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IRAK-1-4 Inhibitor I

Catalog No. T2457 CAS 509093-47-4

Synonyms: IRAK-1/4 Inhibitor I, IRAK-1/4 Inhibitor

IRAK-1-4 Inhibitor I is a dual inhibitor of IRAK4 and IRAK1.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

IRAK-1-4 Inhibitor I, CAS 509093-47-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 112.00
25 mg	In stock	$ 258.00
50 mg	In stock	$ 486.00
100 mg	In stock	$ 695.00
500 mg	In stock	$ 1,490.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 100%

Purity: 99.89%

Purity: 98.77%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	IRAK-1-4 Inhibitor I is a dual inhibitor of IRAK4 and IRAK1.
Targets&IC50	IRAK1:0.2 μM, IRAK4:0.3 μM
In vitro	IRAK-1-4 Inhibitor I has IC50 greater than the highest concentration tested (10 μM) against a panel of 27 other kinases, including the most closely homologous (outside of the IRAK family) Lck and pp60SRC. Additionally, IRAK-1-4 Inhibitor I does not show any signs of cytotoxicity in a 72 h proliferation assay in HeLa cells (ED50>30 μM). Significant inhibition of IRAK-1 is observed with IRAK-1-4 Inhibitor I (IRAK-1 IC50=0.3 μM)[1]. IRAK-1/4 inhibitor eliminates the LPS-induced increases in Bcl10, NF-κB, and IL-8. IRAK-1/4 mediates LPS-induced IL-8 activation and functions upstream of Bcl10. The LPS-induced increase in Bcl10 declines by 73% (from 5.18±0.22 to 2.36±0.08 ng/mL), and the IL-8 response decline by 60% (from 2.64±0.31 to 1.14±0.08 ng/mL)[2].
Kinase Assay	Kinase Assays: Cell-free kinase assays are done in quadruplicate with 1 μM ATP to determine the IC50 values of AV-951 against a variety of recombinant receptor and nonreceptor tyrosine kinases including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFRβ, Flt-3 and FGFR1.
Cell Research	IRAK-1-4 Inhibitor I is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. NCM460 cells, grown in 24-well plates, are incubated with 50 μM IRAK-1/4 inhibitor for 2 h. After 2 h, the media are changed, and new media with or without LPS (10 ng/mL) added. Treatment is terminated at 6 h, and spent media and cells are collected for IL-8 and other assays[2].

Synonyms	IRAK-1/4 Inhibitor I, IRAK-1/4 Inhibitor
Molecular Weight	395.41
Formula	C20H21N5O4
CAS No.	509093-47-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.9 mg/mL(20 mM)

References and Literature

1. Powers JP, et al. Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2842-2845. 2. Bhattacharyya S, et al. Bcl10 mediates LPS-induced activation of NF-kappaB and IL-8 in human intestinal epithelial cells. Am J Physiol Gastrointest Liver Physiol. 2007 Aug;293(2):G429-37. 3. Wu X, Xu M, Liu Y, et al. Dual Pharmacological Inhibition of IRAK1 and IRAK4 Prevents LPS Induced Monocyte Adhesion to Endothelial Cells[J]. bioRxiv. 2021

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Antidepressant Compound Library Anti-Ovarian Cancer Compound Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library Anti-Infection Compound Library Kinase Inhibitor Library Anti-Cancer Compound Library Anti-COVID-19 Compound Library NF-κB Signaling Compound Library

Related Products

Related compounds with same targets

GLPG2534 IRAK inhibitor 6 IRAK inhibitor 3 AS-2444697 IRAK4-IN-20 IRAK4-IN-8 IRAK4-IN-26 HS271

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Keywords

IRAK-1-4 Inhibitor I 509093-47-4 Immunology/Inflammation NF-Κb IRAK IRAK-1/4 Inhibitor I inhibit Interleukin-1 receptor associated kinase IRAK 1 4 Inhibitor I IRAK-1/4 Inhibitor IRAK14 Inhibitor I IL-1R associated kinase Inhibitor inhibitor

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