SML1138

IKK-16 dihydrochloride

≥98% (HPLC)

• 別名: N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide dihydrochloride, IKK16 hydrochloride
• 実験式（ヒル表記法）: C₂₈H₂₉N₅OS · 2HCl
• CAS番号: 873225-46-8
• 分子量: 556.55
• UNSPSCコード: 12352200
• PubChem Substance ID: 329825674

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: powder
• 保管条件: desiccated
• 色: white to beige
• 溶解性: DMSO: 20 mg/mL, clear
• 保管温度: −20°C
• SMILES記法: O=C(N1CCC(N2CCCC2)CC1)C3=CC=C(NC4=NC=CC(C5=CC(C=CC=C6)=C6S5)=N4)C=C3.C
• InChI: 1S/C28H29N5OS.CH4/c34-27(33-17-12-23(13-18-33)32-15-3-4-16-32)20-7-9-22(10-8-20)30-28-29-14-11-24(31-28)26-19-21-5-1-2-6-25(21)35-26;/h1-2,5-11,14,19,23H,3-4,12-13,15-18H2,(H,29,30,31);1H4
• InChI Key: YJGZKHHCMOHIFA-UHFFFAOYSA-N

詳細

アプリケーション

IKK-16 dihydrochloride has been used as an nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor kinase inhibitor (IκB) in B220+ CKO or CreWT naive B cells. It has also been used as a nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB inhibitor) in poly(I:C) transfection-induced retinoic acid-inducible gene (RIG-I), melanoma differentiation-associated gene 5 (MDA-5), and caspase-11 expressing mouse embryonic fibroblasts (MEFs).

生物化学的／生理学的作用

IKK-16 is a selective inhibitor of IKB kinase (IKK), part of the upstream NF-KB signal transduction cascade involved in the cellular response to inflammation. IKK-16 has IC₅₀ values of 40, 70 and 200 nM for IKKβ (IKK-2), IKK complex and IKKα (IKK-1) respectively. In a mouse sepsis model, IKK-16 reduced the multiple organ dysfunction, showing an antiinflammatory and endothelial protective effect likely mediated by inhibition of inflammation through NF-KB. IKK-16 has also been found to have some activity as an inhibitor of protein kinase D (PKD) and of multidrug resistance protein 1 (MDR1, ABCB1).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable