IRAK-1/4 INHIBITOR I Chemical Properties

Density 

1.40

storage temp. 

2-8°C

solubility 

DMSO: ≥5mg/mL

form 

Yellow crystalline solid

pka

11.54±0.43(Predicted)

color 

off-white to light yellow

Safety Information

Hazard Codes 

T

Risk Statements 

25-36/37/38

Safety Statements 

26-36/37-45

RIDADR 

UN 2811 6.1/PG 3

WGK Germany 

3

IRAK-1/4 INHIBITOR I Usage And Synthesis

Uses

IRAK-1/4 Inhibitor (interleukin-1 receptor-associated kinases) are important mediators in signal transduction of TIR family members. This regulation protects against the development of cancers and other diseases.

Uses

IRAK-1/4 inhibitor I has been used in various studies to inhibit IRAK1 in hepatoma cell lines and head and neck squamous cell carcinoma (HNSCC) cell lines.

Biological Activity

irak-1-4 inhibitor i is an inhibitor of both irak-1 and irak-4 with ic50 values of 0.3μm and 0.2μm , respectively [1].il-1 receptor-associated kinases play important roles in signal transduction. there are totally four members of the iraks, they are irak-1, irak-2, irak-m and irak-4. irak-4 can activate nf-κb and mapk pathways and it is shown that the inhibition of irak-4 can be an anti-inflammatory therapy. irak-1-4 inhibitor i is an analog of an initial irak-4 inhibitor hit, which is screened out from a small molecule li brary against irak-4. with the less basic n-ethylenemorpholine moiety, irak-1-4 inhibitor i has a higher potency than other analogs. additionally, it does not show any cytotoxicity in a 72 h proliferation assay in hela cells(ed50 >30μm) [1].

Biochem/physiol Actions

IRAK1 overexpression leads to the development of head and neck squamous cell carcinoma (HNSCC). Therefore, IRAK-1/4 inhibitor I might be a potential therapeutic for HNSCC tumors. Various experimental studies states that IRAK-1/4 inhibitor might have a potential to exhibit?inhibitory effects on the nuclear factor (NF)-κB signaling pathway.

storage

Store at -20°C

References

[1] jay p. powers, shyun li, juan c. jaen, jinqian liu, nigel p. c. walker, zhulun wang and holger wesche. discovery and initial sar of inhibitors of interleukin-1 receptor-associated kinase-4. bioorganic & medicinal chemistry letters. 2006, 16: 2842–2845.

IRAK-1/4 INHIBITOR I(509093-47-4)Related Product Information

• DEMETON S
• 6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine
• N-[2-Methoxy-4-(4-morpholinyl)phenyl]-2-(3-pyridinyl)-4-thiazolecarboxamide
• 4-[[[3-(3,4-Dimethoxyphenyl)imidazo[1,2-b]pyridazin-6-yl]amino]methyl]benzenesulfonamide
• 4-[6-[[(Furan-2-yl)methyl]amino]imidazo[1,2-b]pyridazin-3-yl]phenol
• IRAK-1/4 INHIBITOR I
• 1-(2-DIETHYLAMINO-ETHYL)-1H-BENZOIMIDAZOL-2-YLAMINE