BI 605906 - ≥98%(HPLC), high purity , CAS No.960293-88-3, Inhibitor of inhibitor of nuclear factor kappa B kinase subunit beta

Item Number

B287053

• Synonyms: 3-Amino-4-(1,1-difluoropropyl)-6-[4-(methylsulfonyl)-1-piperidinyl]thieno[2,3-b]pyridine-2-carboxamide
• Specifications & Purity: Moligand™, ≥98%(HPLC)
• Biochemical and Physiological Mechanisms: Selective IKKβinhibitor (IC50= 380 nM). Displays no effect on a panel of 100 kinases, except at IGF1 (IC50= 7.6μM).
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of inhibitor of nuclear factor kappa B kinase subunit beta

Product Description

BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.BI605906 is an inhibitor of IKKβ with improved selectivity. BI605906 inhibits IKKβ in vitro with an IC50 value of 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that is inhibited of over 100 tested, which include IKKα, IKKε and TBK1, is the insulin-like growth factor 1 (IGF1) receptor (IC50=7.6 μM). BI605906 partially inhibits the IL-1-stimulated activation of IKKε/TBK1. In primary mouse hepatocytes, Metformin treatment for 3 hours suppresses TNFα-induced degradation of the NF-κB negative regulator IκB, while modulating AMPK and MTOR signaling in a dose-dependent manner. The magnitude of the effect on IκB is comparable with BI605906. Unlike Metformin, BI605906 (10 μM ) does not suppress signaling downstream of mTOR nor does it activate AMPK. TNF-α-dependent expression of CINC-1/CXCL1, CXCL2, IL-1β, and IL-6 is strongly inhibited by both Metformin and BI605906 (10 μM).