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Merck

5.31237

IRAK4 Inhibitor, Compound 26

Synonim(y):

IRAK4 Inhibitor, Compound 26, Interleukin-1 Receptor Associated Kinase 4 Inhibitor

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Informacje o tej pozycji

Wzór empiryczny (zapis Hilla):
C25H27N5O2
Numer CAS:
Masa cząsteczkowa:
429.51
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
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assay

≥98% (HPLC)

Quality Level

form

powder

potency

94 pM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

pale yellow

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

General description

A cell permeable indolo[2,3-c]quinoline derivatived compound that acts as a selective and highly potent inhibitor of interleukin-1 receptor associated kinase (IRAK4; IC50 = 94 pM). Displays much reduced potency against IRAK1 (IC50 = 65 nM) and displays high selectivity over a panel of other 27 kinases, including several involved in TLR-mediated signaling. Blocks R848-induced TNF-α and IL-6 production in primary human monocytes and inhibits LPS-induced TNF-α production in mice (100 mpk). Shows minimal inhibition of Cyp2C9, 2D6, and 3A4 and has excellent microsomal stability and desirable aqueous solubility (100 μg/ml at pH 7.4).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
IRAK4
Reversible: yes

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.

Other Notes

Tumey, L.N., et al. 2014 Bioorg. Med. Chem. Lett. 24, 2066.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)
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Klasa składowania

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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