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）

Clear solution

30%PEG400 1 0.5%Tween80 2 5%propylene glycol

30.0mg/ml

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 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. ^[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, IKK complex 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

[1] Waelchli R, et al. Bioorg Med Chem Lett, 2006, 16(1), 108-112.

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：

FAT10 is phosphorylated by IKKβ to inhibit the antiviral type-I interferon response [ Life Sci Alliance, 2024, 10.26508/lsa.202101282]	PubMed: 37940187
Serotonin reduction in post-acute sequelae of viral infection [ Cell, 2023, 186(22):4851-4867.e20]	PubMed: 37848036
Intestinal epithelial HDAC3 and MHC class II coordinate microbiota-specific immunity [ J Clin Invest, 2023, 133(4)e162190]	PubMed: 36602872
Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding [ SCIENCE ADVANCES, 2023, Vol-9,-Issue-12]	PubMed: None
Integrated single-cell (phospho-)protein and RNA detection uncovers phenotypic characteristics and active signal transduction of human antibody secreting cells [ Mol Cell Proteomics, 2023, S1535-9476(23)00001-4]	PubMed: 36623694
Ectopic CH60 mediates HAPLN1-induced cell survival signaling in multiple myeloma [ Life Sci Alliance, 2023, 6(3)e202201636]	PubMed: 36625202
Breast tumors interfere with endothelial TRAIL at the premetastatic niche to promote cancer cell seeding [ Sci Adv, 2023, 9(12):eadd5028]	PubMed: 36947620
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909]	PubMed: none
The RNF26/CBX7 axis modulates the TNF pathway to promote cell proliferation and regulate sensitivity to TKIs in ccRCC [ Int J Biol Sci, 2022, 18(5):2132-2145]	PubMed: 35342353
Proteomic identification of proliferation and progression markers in human polycythemia vera stem and progenitor cells [ Blood Adv, 2022, bloodadvances.2021005344]	PubMed: 35008095

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。