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203646 Sigma-Aldrich

BMP Inhibitor II, DMH1 - CAS 1206711-16-1 - Calbiochem

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: ALK2/3 Inhibitor, DMH1, Bone Morphogenetic Protein Inhibitor, DMH1, 4-(6-(4-Isopropoxyphenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline, BMP Inhibitor II, DMH1 - CAS 1206711-16-1 - Calbiochem

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Properties

Quality Level   100
assay   ≥97% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   orange
solubility   DMSO: 16.6 mg/mL
shipped in   ambient

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 µM in reporter assays using C2C12BRA expressing constitutively active ALK2, ALK3, or ALK6, respectively). Comparing to its non-BMPR-selective structural analog dorsomorphin (DM; Cat. Nos. 171260 & 171261), DMH1 is 12.5-times more potent in preventing BMP pathway-dependent DV (dorsoventral) development (EC100 = 0.2 µM DMH1 or 2.5 µM 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 µM.

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 (Cat. Nos. 171260 & 171261), DMH1 is 12.5-times more potent in preventing BMP pathway-dependent dorsoventral development (EC100 = 0.2 µM) 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 µM.

Packaging

5 mg in Glass bottle

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.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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