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Merck

616454

A 83-01

≥97% (HPLC), solid, TGF-β RI kinase inhibitor, Calbiochem

別名:

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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この商品について

実験式（ヒル表記法）:
C25H19N5S
CAS番号:
909910-43-6
分子量:
421.52
MDL number:
MFCD08705403
UNSPSC Code:
12352200
NACRES:
NA.54

主要文書

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製品名

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).

SMILES string

S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1

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)

InChI key

HIJMSZGHKQPPJS-UHFFFAOYSA-N

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 20 mg/mL

shipped in

ambient

Quality Level

200

storage temp.

2-8°C

Biochem/physiol Actions

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

Disclaimer

Toxicity: Harmful (C)

General description

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.

Other Notes

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

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

保管分類

11 - Combustible Solids

wgk

WGK 3

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

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文書ライブラリにアクセスする

Felix Kretzschmar et al.
Biology, 10(12) (2021-12-25)
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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グローバルトレードアイテム番号

カタログ番号GTIN
616454-2MGCN04055977185867

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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