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

C₂₄H₂₀N₄O

380.44

MFCD18384963

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.
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.

Toxicity: Regulatory Review (Z)

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

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

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

100

≥97% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

orange

DMSO: 16.6 mg/mL

ambient

2-8℃

5 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3