IKK-16

別名: IKK Inhibitor VII

目錄號(hào)：S2882 Purity: 99.07%

IKK-16是一種選擇性的IκB激酶(IKK)抑制劑，作用于IKK-2，IKK complex和IKK-1，無(wú)細(xì)胞試驗(yàn)中IC50分別為40 nM，70 nM和200 nM。IKK-16 還可抑制細(xì)胞內(nèi)LRRK2 Ser935的磷酸化和體外實(shí)驗(yàn)中LRRK2的激酶活性，對(duì)應(yīng)的IC50值為50 nM。

IKK-16 Chemical Structure

CAS: 873225-46-8

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1814.56	現(xiàn)貨
10mg	1405.59	現(xiàn)貨
50mg	5478.17	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次： S288201 DMSO]97 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false 純度： 99.07%

99.07

IKK-16相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	IκB IKK	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	BAY 11-7082 TPCA-1 Bay 11-7085 BMS-345541 IMD 0354 Bardoxolone Methyl MRT67307 HCl SC-514 LY2409881 TBK1/IKKε-IN-5 PS-1145 Dehydrocostus Lactone Wedelolactone WS6 BAY-985 AZD3264 WS3 TBK1/IKKε-IN-2 Rosmarinic acid	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	FDA藥物庫(kù) 免疫/炎癥分子化合物庫(kù) 小分子免疫腫瘤化合物庫(kù) NF-κB信號(hào)通路庫(kù) FDA抗癌藥物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	孵育時(shí)間	活性描述	文獻(xiàn)信息
bovine retinal endothelial cells	Function assay	30 mins	Inhibition of atypical PKCzeta in bovine retinal endothelial cells assessed as TNFalpha/VEGF-induced endothelial permeability preincubated for 30 mins followed by TNFalpha induction for 1 hr and VEGF induction for 30 mins measured every 30 mins for 4 hrs , EC50 = 0.002 μM.	23566515
HEK293	Function assay	3 hrs	Inhibition of atypical PKCzeta in HEK293 cells assessed as TNF-induced NFkappaB activation incubated for 3 hrs prior to TNF induction measured after 5 hrs by bright-glo luciferase reporter gene assay, EC50 = 0.003 μM.	23566515
HeLa	Function assay		Inhibitory activity against IKK complex isolated from HeLa cells, IC50 = 0.07 μM.	16236504
HUVEC	Function assay		Inhibition of TNF-alpha-stimulated expression of ICAM1 in HUVEC cells, IC50 = 0.3 μM.	16236504
HUVEC	Function assay		Inhibition of TNF-alpha-stimulated expression of VCAM1 in HUVEC cells, IC50 = 0.3 μM.	16236504
HUVEC	Function assay		Inhibition of TNF-alpha-stimulated expression of E-selectin in HUVEC cells, IC50 = 0.5 μM.	16236504
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
U-2 OS	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
NB1643	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

IKK2 ^[1] (Cell-free assay)	IKK complex ^[1] (Cell-free assay)	IKK1 ^[1] (Cell-free assay)
40 nM	70 nM	200 nM

體外研究(In Vitro)
體外研究活性	IKK-16抑制HUVEC細(xì)胞中TNFα刺激的黏附分子E-selectin, ICAM-1, 和VCAM-1的表達(dá)。盡管 IKK-16也具有抑制IFNγ誘導(dǎo)的β2 微球蛋白或HLA-DR表達(dá)的活性，但是其效價(jià)在這些分析中要低4-10倍。 ^[1]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	IKK-16 對(duì)大鼠和小鼠具有口服活性，在體內(nèi)可以抑制脂多糖誘導(dǎo)的TNF-α 的釋放，還可以抑制硫膠質(zhì)誘導(dǎo)的腹膜炎中中性粒細(xì)胞外滲^[1]。

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

參考文獻(xiàn)

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

化學(xué)信息&溶解度

分子量	483.63	分子式	C₂₈H₂₉N₅OS
CAS號(hào)	873225-46-8	SDF	Download IKK-16 SDF
Smiles	C1CCN(C1)C2CCN(CC2)C(=O)C3=CC=C(C=C3)NC4=NC=CC(=N4)C5=CC6=CC=CC=C6S5
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 97 mg/mL ( (200.56 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊(cè)

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