6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine
6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine Basic information
- Product Name:
- 6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine
- Synonyms:
-
- 6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine
- Cyclopamine inhibitor 1
- IRAK inhibitor 1
- 2-PyridinaMine, 6-iMidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-
- 2-a]pyridin-3-yl-N-4-piperidinyl-
- 6-imidazo[1
- IRAK inhibitor
- IRAK inhibitor 1,Inhibitor,inhibit,Interleukin-1 receptor associated kinase,IL-1R associated kinase,IRAK inhibitor1,IRAK inhibitor-1,IRAK
- CAS:
- 1042224-63-4
- MF:
- C17H19N5
- MW:
- 293.37
- Mol File:
- 1042224-63-4.mol
6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine Chemical Properties
- Density
- 1.32
- storage temp.
- Store at -20°C
- solubility
- insoluble in EtOH; insoluble in H2O; ≥14.4 mg/mL in DMSO
- form
- Powder
- pka
- 9.94±0.10(Predicted)
- color
- Light yellow to yellow
6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine Usage And Synthesis
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].
target
IRAK-4
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.
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