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35

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T63919	IKKβ-IN-1
	IKKβ-IN-1 是一种有效的、口服具有活力的 IkappaB(IKK-β) 抑制剂 (IC50: 0.20 μM)。IKKβ-IN-1 能够减少抑制小鼠巨噬细胞中 PGE2和 TNF-α的产生。IKKβ-IN-1 对小鼠具有保护作用，使其免受感染性休克诱导的死亡。
T6176	IKK 16 IKK Inhibitor VII,IKK-16,IKK16	IκB/IKK; LRRK2	Autophagy; NF-κB
	IKK 16 (IKK Inhibitor VII) 是一种选择性的 IκB 激酶 (IKK) 抑制剂，作用于 IKK2、IKK complex 和 IKK1，IC50分别为 40 nM、70 nM 和 200 nM。它还抑制富亮氨酸重复激酶 2，IC50为 50 nM。
T36524	IKK2-IN-4 5-Phenyl-2-ureidothiophene-3-carboxylic Acid Amide,IKK2 Inhibitor IV	IκB/IKK; TNF	Apoptosis; NF-κB
	IKK2-IN-4 (IKK2 Inhibitor IV)是一种高效的 IKK-2 抑制剂，IC50 值为 25 nM。IKK2-IN-4 对 LPS 诱导的 PBMC 中 TNFα 的产生有抑制作用。
TP1615L	IKKγ NBD Inhibitory Peptide acetate IKKγ NBD Inhibitory Peptide acetate(372146-18-4 free base)	NF-κB	NF-κB
	IKKγ NBD Inhibitory Peptide acetate 是一种 NEMO 结合结构域肽（NBD 肽）乙酸盐，对应于 NEMO 氨基末端 α-螺旋区域。它显示可阻断 TNF-α 诱导的 NF-kB 活化。
T15559	TBK1/IKKε-IN-2	IκB/IKK	NF-κB
	TBK1/IKKε-IN-2 是双重TBK1和IKKε抑制剂。
T7951	TBK1/IKKε-IN-5	IκB/IKK	NF-κB
	TBK1/IKKε-IN-5 是一种 TBK1 (IC50:1 nM) 和 IKKε (IC50:5.6 nM) 的双抑制剂。
T6150	TAK-715	p38 MAPK; Casein Kinase; JNK	MAPK; Metabolism; Stem Cells
	TAK-715 是一种具有口服活性的p38 MAPK 抑制剂，对 p38α 和 p38β 的IC50分别为 7.1 nM 和200 nM。它抑制酪蛋白激酶 I (CK1δ/ε)，调节 Wnt/β-catenin 信号传导的激活，有抗炎活性。
T40700	IKK-IN-3
	IKK-IN-3 is a highly potent and selective inhibitor of IkappaB kinase 2 (IKK2 or IKKβ). It exhibits impressive inhibitory activity against IKK2 (IC50 = 19 nM), while also demonstrating significant efficacy against IKK1 (or IKKα) with an IC50 value of 400 nM.
T61059	IKK-IN-4
	IKK-IN-4 是IkappaB 激酶2的选择性抑制剂，其对 IKKβ 和 IKKα 的IC50值分别为 45 nM 和 650 nM。
T39841	TBK1/IKKε-IN-6 TBK1/IKKε-IN-6
	TBK1/IKKε-IN-6 (example 110) is a potent inhibitor of TBK1 and IKKε, with IC50 values of less than 100 nM for both enzymes.
T38263	TBK1/IKKε-IN-4 TBK1/IKKε-IN-4
	TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1/IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1/IK...
T71747	IKKß-IN-124
	IKKß-IN-124 is an allosteric inhibitor of IκBα phosphorylation and NF-κB transcriptional activity through selective capture of the inactive conformation and hence blockade of IKKβ S177/S181 phosphorylation.
T76024	IKKγ NBD Inhibitory Peptide TFA
	IKKγ NBD 抑制肽 TFA 是一种高度特异性的NF-κB 抑制剂。IKKγ NBD 抑制肽 TFA 通过阻断 IKKγ/NEMO 结合域 (NBD) 与 IKKα 和 IKKβ 之间的相互作用，而阻断 TNF-α 诱导的NF-κB 激活。IKKγ NBD 抑制肽 TFA 可显著降低炎症、改善脑缺血所致的神经功能缺损。
TQ0306	MLN120B	IκB/IKK	NF-κB
	MLN120B 是一种ATP 竞争性的、有效的、具有口服活性的IKKβ抑制剂，IC50=60 nM。它在体内外抑制多发性骨髓瘤细胞生长，也可用于研究类风湿关节炎。
T5209	INH14	IκB/IKK	NF-κB
	INH14 是 IKKα (IC50:8.97 μM) / IKKβ (IC50:3.59 μM) 的抑制剂。它能够抑制 IKKα/β 依赖性 TLR 炎症反应，抑制 TAK1/TAB1 的下游和 NF-kB 信号通路。它具有抗炎和抗癌作用。
T8910	2-AMINO-5-PHENYL-THIOPHENE-3-CARBOXYLIC	IκB/IKK	NF-κB
	2-AMINO-5-PHENYL-THIOPHENE-3-CARBOXYLIC 是 IKKβ 的抑制剂。
T6141	IMD-0354 IKK2 Inhibitor V,IMD 0354	IκB/IKK	NF-κB
	IMD-0354 (IKK2 Inhibitor V) 是一种选择性IKKβ抑制剂，能够抑制 NF-κB 活性。它能够抑制 TNF-α 诱导的 NF-κB 转录活性，IC50=1.2 μM。
T125120	Cyclo(L-Pro-L-Val)	IκB/IKK; NOS; NF-κB; COX; Antibacterial	Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB
	Cyclo(L-Pro-L-Val) 是从辣椒溶杆菌AZ2和白斑分枝杆菌果实中提取出的 2,5-二酮哌嗪，具有抗炎活性，对植物病原微生物 (如 R. fascians LMG 3605) 具有毒性活性，能抑制革兰氏阳性植物病原菌。Cyclo(L-Pro-L-Val) 以浓度依赖性方式显著抑制了IKKα、IKKβ、IκBα和NF-κB 的磷酸化以及iNOS 和COX-2的活化，是治疗炎症相关疾病的潜在治疗剂。
T14567	BI605906	IκB/IKK	NF-κB
	BI605906 is an inhibitor of IKKβ. When assayed at 0.1 mM ATP, the IC50 value is 380 nM.
T23137	PF 184	Others	Others
	IKKβ inhibitor
T14669	BMS-066	IκB/IKK; Tyrosine Kinases	NF-κB; Tyrosine Kinase/Adaptors
	BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
T10237	ACHP Hydrochloride IKK-2 Inhibitor VIII	IκB/IKK	NF-κB
	ACHP Hydrochloride (IKK-2 Inhibitor VIII) 是选择性的IKK-β抑制剂 (IC50=5.8 nM)。
T14508	Bay 65-1942 hydrochloride	IκB/IKK	NF-κB
	Bay 65-1942 hydrochloride is an inhibitor of ATP-competitive and selective IKKβ.
T10472L	Bay 65-1942 free base	IκB/IKK	NF-κB
	Bay 65-1942 free base is an inhibitor of ATP-competitive and selective IKKβ.
T10472	Bay 65-1942 (R form) Bay 65-1942 R form	Others	Others
	Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is a selective and ATP-competitive IKKβ inhibitor.
T37449	SR 12460
	SR 12460 is a mimetic of the IκB kinase β (IKKβ) NEMO/IKKγ-binding domain (NBD) that inhibits the protein-protein interaction between the IKK complex subunits NF-κB essential modulator (NEMO/IKKγ) and IKKβ.1It inhibits TNF-α-induced NF-κB activation in a reporter assay when used at concentrations ranging from 25 to 150 μM. It reduces LPS-induced production of IL-6 in RAW 264.7 cells. SR 12460 (30 mg/kg) improves grip strength in themdxmouse model of Duchenne muscular dystrophy. 1.Zhao, J., Zhang...
T39199	ML 120B dihydrochloride ML120B dihydrochloride
	MLN120B dihydrochloride (ML120B dihydrochloride) is a highly potent, orally active inhibitor of IKKβ. It competitively binds to ATP and exhibits an impressive IC50 value of 60 nM. This compound effectively suppresses the growth of multiple myeloma cells both in vitro and in vivo. Furthermore, MLN120B dihydrochloride is valuable in the field of rheumatoid arthritis research.
T78371	Ac2-26 ammonium
	Ac2-26 ammonium是一种具抗炎作用的annexin 1 N末端肽。该化合物能够通过伴侣介导的自噬(CMA)机制降低溶酶体中的IKKβ蛋白含量，从而改善肺缺血再灌注损伤，并在哮喘大鼠模型中抑制气道炎症以及高反应性的表现。
T36192	CAY10682
	(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 (Ki = 83 nM) and also dose-dependently reduces activation of the NF-κB pathway. It specifically prevents phosphorylation of IκBα by the kinases IKKα, IKKβ, and IKK (IC50s = 80.5, 78.2, and 57.1...
T38158	StA-IFN-1
	StA-IFN-1 is an inhibitor of the interferon (IFN) induction pathway with an IC50 value of 4.1 μM in a GFP reporter assay for IFN induction similar to TPCA-1 , which specifically inhibits the IKKβ component of the IFN induction pathway. It does not show inhibitory activity in a GFP reporter assay for IFN signaling in which ruxolitinib , which is specific for the IFN signaling component JAK1, is active. StA-IFN-1 reduces the levels of IFN-β, but not ISG MxA, mRNA, suggesting that it is selective f...
T83670	F1 TFA Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide
	F1是一种抗炎肽，由HIV-1 Tat蛋白质转导域与对应于抑制因子NF-κB激酶-相互作用肽（IKIP）46-60残基的15氨基酸肽链接而成。在5 µM浓度下，F1抑制了小鼠腹腔巨噬细胞中LPS诱导的IκB激酶α（IKKα）和IKKβ的磷酸化以及NF-κB（p65）的核内转移。在体内，F1（5 mg/kg）降低了LPS诱导的脓毒症小鼠模型中IL-6、TNF-α和IL-1β的血清水平，并增加了生存率。
T36408	Rhein-13C4 Rhein-13C4
	Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically i...
T11573	HPN-01	Others	Others
	HPN-01 is a selective IKK inhibitor (pIC50s: 6.4, 7.0, and <4.8 for IKK-α, IKK-β, and IKK-ε). HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, ErbB2, EGFR, GSK3β, Src, PLK1, and VEGFR-2.
T15243	Ertiprotafib PTP 112	Phosphatase; PPAR	DNA Damage/DNA Repair; Metabolism
	Ertiprotafib is a PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist inhibitor ( IC50s: 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ).
T36779	NG 25 (hydrochloride hydrate)
	NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv...

化合物

Cat.No: T63919

Cat.No: T6176

Synonym: IKK Inhibitor VII,IKK-16,IKK16

Target: IκB/IKK, LRRK2

Cat.No: T36524

Synonym: 5-Phenyl-2-ureidothiophene-3-carboxylic Acid Amide,IKK2 Inhibitor IV

Target: IκB/IKK, TNF

IKKγ NBD Inhibitory Peptide acetate

Cat.No: TP1615L

Synonym: IKKγ NBD Inhibitory Peptide acetate(372146-18-4 free base)

Target: NF-κB

TBK1/IKKε-IN-2

Cat.No: T15559

Target: IκB/IKK

TBK1/IKKε-IN-5

Cat.No: T7951

Target: IκB/IKK

Cat.No: T6150

Target: p38 MAPK, Casein Kinase, JNK

Cat.No: T40700

Cat.No: T61059

TBK1/IKKε-IN-6

Cat.No: T39841

Synonym: TBK1/IKKε-IN-6

TBK1/IKKε-IN-4

Cat.No: T38263

Synonym: TBK1/IKKε-IN-4

Cat.No: T71747

IKKγ NBD Inhibitory Peptide TFA

Cat.No: T76024

Cat.No: TQ0306

Target: IκB/IKK

Cat.No: T5209

Target: IκB/IKK

2-AMINO-5-PHENYL-THIOPHENE-3-CARBOXYLIC

Cat.No: T8910

Target: IκB/IKK

Cat.No: T6141

Synonym: IKK2 Inhibitor V,IMD 0354

Target: IκB/IKK

Cyclo(L-Pro-L-Val)

Cat.No: T125120

Target: IκB/IKK, NOS, NF-κB, COX, Antibacterial

Cat.No: T14567

Target: IκB/IKK

Cat.No: T23137

Target: Others

Cat.No: T14669

Target: IκB/IKK, Tyrosine Kinases

ACHP Hydrochloride

Cat.No: T10237

Synonym: IKK-2 Inhibitor VIII

Target: IκB/IKK

Bay 65-1942 hydrochloride

Cat.No: T14508

Target: IκB/IKK

Bay 65-1942 free base

Cat.No: T10472L

Target: IκB/IKK

Bay 65-1942 (R form)

Cat.No: T10472

Synonym: Bay 65-1942 R form

Target: Others

Cat.No: T37449

ML 120B dihydrochloride

Cat.No: T39199

Synonym: ML120B dihydrochloride

Ac2-26 ammonium

Cat.No: T78371

Cat.No: T36192

Cat.No: T38158

Cat.No: T83670

Synonym: Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide

Cat.No: T36408

Synonym: Rhein-13C4

Cat.No: T11573

Target: Others

Cat.No: T15243

Synonym: PTP 112

Target: Phosphatase, PPAR

NG 25 (hydrochloride hydrate)

Cat.No: T36779

Cat. No.	Product Name	Target	Signaling Pathways
T2765	Rosmarinic acid Labiatenic acid,迷迭香酸,Rosemary acid	Apoptosis; IκB/IKK; MAO; Endogenous Metabolite; Transferase; Monoamine Oxidase	Apoptosis; Metabolism; Neuroscience; NF-κB
	Rosmarinic acid (Labiatenic acid) 广泛存在植物中，具有抗氧化、抗炎和抗菌活性。它抑制 MAO-A，MAO-B 和 COMT，IC50分别为 50.1，184.6 和 26.7 μM。
T72208	1-Dehydro-[10]-gingerdione
	1-Dehydro-[10]-gingerdione 通过靶向IKKβ的激活环直接抑制 IKKβ 活性，从而破坏用激动剂刺激的巨噬细胞中 IKKβ 催化的 IκBα 磷酸化。1-Dehydro-[10]-gingerdione 抑制 LPS 诱导的NF-κB 转录活性。1-Dehydro-[10]-gingerdione 具有用于NF-κB 相关炎症和自身免疫性疾病研究的潜力。

天然产物

Rosmarinic acid

Cat.No: T2765

Synonym: Labiatenic acid,迷迭香酸,Rosemary acid

Target: Apoptosis, IκB/IKK, MAO, Endogenous Metabolite, Transferase, Monoamine Oxidase

1-Dehydro-[10]-gingerdione

Cat.No: T72208

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