DMH2
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2147 mL | 11.0735 mL | 22.1469 mL | |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4294 mL | |
| 10 mM | 0.2215 mL | 1.1073 mL | 2.2147 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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