1. Autophagy
    TGF-beta/Smad
  2. Autophagy
    TGF-β Receptor

DMH-1 

Cat. No.: HY-12273 Purity: 99.65%
Handling Instructions

DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.

For research use only. We do not sell to patients.

DMH-1 Chemical Structure

DMH-1 Chemical Structure

CAS No. : 1206711-16-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.

IC50 & Target

IC50: 27 nM (ALK1), 107.9 nM (ALK2), <5 nM (ALK3), 47.6 nM (ALK6)[1]

In Vitro

DMH-1 (0.5 μM) induces regulation of OCT4, Nanog, and PAX6 protein expression. DMH-1 significantly reduces the percentage of cells expressing the pluripotency marker proteins OCT4 and Nanog in both SM3 and CA6 cells. PAX6 expression is significantly up-regulated by day 5 and day 7 in CA6 and SM3 cells, respectively. DMH-1 induces regulation of pluripotency and neural precursor marker mRNAs. PAX6 can regulate the expression of SOX1 independently by manipulating the DMH-1 concentration during the neural induction of hiPSCs[2]. DMH-1 (5 μM and 10 μM) inhibits CDDP-induced autophagy in HeLa cells and enhances the ability of CDDP to reduce HeLa cell viability, inhibits tamoxifen-induced autophagy in MCF-7 cells and enhances the ability of tamoxifen to reduce MCF-7 cell viability, inhibits 5-FU-induced autophagy in both MCF-7 and HeLa cells but does not affect the inhibitory effects of 5-FU on MCF-7 and HeLa cell viability. DMH-1 enhances the apoptotic induction effects of CDDP on HeLa cells after 24 h treatment. DMH-1 inhibits HeLa and MCF-7 cell proliferation[3]. DMH-1 (20 μM) reduces the canonical phosphorylation of Smads 1,5 and 9. DMH-1 in combination with Cisplatin significantly decreases Ki-67 positive staining in the OVCAR8 cells. DMH-1 (20 µM) upregulates JAG1, reduces CYP1B1 and increases HAPLN1 expression in both OVCAR8 and NCI-RES cells[4].

In Vivo

DMH1 (5 mg/kg, i.p.) treatment significantly reduces the tumor growth in human lung cancer xenograft model[5].

Solvent & Solubility
In Vitro: 

DMSO : 11.5 mg/mL (30.23 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[3]

Cells are seeded in 96-well plates and treated with different drugs for appropriate time. Then 5 mg/mL MTT is added and incubated for 4 h at 37°C. Medium is then removed and 200 μL of DMSO is added to dissolve the crystal. Absorbance is measured at a wavelength of 490 nm with a plate reader.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[5]

Sub-confluent A549 cells are trypsinized and then suspended in serum free RPMI 1640 medium. The cell suspension (1×106 cells in 100 µL medium for each injection) is injected subcutaneously into both the right and left flanks of eight-week old NOD SCID mice (n=5 for each group). Mice are given Intraperitoneal (i.p.) injection of the vehicle (12.5% 2-hydroxypropyl-β-cyclodextrin) or 5 mg/kg DMH1 every other day. The tumor sizes are measured with a vernier caliper from the sixth day to the fourth week after tumor implantation. The tumor volume (V) is calculated according to the formulation: Volume=(width)2×length/2. The tumor tissues are dissected at the end of study, and are sectioned and stained with H & E, and for immunohistochemical analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

380.44

Formula

C₂₄H₂₀N₄O

CAS No.

1206711-16-1

SMILES

CC(C)OC1=CC=C(C2=CN3C(N=C2)=C(C4=CC=NC5=CC=CC=C45)C=N3)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.65%

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DMH-1
Cat. No.:
HY-12273
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DMH-1

Cat. No.: HY-12273