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Sigma-Aldrich

DMH1

≥97% (HPLC), solid, BMP inhibitor, Calbiochem®

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

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About This Item

Empirical Formula (Hill Notation):
C24H20N4O
CAS Number:
Molecular Weight:
380.44
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77

product name

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.

Quality Level

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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Eduardo Branco de Sousa et al.
Revista brasileira de ortopedia, 57(2), 314-320 (2021-03-31)
Objective  Our goal was to evaluate the modulation of the synovial fluid cells (SFC) from patients with and without osteoarthritis (OA) by bone morphogenetic protein 4 (BMP-4), Smad-3 and transforming growth factor beta (TGF-β). Methods  Synovial fluid was collected from
Transient suppression of SUMOylation in embryonic stem cells generates embryo-like structures.
Cossec, et al.
Cell Reports, 42, 112380-112380 (2023)

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