product name IKK-16
Description: IKK-16 (also known as IKK Inhibitor VII) is a novel , potent and selective IκBα kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. In addition, IKK-16 has been found to be active at thioglycollate-induced peritonitis model in the mouse. Furthermore, IKK-16 has revealed to be an orally bio-available in rats and mice, and have significant in vivo activity in an acute model of cytokine release.
References: Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12.
483.63
Formula
C28H29N5OS
CAS No.
873225-46-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 97 mg/mL (200.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: IKK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although IKK-16 shows activity in the IFNγ-induced expression of β2 microglobulin or HLA-DR, its potency in these assays is 4- to 10-fold weaker. Kinase Assay: Cell Assay: IKK-16 (IKK Inhibitor VII) inhibited IKK2 by the blockade of IκBα degradation and suppressed TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Moreover, IKK-16 also showed activity in the IFNγ-induced expression of the MHC molecules β2 microglobulin and HLA-DR, but its potency in these assays is 4- to 10-fold weaker than the adhesion molecules assay. |
|---|---|
| In Vivo | IKK-16 is orally bio-available in rats and mice, and it inhibits LPS-induced TNF-α release in vivo and neutrophil extravasion in thioglycollate-induced peritonitis |
| Animal model | Rat model; thioglycollate-induced peritonitis model in the mouse |
| Formulation & Dosage | 30 mg/kg; s.c. injection or oral administration |
| References | Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. |
