All Photos(1)
Synonym(s):
3-Amino-4-(1,1-difluoro-propyl)-6-(4-methanesulfonyl-piperidin-1-yl)-thieno[2,3-b]pyridine-2-carboxylic acid amide, 3-Amino-4-(1,1-difluoropropyl)-6-[4-(methylsulfonyl)-1-piperidinyl]-thieno[2,3-b]pyridine-2-carboxamide, BI 605906, BI-605906
Empirical Formula (Hill Notation):
C17H22F2N4O3S2
CAS Number:
Molecular Weight:
432.51
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
, White to very dark gray
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
CCC(F)(C1=C2C(SC(C(N)=O)=C2N)=NC(N3CCC(CC3)S(C)(=O)=O)=C1)F
Biochem/physiol Actions
BI605906 is a selective, ATP-competitive IκB kinase β (IKK2, IKKβ, IKK-beta) inhibitor (IC50 = 380 nM, [ATP] = 0.1 mM) with no potency toward 100 other kinases, including IKKα, IKKε, TBK1, and IGF1R (IC50 ≥7.6 µM). BI605906 (10 µM) effectively blocks IKK-β-dependent phosphorylation of IKKε and TBK1 in IKKα-/- MEFs upon IL-1α (5 ng/mL) induction.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Kristopher Clark et al.
The Biochemical journal, 434(1), 93-104 (2010-12-09)
Members of the IKK {IκB [inhibitor of NF-κB (nuclear factor κB)] kinase} family play a central role in innate immunity by inducing NF-κB- and IRF [IFN (interferon) regulatory factor]-dependent gene transcription programmes required for the production of pro-inflammatory cytokines and
Amy R Cameron et al.
Circulation research, 119(5), 652-665 (2016-07-16)
The diabetes mellitus drug metformin is under investigation in cardiovascular disease, but the molecular mechanisms underlying possible benefits are poorly understood. Here, we have studied anti-inflammatory effects of the drug and their relationship to antihyperglycemic properties. In primary hepatocytes from
Raid B Nisr et al.
Cellular and molecular life sciences : CMLS, 76(24), 4887-4904 (2019-05-19)
Sustained nutrient (fuel) excess, as occurs during obesity and diabetes, has been linked to increased inflammation, impaired mitochondrial homeostasis, lipotoxicity, and insulin resistance in skeletal muscle. Precisely how mitochondrial dysfunction is initiated and whether it contributes to insulin resistance in
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