IKK/IκB

Inhibitory Selectivity

Catalog No.	Inhibitor Name	IκB	IKK	Other
A11957	BAY 11-7082	*		E2-conjugating enzymes
A12836	IKK-16		***
A11579	TPCA-1		****
A12559	BMS-345541		**
A12746	SC-514		**	CDK2/CyclinA,AUR2,PRAK
A12470	Bay 11-7085	*
A12789	PS-1145		***
A15488	LY2409881		****
A11148	BX-795			PDK-1,c-Kit,CDK2/CyclinE
A12837	IMD 0354
A11323	Bardoxolone Methyl			NF-κB,Nrf2
A15900	AZD3264
A12953	WS6			EBP1
A12952	WS3			EBP1
A11318	BMS-345541 HCl		**
A11339	Bay 65-1942	*
A11485	MRT67307		**	TBK1
A13108	PHA 408
A15171	MLN120B

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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BMS-066

Catalog No. A21972
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IKKβ/Tyk2 pseudokinase inhibitor

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively. 了解更多

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IKK epsilon-IN-1

Catalog No. A16298
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IKK-ε 抑制剂

IKK epsilon-IN-1是有效的IKKε抑制剂；抑制IRF3的原位IKKε介导的磷酸化，IC50值小于约100 nM。了解更多

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IKK-3 Inhibitor

Catalog No. A11463
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IKK 抑制剂

IKK-3 Inhibitor是一种有效的，选择性的IKK-ε激酶抑制剂，IC50为40 nM。在IKK-α和IKK-β处无效。了解更多

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IKK-2 inhibitor VIII

Catalog No. A11452
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IKK 抑制剂

IKK-2 inhibitor VIII是一种有效的、选择性IKK-2抑制剂，IC50为8.5 nM。了解更多

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MRT67307

Catalog No. A11485
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SIK/TBK-1/IKKe 抑制剂

MRT67307是一种强效双IKK?和TBK1抑制剂，IC50分别为160和19 nM。了解更多

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AZD3264

Catalog No. A15900
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IKK2 抑制剂?

AZD3264是一种新型的IKK2抑制剂。了解更多

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LY2409881

Catalog No. A15488
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IKK2 抑制剂

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倍以上。了解更多

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MLN120B

Catalog No. A15171
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IκB Kinase β 抑制剂

MLN120B是有效的IKKbeta抑制剂。了解更多

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Bay 65-1942 R form

Catalog No. A15018
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IKK 抑制剂?

Bay 65-1942 R form是一种ATP竞争性抑制剂，可选择性靶向IKKβ激酶。了解更多

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Wedelolactone

Catalog No. A14804
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IKK 抑制剂 II

Wedelolactone是最初从白花苜蓿中提取的化合物，已显示出抑制caspase-11的作用，而caspase-11是促炎性细胞因子IL-1β成熟和病理性细胞凋亡的关键调节剂。了解更多

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- Shigetoshi Yokoyama, .et al. A novel pathway of LPS uptake through syndecan-1 leading to pyroptotic cell death, eLife, 2018, 7: e37854 PMID: 30526845
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Bardoxolone methyl (RTA 402)

Catalog No. A11323
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IκB/IKK 抑制剂

Bardoxolone甲基是口服的一流的合成三萜类化合物。它是Nrf2途径的诱导剂，可以抑制氧化应激和炎症。了解更多

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- Nakamura S, .et al. Nrf2 Activator RS9 Suppresses Pathological Ocular Angiogenesis and Hyperpermeability, Invest Ophthalmol Vis Sci, 2019, 60: 1943-1952
- Hisamichi M, .et al. Role of bardoxolone methyl, a nuclear factor erythroid 2-related factor 2 activator, in aldosterone- and salt-induced renal injury, Hypertens Res, 2018, Jan;41(1):8-17 PMID: 28978980
- Takahiko Imai, .et al. Nrf2 activator ameliorates hemorrhagic transformation in focal cerebral ischemia under anticoagulation, Neurobiol Dis, 2016, May;89:136-46 PMID: 26850917
- Takagi T, .et al. Temporal activation of Nrf2 in the penumbra and Nrf2 activator-mediated neuroprotection in ischemia-reperfusion injury., Free Radic Biol Med., 2014, 72:124-33 PMID: 24746614
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Bay 65-1942

Catalog No. A11339
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IKKβ 抑制剂

Bay 65-1942是选择性靶向IKKβ激酶活性的ATP竞争性抑制剂。了解更多

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BMS-345541 HCl

Catalog No. A11318
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IKK 抑制剂

BMS-345541 HCl是一种细胞可渗透且高度选择性的IKB激酶（IKK）抑制剂，可在酶的变构位点结合并阻断小鼠中NF-kB依赖性转录。了解更多

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Bardoxolone (CDDO)

Catalog No. A11324
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IκB/IKK 抑制剂

Bardoxolone (CDDO)，以前被称为RTA 402，是Reata's抗氧化炎症调节剂(AIMs)组合中的先导分子。了解更多

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- Rothan HA, .et al. Small molecule grp94 inhibitors block dengue and Zika virus replication, Antiviral Res, 2019, Aug 14;171:104590 PMID: 31421166
- Turpaev K, .et al. Aromatic malononitriles stimulate the resistance of insulin-producing beta-cells to oxidants and inflammatory cytokines, Eur J Pharmacol, 2016, Aug 5;784:69-80 PMID: 27178899
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Bay 65-1942 HCl

Catalog No. A11338
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IKKβ kinase 抑制剂

Bay 65-1942 HCl是选择性靶向IKKβ激酶活性的ATP竞争性抑制剂。了解更多

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BX-795

Catalog No. A11148
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PDK-1 抑制剂

BX-795是有效的PDK1抑制剂，可阻断肿瘤细胞中的PDK1/Akt信号传导并抑制培养物中多种肿瘤细胞系的锚定依赖性生长或诱导凋亡。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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IKK 16 hydrochloride

Catalog No. A21588
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IKK2/IKK complex/IKK1 inhibitor

IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. 了解更多

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IKK-IN-1

Catalog No. A21221
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IKK inhibitor

IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13. 了解更多

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INH14

Catalog No. A19119
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IKKα/IKKβ inhibitor

INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. 了解更多

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TBK1/IKKε-IN-5

Catalog No. A18400
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dual TBK1 and IKKε inhibitor

TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor, with IC50 values of 1 nM and 5.6 nM for TBK1 and IKKε, respectively. 了解更多

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CDDO-EA

Catalog No. A16299
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Nrf2 activator

CDDO-EA是Nrf2/ARE的激活剂；神经保护作用。了解更多

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Amlexanox

Catalog No. A16297
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IKKε /TBK1 抑制剂

Amlexanox是一种抗炎抗过敏免疫调节剂，用于治疗复发性口疮（溃疡疮）和（在日本）几种炎性疾病。了解更多

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Bay 11-7821

Catalog No. A11957
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E2 ubiquitin conjugating enzyme 抑制剂

Bay 11-7821是TNF-α刺激的IκBα磷酸化的不可逆抑制剂。了解更多

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- Ali Nasrollahzadeh, .et al. Blockade of Nuclear Factor-??b (NF-??b) Pathway Using Bay 11-7082 Enhances Arsenic Trioxide-Induced Antiproliferative Activity in U87 Glioblastoma Cells, Rep Biochem Mol Biol, 2022, Jan;10(4):602-613 PMID: 35291620
- Ali Nasrollahzadeh, .et al. Arsenic trioxide and BIBR1532 synergistically inhibit breast cancer cell proliferation through attenuation of NF-κB signaling pathway, Life Sci, 2020, Jul 6;257:118060 PMID: 32645343
- Momeny M, .et al. Blockade of nuclear factor-κB (NF-κB) pathway inhibits growth and induces apoptosis in chemoresistant ovarian carcinoma cells, Int J Biochem Cell Biol, 2018, Jun;99:1-9 PMID: 29567488
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PS-1145

Catalog No. A12789
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IKK 抑制剂

PS-1145是一种高度特异性的IKB激酶（IKK）抑制剂，可有效抑制PC细胞的基础和诱导型NF-kB活性。了解更多

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SC-514

Catalog No. A12746
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IκB/IKK 抑制剂

SC-514是一种具有口服活性的，具有ATP竞争性的IKKβ抑制剂（IC50 = 3-12μM），其选择性是JNK，p38，MK2和ERK等28种其他激酶的10倍以上。了解更多

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IKK-16

Catalog No. A12836
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IKK 抑制剂

IKK 16是针对IKK-2，IKK复合物和IKK-1的选择性IκB激酶（IKK）抑制剂，IC50分别为40 nM，70 nM和200 nM。了解更多

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- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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IMD 0354

Catalog No. A12837
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IKK 抑制剂

IMD 0354是IκB激酶-β（IKKβ）抑制剂，可阻断NF-κB核易位。了解更多

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- Anton Lennikov, .et al. Selective IKK2 inhibitor IMD0354 disrupts NF-κB signaling to suppress corneal inflammation and angiogenesis, Angiogenesis, 2018, 21(2): 267-285 PMID: 29332242
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BI605906

Catalog No. A13537
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IKKβ 抑制剂

BI605906是IKK beta的新型抑制剂。了解更多

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BMS-345541

Catalog No. A12559
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IKK2/IKK1 抑制剂

BMS-345541是IKK-2和IKK-1催化亚基的高度选择性抑制剂，IC50为0.3 μM和4 μM。了解更多

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BAY 11-7085

Catalog No. A12470
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κB/IKK 抑制剂

BAY 11-7085是TNFα诱导的IκBα磷酸化的不可逆抑制剂，IC50为10μM。了解更多

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- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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WS6

Catalog No. A12953
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EBP1 抑制剂

WS6是通过调节Erb3结合蛋白1（EBP1）和IκB激酶途径的β细胞增殖诱导剂。了解更多

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WS3

Catalog No. A12952
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EBP1 抑制剂

WS3是通过调节Erb3结合蛋白1（EBP1）和IκB激酶途径的β细胞增殖诱导剂。了解更多

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TPCA-1

Catalog No. A11579
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IKK-2 抑制剂

TPCA-1是一种有效且选择性的人IκB激酶2（IKK-2）抑制剂，IKK-2的IC50 = 17.9 nM，而IKK-1的IC50为400nM。了解更多

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- Dongdong Fang, etc. Epithelial-Mesenchymal Transition of Ovarian Cancer Cells Is Sustained by Rac1 through Simultaneous Activation of MEK1/2 and Src Signaling Pathways. Oncogene. 2017 Mar; 36(11): 1546–1558.
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PHA 408

Catalog No. A13108
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IKK-2 抑制剂

PHA 408是一种有效的，高度选择性的，具有ATP竞争性的IKB激酶2（IKK-2）抑制剂（IC50：40 nM），它以相对较慢的释放速率紧密结合IKK-2。强烈推荐您研究IKK-2调节NF-KB信号传导机制的工具。了解更多

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