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203646

Sigma-Aldrich

DMH1

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

Synonyme(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

Formule empirique (notation de Hill):
C24H20N4O
Numéro CAS:
Poids moléculaire :
380.44
Numéro MDL:
Code UNSPSC :
51111800
Nomenclature 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.

Niveau de qualité

Pureté

≥97% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

orange

Solubilité

DMSO: 16.6 mg/mL

Conditions d'expédition

ambient

Température de stockage

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

Clé InChI

JMIFGARJSWXZSH-UHFFFAOYSA-N

Description générale

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Regulatory Review (Z)

Reconstitution

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

Autres remarques

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

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

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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