203646

BMP Inhibitor II, DMH1

The BMP Inhibitor II, DMH1, also referenced under CAS 1206711-16-1, controls the biological activity of BMP. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): BMP Inhibitor II, DMH1, ALK2/3 Inhibitor, DMH1, Bone Morphogenetic Protein Inhibitor, DMH1, 4-(6-(4-Isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline
• Empirical Formula (Hill Notation): C₂₄H₂₀N₄O
• CAS Number: 1206711-16-1
• Molecular Weight: 380.44
• MDL number: MFCD18384963
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: orange
• solubility: DMSO: 16.6 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C24H20N4O/c1-16(2)29-19-9-7-17(8-10-19)18-13-26-24-22(14-27-28(24)15-18)20-11-12-25-23-6-4-3-5-21(20)23/h3-16H,1-2H3
• InChI key: JMIFGARJSWXZSH-UHFFFAOYSA-N

Description

General description

A cell-permeable, potent, and highly selective BMPR (bone morphogenetic protein receptor) inhibitior (IC₅₀ against human ALK2/BMPR-I = 107.9 nM) that exhibits no inhibitory activity against ALK5, AMPK, FLK1/KDR/VEGRF2, or PDGFRβ. Effectively blocks ALK2- and ALK3-, but not ALK6-, mediated transcription activity (IC₅₀<500 nM, <100 nM, and >10 M in reporter assays using C2C12BRA expressing constitutively active ALK2, ALK3, or ALK6, respectively). Comparing to its non-BMPR-selective structural analog dorsomorphin, DMH1 is 12.5-times more potent in preventing BMP pathway-dependent DV (dorsoventral) development (EC₁₀₀ = 0.2 M DMH1 or 2.5 M DM) in zebrafish embryo in vivo, while being non-toxic to the fish embryo and exhibiting no effect against VEGF signaling-dependent intersomitic vessel (ISV) formation even at concentrations as high as 50 M.

A cell-permeable, potent, and highly selective BMPR inhibitior (IC₅₀ against human ALK2/BMPR-I = 107.9 nM), exhibiting no activity toward ALK5, ALK6, AMPK, FLK1/KDR/VEGRF2, or PDGFRβ. Comparing to its non-BMPR-selective structural analog dorsomorphin DMH1 is 12.5-times more potent in preventing BMP pathway-dependent dorsoventral development (EC₁₀₀ = 0.2 M) in zebrafish embryo in vivo, while being non-toxic to the fish embryo and exhibiting no effect against VEGF signaling-dependent intersomitic vessel formation even at concentrations as high as 50 M.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Hao, J., et al. 2010. ACS Chem.Biol.5, 245.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable