Biaffin

Newsletter

kinases protein kinase inhibitors signaling activators kinase substrates antibodies bioluminescence assays
JNK inhibitor VIII, 1 mg  

JNK inhibitor VIII, 1 mg

N-(4-Amino-5-cyano-6-ethoxy-2-pyridinyl)-2,5-dimethoxybenzeneacetamide

 potent ATP-competitive inhibitor of JNK1, JNK2 and JNK3

More details

PKI-JNKI-001

95,00 €

Background: JNK inhibitor VIII is an aminopyridine-based compound acting as potent ATP-competitive inhibitor of JNK1, JNK2 and JNK3 (Ki = 2nM, 4 nM and 52 nM). Due to a different hydrogen-bonding network of these kinase ATP-site ligands a >1000-fold selectivity.
for JNK over other MAP kinases was achieved. The compound inhibited the phosphorylation of c-Jun, a direct substrate of JNK (EC50 = 920 nM).

Chemical formula: C18H20N4O4
Chemical Name:    N-(4-Amino-5-cyano-6-ethoxy-2-pyridinyl)-2,5-dimethoxybenzeneacetamide
Molecular Weight: 356.38 g/mol
Purity:  >95%
CAS no.  894804-07-0
Appearance:  brown solid
Solubility: Soluble to 100 mM in DMSO

Product specific literature references:
Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM. (2006) “Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.” J Med Chem. 2006 Jun 15;49(12):3563-80.

Kauskot A, Adam F, Mazharian A, Ajzenberg N, Berrou E, Bonnefoy A, Rosa JP, Hoylaerts MF, Bryckaert M.(2007) “Involvement of the mitogen-activated protein kinase c-Jun NH2-terminal kinase 1 in thrombus formation.” J Biol Chem.;282(44):31990-9.

Liu G, Zhao H, Liu B, Xin Z, Liu M, Kosogof C, Szczepankiewicz BG, Wang S, Clampit JE, Gum RJ, Haasch DL, Trevillyan JM, Sham HL. (2006) “Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.” Bioorg Med Chem Lett.;16(22):5723-30.

Turpeinen T, Nieminen R, Moilanen E, Korhonen R. “Mitogen-activated protein kinase phosphatase-1 negatively regulates the expression of interleukin-6, interleukin-8, and cyclooxygenase-2 in A549 human lung epithelial cells.” (2010) J Pharmacol Exp Ther.;333(1):310-8.

 

The following products could also be interesting for you: