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407602

Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor

Name: Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor
Brand: MM

InSolution, ≥98%

别名:

InSolution Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor, N-(1-(2-morpholinoethyl)-1H-benzo[d]imidazol-2-yl)-3-nitrobenzamide, N-(2-Morpholinylethyl)-2-(3-nitrobenzoylamido)-benzimidazole

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关于此项目

经验公式（希尔记法）:

C₂₀H₂₁N₅O₄

化学文摘社编号:

509093-47-4

分子量:

395.41

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD09752602

Assay:

≥98% (HPLC)

Form:

liquid

Quality level:

100

Storage condition:

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

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属性

Quality Level

100

assay

≥98% (HPLC)

form

liquid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

shipped in

dry ice

storage temp.

−70°C

SMILES string

[N+](=O)([O-])c1cc(ccc1)C(=O)Nc2[n](c4c(n2)cccc4)CCN3CCOCC3

InChI

1S/C20H21N5O4/c26-19(15-4-3-5-16(14-15)25(27)28)22-20-21-17-6-1-2-7-18(17)24(20)9-8-23-10-12-29-13-11-23/h1-7,14H,8-13H2,(H,21,22,26)

InChI key

QTCFYQHZJIIHBS-UHFFFAOYSA-N

说明

General description

A cell-permeable benzimidazole compound that acts as a potent and selective inhibitor of interleukin-1 receptor-associated kinases (IC₅₀ = 300 nM and 200 nM for IRAK-1 and -4). Shown to exhibit little activity against a panel of 27 other kinases (IC₅₀ >10 µM), including lck and src. The solid form of this compound (Cat. No. 407601) is also available.

Biochem/physiol Actions

Primary Target
IRAK-1/4

Reversible: yes

Target IC₅₀: 300 nM and 200 nM for IRAK-1 and -4

Packaging

Packaged under inert gas

Preparation Note

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.

Other Notes

Srivastava, R., et al. 2012. Cancer Res.72, In press.
Bhattacharyya, S., et al. 2007. Am. J. Physiol. Gastrointest. Liver Physiol.293, G429.
Powers, J.P., et al. 2006. Bioorg. Med. Chem. Lett.16, 2842.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

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存储类别

10 - Combustible liquids

wgk

WGK 2

flash_point_f

188.6 °F - closed cup - (refers to pure substance)

flash_point_c

87 °C - closed cup - (refers to pure substance)

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Suppression of TLR signaling by IRAK-1 and -4 dual inhibitor decreases TPF-resistance-induced pro-oncogenic effects in HNSCC.

Humayara Khan et al.

3 Biotech, 13(1), 14-14 (2022-12-22)

Combination of docetaxel, cisplatin and 5-FU, known as TPF, is an FDA-approved treatment for head and neck squamous cell carcinoma (HNSCC). Acquired chemo-resistance to TPF, a primary reason for non-responsiveness to the treatment and relapse of tumor is a major

Augmentation of therapeutic responses in melanoma by inhibition of IRAK-1,-4.

Ratika Srivastava et al.

Cancer research, 72(23), 6209-6216 (2012-10-09)

Toll-like receptors (TLR) are expressed by a variety of cancers, including melanoma, but their functional contributions in cancer cells are uncertain. To approach this question, we evaluated the effects of stimulating or inhibiting the TLR/IL-1 receptor-associated kinases IRAK-1 and IRAK-4

Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.

Jay P Powers et al.

Bioorganic & medicinal chemistry letters, 16(11), 2842-2845 (2006-03-28)

High-throughput screening of a small-molecule compound library resulted in the identification of a novel series of N-acyl 2-aminobenzimidazoles that are potent inhibitors of interleukin-1 receptor-associated kinase-4.

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全球贸易项目编号

货号	GTIN
407602-5MG	04055977211306