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TGF-β RI Kinase Inhibitor IV

TGF-β RI Kinase Inhibitor IV, CAS 909910-43-6, is a cell-permeable, selective inhibitor of ALK-4/5/7-mediated signaling (IC₅₀ = 45, 12, and 7.5 nM, respectively).

Synonyme(s) :

TGF-β RI Kinase Inhibitor IV, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor IV, 3-(6-Methylpyridin-2-yl)-4-(4-quinolyl)-1-phenylthiocarbamoyl-1H-pyrazole, A-83-01, ALK5 Inhibitor IV

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About This Item

Formule empirique (notation de Hill):
C25H19N5S
Numéro CAS:
909910-43-6
Poids moléculaire :
421.52
Code UNSPSC :
12352200

Niveau de qualité

200

Pureté

≥97% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

pale yellow

Solubilité

DMSO: 20 mg/mL

Conditions d'expédition

ambient

Température de stockage

2-8°C

InChI

1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)

Clé InChI

HIJMSZGHKQPPJS-UHFFFAOYSA-N

Description générale

A cell-permeable trisubstituted pyrazole compound that has been shown to selectively inhibit ALK-4/5/7-mediated (IC50 = 45, 12, and 7.5 nM, respectively, in luciferase transcription activity assays), but not ALK-1/2/3/6-mediated cellular signaling in Mv1Lu R4-2 transfectants expressing the individual Type I TGF-β receptors. Inhibits TGF-β-induced Smad2-phosphorylation in HaCaT cells and epithelial-to-mesenchymal transition in NMuMG cells at a concentration of 1 µM.

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
ALK-4/5/7
Product does not compete with ATP.
Reversible: no
Target IC50: 45, 12, and 7.5 nM, respectively, in inhibit ALK-4/5/7-mediated luciferase transcription activity assays

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Tojo, M., et al. 2005. Cancer Sci.96, 791.

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

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Felix Kretzschmar et al.
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As resident innate immune cells of the CNS, microglia play important essential roles during physiological and pathological situations. Recent reports have described the expression of Lilrb4 in disease-associated and aged microglia. Here, we characterized the expression of Lilrb4 in microglia
Alexander von Ehr et al.
Frontiers in cellular neuroscience, 14, 66-66 (2020-04-17)
Microglia are constantly surveying their microenvironment and rapidly react to impairments by changing their morphology, migrating toward stimuli and adopting gene expression profiles characterizing their activated state. The increased expression of the M2-like marker Mannose receptor 1 (Mrc1), which is
Erin R Spiller et al.
Frontiers in oncology, 11, 771173-771173 (2022-01-08)
Three-quarters of compounds that enter clinical trials fail to make it to market due to safety or efficacy concerns. This statistic strongly suggests a need for better screening methods that result in improved translatability of compounds during the preclinical testing
Abdelraheim Attaai et al.
Glia, 66(8), 1695-1708 (2018-03-27)
Microglia are involved in a widespread set of physiological and pathological processes and further play important roles during neurodevelopmental events. Postnatal maturation of microglia has been associated with the establishment of microglia-specific gene expression patterns. The mechanisms governing microglia maturation
Julian Heuberger et al.
EMBO molecular medicine, 13(4), e13191-e13191 (2021-02-06)
SARS-CoV-2, the agent that causes COVID-19, invades epithelial cells, including those of the respiratory and gastrointestinal mucosa, using angiotensin-converting enzyme-2 (ACE2) as a receptor. Subsequent inflammation can promote rapid virus clearance, but severe cases of COVID-19 are characterized by an
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