IKK-16

製品コードS2882 バッチS288201

印刷

化学情報

Synonyms

IKK Inhibitor VII

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₈H₂₉N₅OS

分子量

483.63

CAS No.

873225-46-8

Solubility (25°C)*

体外

DMSO

97 mg/mL (200.56 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	30.000mg/ml (62.03mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	IKK-16 is a selective IκB 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. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in vitro with IC50 of 50 nM.
in vitro	IKK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. Although this compound shows activity in the IFNγ-induced expression of β2 microglobulin or HLA-DR, its potency in these assays is 4- to 10-fold weaker. ^[1]
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.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度
	反応時間
	実験の流れ	40, 70 and 200 nM (IC50) for IKK-2, this compound and IKK-1
動物実験	動物モデル	Rats & Mice
	投薬量	30 mg/kg
	投与方法	s.c. & p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/16236504/

カスタマーフィードバック

: Data from [Data independently produced by , , J Immunol, 2016, 197(3):726-35.]

: Data from [Data independently produced by , , Cell Transplant, 2014, 23(4-5): 641-56]

: Data from [Data independently produced by , , Biomol Ther (Seoul), 2016, 24(2):132-9.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Phosphorylation of H3.3 at Serine 31 acts as a switch of nucleosome dynamics for transcription [ Nucleic Acids Res, 2025, 53(17)gkaf891]	PubMed: 40966506
Molecular control of PDPNhi macrophage subset induction by ADAP as a host defense in sepsis [ JCI Insight, 2025, e186456]	PubMed: 39903516
TLR4 endocytosis and endosomal TLR4 signaling are distinct and independent outcomes of TLR4 activation [ EMBO Rep, 2025, 10.1038/s44319-025-00444-2]	PubMed: 40204912
Nbeal2 Inactivation Triggers Abl1 Stabilisation and Dysregulated Subcellular Localisation of the Multi-Drug-Resistant Protein MDR1 (ABCB1) in Mast Cells [ Immunology, 2025, NONE]	PubMed: 41111259
Monoclonal Antibodies to Thyrotropin Receptor With Thyroid-Stimulating Activity Activate the NF-κB Pathway to Induce Chemokine Expression [ J Cell Mol Med, 2025, 29(11):e70647]	PubMed: 40500868
Noncanonical role of Golgi-associated macrophage TAZ in chronic inflammation and tumorigenesis [ Sci Adv, 2025, 11(4):eadq2395]	PubMed: 39841821
Genetic mechanisms of resistance to targeted KRAS inhibition [ bioRxiv, 2025, 2025.08.04.668444]	PubMed: 40799582
Hypoxia-induced histone methylation and NF-κB activation in pancreas cancer fibroblasts promote EMT-supportive growth factor secretion [ bioRxiv, 2025, 2025.01.30.635486]	PubMed: 39974981
Size- and polymer-dependent toxicity of amorphous environmentally relevant micro- and nanoplastics in human bronchial epithelial cells [ Microplast nanoplast, 2025, 5(1):19]	PubMed: 40385552
Linear ubiquitination mediates coronavirus NSP14-induced NF-κB activation [ Cell Commun Signal, 2024, 22(1):573]	PubMed: 39616385

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。