1042224-63-4 Usage
Biological Activity
the interleukin-1 receptor associated kinase (irak) family is comprised of four family members irak-1, irak-2, irak-3/m, and irak-4. upon activation of their upstream cognate receptors, irak-4 is thought to phosphorylate irak-1 resulting in the activation and autophosphorylation of irak-1 an subsequent phosphorylation of downstream substrates. irak inhibitor 1 is an inhibitor of interleukin-1 receptor associated kinase 4 (irak-4).
in vitro
the regioisomeric pyridines irak inhibitor 1 (6) and it analogue (7) showed contrasting sar, with the 2,6-pyridine isomer irak inhibitor 1 having low-nanomolar potency whilst the 2,4-pyridine isomer 7 showed little activity, despite having a more accessible bidentate-binding motif. at 10 μm, irak inhibitor 1 was found to have 39% inhibition for jnk-1 and 15% inhibition for jnk-2, respectivley [1].
IC 50
35 nm for irak-4
references
[1] buckley gm, ceska ta, fraser jl, gowers l, groom cr, higueruelo ap, jenkins k, mack sr, morgan t, parry dm, pitt wr, rausch o, richard md, sabin v. irak-4 inhibitors. part ii: a structure-based assessment of imidazo[1,2-a]pyridine binding. bioorg med chem lett. 2008;18(11):3291-5.
Check Digit Verification of cas no
The CAS Registry Mumber 1042224-63-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,4,2,2,2 and 4 respectively; the second part has 2 digits, 6 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1042224-63:
(9*1)+(8*0)+(7*4)+(6*2)+(5*2)+(4*2)+(3*4)+(2*6)+(1*3)=94
94 % 10 = 4
So 1042224-63-4 is a valid CAS Registry Number.
1042224-63-4Relevant academic research and scientific papers
Buckley, George M.,Ceska, Thomas A.,Fraser, Joanne L.,Gowers, Lewis,Groom, Colin R.,Higueruelo, Alicia Perez,Jenkins, Kerry,Mack, Stephen R.,Morgan, Trevor,Parry, David M.,Pitt, William R.,Rausch, Oliver,Richard, Marianna D.,Sabin, Verity
, p. 3291 - 3295 (2008)
A potent IRAK-4 inhibitor was identified through routine project cross screening. The binding mode was inferred using a combination of in silico docking into an IRAK-4 homology model, surrogate crystal structure analysis and chemical analogue SAR.
