IKK 选择性抑制剂 | 调节剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S3615 Dehydrocostus Lactone

Dehydrocostus lactone (DHE), a natural sesquiterpene lactone, inhibits IKKβ activity, IκBα phosphorylation and degradation, coactivators p300 recruitments and p50/p65 NF-κB nuclear translocation, and their DNA binding activity on COX-2 promoter. It has anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.

S8922 TBK1/IKKε-IN-1(compound 1)

TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo.

Selective TBK1, IC50: 1.0 nM; IKKε, IC50: 5.6 nM
S8935 BAY-985

BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM).

Selective IKKε, IC50: 2 nM; TBK1, IC50: 2 nM; TBK1, IC50: 30 nM
S2824 TPCA-1

TPCA-1是一种IKK-2抑制剂,无细胞试验中IC50为17.9 nM,抑制NF-κB通路,比作用于IKK-1选择性高22倍。

Selective IKK2, IC50: 17.9 nM
S7697 LY2409881

LY2409881 是一种有效的选择性 IKK2 抑制剂,IC50 为 30 nM,选择性比IKK1和其他常见激酶高10倍多。

Selective IKK2, IC50: 30 nM
S2882 IKK-16 (IKK Inhibitor VII)

IKK-16 (IKK Inhibitor VII)是一种选择性的IκB激酶(IKK)抑制剂,作用于IKK-2IKK complexIKK-1,无细胞试验中IC50分别为40 nM,70 nM和200 nM。

Selective IKK2, IC50: 40 nM; IKK1, IC50: 200 nM; IKK complex, IC50: 70 nM
S7691 PS-1145

PS-1145是一种特异性IKK抑制剂,IC50 为 88 nM。

Selective IKK, IC50: 88 nM
S7948 MRT67307 HCl

MRT67307是一种高效的双重的IKKϵ /TBK1抑制剂,其IC50分别为160和19 nM。

Selective IKKϵ, IC50: 160 nM; TBK1, IC50: 190 nM
S8044 BMS-345541

BMS-345541是一种催化亚基的高选择性抑制剂,作用于IKK-2IKK-1,无细胞试验中IC50分别为0.3 μM和4 μM。

Selective IKK1, IC50: 4 μM; IKK2, IC50: 0.3 μM
S3168 cis-Resveratrol

cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA po

Selective IKKβ, IC50: 1 μM
S1396 Resveratrol (SRT501)

Resveratrol具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。

Selective IKK β, IC50: 1 μM
S6714 INH14

INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively.

Selective IKKα, IC50: 8.975 μM; IKKβ, IC50: 3.598 μM
S4907 SC-514

SC-514是一种口服有效的,ATP竞争性的IKK-2抑制剂,IC50为3-12 μM,抑制NF-κB依赖性的基因表达,不抑制其他IKK异构体或其他丝-苏氨酸和酪氨酸激酶。

Selective IKK2, IC50: 3 μM-12 μM
S3612 Rosmarinic acid

Rosmarinic acid (RA, Rosemary acid) is a naturally occurring hydroxylated compound. It has the ability to block complement fixation, inhibit lipoxygenase and cyclooxygenase activity and inhibit the expression of CCL11 and CCR3 by suppressing the IKK-β activity in NF-κB activation signaling.

Selective IKK β, IC50: 12 μM
S2864 IMD 0354

IMD 0354是一种IKKβ抑制剂,作用于NF-κβ通路,抑制IκBα磷酸化。

S8078 Bardoxolone Methyl

Bardoxolone Methyl是一种IKK抑制剂,具有强的促凋亡和抗炎活性。同时还是有效的Nrf2激活剂和NF-κB抑制剂。

S7441 WS3

WS3是一种β细胞增殖诱导剂,通过调节Erb3 binding protein-1 (EBP1)IκB kinase通路发挥作用。

S3648 Amlexanox (AA-673)

Amlexanox (AA-673, CHX-3673, Amoxanox) is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.

S7851 AZD3264


S0425 TBK1/IKKε-IN-2

TBK1/IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε.

S9417 Homoplantaginin

Homoplantaginin (Hispidulin-7-glucoside), a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

S7442 WS6

WS6通过调节Erb3 binding protein-1 (EBP1)IκB kinase通路诱导β细胞增殖。

S1681 Mesalamine (5-ASA)


S3298 Caulophylline (N-Methylcytisine)

Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation.