IκB/IKK

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1274	BX-795	<1 mg/mL	100 mg/mL	<1 mg/mL
S1396	Resveratrol	<1 mg/mL	45 mg/mL	<1 mg/mL
S2913	BAY 11-7082	<1 mg/mL	41 mg/mL	10 mg/mL
S2882	IKK-16 (IKK Inhibitor VII)	<1 mg/mL	97 mg/mL	<1 mg/mL
S2824	TPCA-1	<1 mg/mL	56 mg/mL	<1 mg/mL
S1321	Urolithin B	<1 mg/mL	42 mg/mL	12 mg/mL
S8922	TBK1/IKKε-IN-1(compound 1)	˂1 mg/mL	10 mg/mL	˂1 mg/mL
S0425	TBK1/IKKε-IN-2	<1 mg/mL	60 mg/mL	<1 mg/mL
S2864	IMD 0354	<1 mg/mL	10 mg/mL	77 mg/mL
S8078	Bardoxolone Methyl	<1 mg/mL	21 mg/mL	<1 mg/mL
S8044	BMS-345541	<1 mg/mL	9 mg/mL	''<1 mg/mL
S4907	SC-514	<1 mg/mL	45 mg/mL	<1 mg/mL
S1681	Mesalamine	<1 mg/mL	31 mg/mL	31 mg/mL
S7352	Bay 11-7085	<1 mg/mL	50 mg/mL	50 mg/mL
S3615	Dehydrocostus Lactone	<1 mg/mL	46 mg/mL	46 mg/mL
S7851	AZD3264	<1 mg/mL	88 mg/mL	2 mg/mL
S7697	LY2409881	<1 mg/mL	20 mg/mL	<1 mg/mL
S7691	PS-1145	<1 mg/mL	64 mg/mL	2 mg/mL
S3648	Amlexanox	<1 mg/mL	59 mg/mL	'1 mg/mL
S7948	MRT67307 HCl	92 mg/mL	92 mg/mL	92 mg/mL
S9042	Wedelolactone	-1 mg/mL	63 mg/mL	-1 mg/mL
S9417	Homoplantaginin	-1 mg/mL	92 mg/mL	-1 mg/mL
S3607	Sarsasapogenin	<1 mg/mL	<1 mg/mL	5 mg/mL
S6714	INH14	<1 mg/mL	48 mg/mL	18 mg/mL
S9184	Forsythoside B	-1 mg/mL	100 mg/mL	-1 mg/mL
S3612	Rosmarinic acid	24 mg/mL	72 mg/mL	72 mg/mL
S3298	Caulophylline (N-Methylcytisine)	-1 mg/mL	100 mg/mL	-1 mg/mL
S7441	WS3	<1 mg/mL	100 mg/mL	80 mg/mL
S7442	WS6	<1 mg/mL	100 mg/mL	100 mg/mL

亜型選択性的な製品

IκB/IKK製品

All (31) IκB/IKK阻害剤(28) IκB/IKK拮抗剤(1) IκB/IKKモジュレータ(2)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1274	BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1.	J Thromb Haemost, 2020, 10.1111/jth.14748 Biochim Biophys Acta Mol Cell Res, 2020, S0167-4889(20)30287-1 Antimicrob Agents Chemother, 2020, AAC.00245-20	Induction of basal p62 Ser403 phosphorylation in ULK1/2-deﬁcient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
S1396	Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases（LOX, IC50=2.7 μM）, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.	Bone, 2020, 133:115252 J Biol Chem, 2020, 13;295(11):3485-3496 Life Sci, 2020, S0024-3205(20)31542-3	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
S2913	BAY 11-7082 BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.	J Cell Physiol, 2021, 236(2):1375-1390 Nat Commun, 2020, 19;11(1):2487 Sci Adv, 2020, 26;6(9):eaay9269	Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
S2882	IKK-16 (IKK Inhibitor VII) IKK-16 (IKK Inhibitor VII) 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.	Nature, 2020, 583(7818):852-857 EMBO J, 2020, 1;39(7):e103304 Cell Rep, 2020, 30(10):3383-3396	Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
S2824	TPCA-1 TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.	Nat Med, 2020, 10.1038/s41591-020-1073-3 Cell Death Dis, 2020, 24;11(4):282 Cells, 2020, 9(2)	AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
S1321^新	Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S0949^新	Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S8922^新	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.
S0425^新	TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε.
S8935^新	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).
S2864	IMD 0354 IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.	Adv Sci (Weinh), 2020, 7(18):2000906 J Allergy Clin Immunol, 2020, 145(1):437-440 Mucosal Immunol, 2020, 13(1):86-95	(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, P < 0.01 and *P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
S8078	Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.	Cancers (Basel), 2020, 12(6):E1645 Antioxidants (Basel), 2020, 9(1) Life Sci, 2020, 265:118853	Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
S8044	BMS-345541 BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively.	Nature, 2020, 579(7798):284-290 Nat Commun, 2020, 27;11(1):2042 Biochem Pharmacol, 2020, 12:114023	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S4907	SC-514 SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.	Hepatology, 2020, 10.1002/hep.31249 J Immunol, 2020, 20 pii: ji1901089 J Cell Physiol, 2020, 10.1002/jcp.30192
S1681	Mesalamine Mesalamine (5-Aminosalicylic acid) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.	Antiviral Res, 2020, 185:104993
S7352	Bay 11-7085 BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.	Adv Sci (Weinh), 2020, 7(17):2000593 Cells, 2020, 9(2) Mol Oncol, 2020, 14(12):3211-3233	VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10^-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10^-7mol/L salusin-β treatment alone.
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.	Int Immunopharmacol, 2020, 78:106075 J Cell Mol Med, 2019, 23(8):5762-5770
S7851	AZD3264 AZD3264 is a novel IKK2 inhibitor.	Redox Biol, 2017, 11:562-576	(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
S7697	LY2409881 LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.	Nat Commun, 2019, 10(1):2924 Mol Pharm, 2018, 15(2):609-618 J Biol Chem, 2018, 293(30):11913-11927	A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
S7691	PS-1145 PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.	J Biol Chem, 2018, 293(19):7268-7280 Redox Biol, 2017, 562-576 Blood, 2016, 128(1):82-92	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S3648	Amlexanox Amlexanox (AA-673, CHX-3673) is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.	Sci China Life Sci, 2020, 10.1007/s11427-020-1736-5 Onco Targets Ther, 2020, 13:2997-3011 Theranostics, 2020, 10(5):2358-2373
S7948	MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.	Cell Rep, 2020, 33(5):108339 Cancer Discov, 2020, 10(3):382-393 Cell Death Differ, 2020, 10.1038/s41418-020-0588-y
S9042	Wedelolactone Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα.	Int Immunopharmacol, 2019, 73:17-22
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.
S3607	Sarsasapogenin Sarsasapogenin (SAR, Parigenin) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signaling pathways. SAR potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.
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.
S9184	Forsythoside B Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
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.
S3298^新	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.
S7441	WS3 WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
S7442	WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1274	BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1.	J Thromb Haemost, 2020, 10.1111/jth.14748 Biochim Biophys Acta Mol Cell Res, 2020, S0167-4889(20)30287-1 Antimicrob Agents Chemother, 2020, AAC.00245-20	Induction of basal p62 Ser403 phosphorylation in ULK1/2-deﬁcient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
S1396	Resveratrol Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases（LOX, IC50=2.7 μM）, kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.	Bone, 2020, 133:115252 J Biol Chem, 2020, 13;295(11):3485-3496 Life Sci, 2020, S0024-3205(20)31542-3	Cellular senescence and SIRT1 phosphorylation was monitored in PAECs (P2) incubated in DMEM containing HDL (50 mg/L), LDL (50 mg/L), or resveratrol (100 μM) for 24 hours.
S2913	BAY 11-7082 BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.	J Cell Physiol, 2021, 236(2):1375-1390 Nat Commun, 2020, 19;11(1):2487 Sci Adv, 2020, 26;6(9):eaay9269	Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
S2882	IKK-16 (IKK Inhibitor VII) IKK-16 (IKK Inhibitor VII) 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.	Nature, 2020, 583(7818):852-857 EMBO J, 2020, 1;39(7):e103304 Cell Rep, 2020, 30(10):3383-3396	Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
S2824	TPCA-1 TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis.	Nat Med, 2020, 10.1038/s41591-020-1073-3 Cell Death Dis, 2020, 24;11(4):282 Cells, 2020, 9(2)	AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies.
S1321^新	Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S0949^新	Cucurbitacin IIb Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis.
S8922^新	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.
S0425^新	TBK1/IKKε-IN-2 TBK1/IKKε-IN-2 is a dual inhibitor of TBK1 and IKKε.
S8935^新	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).
S2864	IMD 0354 IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.	Adv Sci (Weinh), 2020, 7(18):2000906 J Allergy Clin Immunol, 2020, 145(1):437-440 Mucosal Immunol, 2020, 13(1):86-95	(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, P < 0.01 and *P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
S8078	Bardoxolone Methyl Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.	Cancers (Basel), 2020, 12(6):E1645 Antioxidants (Basel), 2020, 9(1) Life Sci, 2020, 265:118853	Renal Nrf2 activity was shown in RTA402-treated acFSGS (RTA402 + acFSGS) mice as early as day 7 (RTA402 + acFSGS) and persisted to day 28, compared to vehicle + acFSGS mice. Kidney in situ ROS production demonstrated by DHE detection.
S8044	BMS-345541 BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively.	Nature, 2020, 579(7798):284-290 Nat Commun, 2020, 27;11(1):2042 Biochem Pharmacol, 2020, 12:114023	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S4907	SC-514 SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.	Hepatology, 2020, 10.1002/hep.31249 J Immunol, 2020, 20 pii: ji1901089 J Cell Physiol, 2020, 10.1002/jcp.30192
S1681	Mesalamine Mesalamine (5-Aminosalicylic acid) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.	Antiviral Res, 2020, 185:104993
S7352	Bay 11-7085 BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.	Adv Sci (Weinh), 2020, 7(17):2000593 Cells, 2020, 9(2) Mol Oncol, 2020, 14(12):3211-3233	VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10^-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10^-7mol/L salusin-β treatment alone.
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.	Int Immunopharmacol, 2020, 78:106075 J Cell Mol Med, 2019, 23(8):5762-5770
S7851	AZD3264 AZD3264 is a novel IKK2 inhibitor.	Redox Biol, 2017, 11:562-576	(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
S7697	LY2409881 LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.	Nat Commun, 2019, 10(1):2924 Mol Pharm, 2018, 15(2):609-618 J Biol Chem, 2018, 293(30):11913-11927	A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
S7691	PS-1145 PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.	J Biol Chem, 2018, 293(19):7268-7280 Redox Biol, 2017, 562-576 Blood, 2016, 128(1):82-92	(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. , p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. , p<0.05.
S3648	Amlexanox Amlexanox (AA-673, CHX-3673) is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.	Sci China Life Sci, 2020, 10.1007/s11427-020-1736-5 Onco Targets Ther, 2020, 13:2997-3011 Theranostics, 2020, 10(5):2358-2373
S7948	MRT67307 HCl MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy.	Cell Rep, 2020, 33(5):108339 Cancer Discov, 2020, 10(3):382-393 Cell Death Differ, 2020, 10.1038/s41418-020-0588-y
S9042	Wedelolactone Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα.	Int Immunopharmacol, 2019, 73:17-22
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.
S3607	Sarsasapogenin Sarsasapogenin (SAR, Parigenin) is a steroidal sapogenin. It can provoke the generation of reactive oxygen species and activate unfolded protein response (UPR) signaling pathways. SAR potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.
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.
S9184	Forsythoside B Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
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.

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S3298^新	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.

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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.

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S7441	WS3 WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
S7442	WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

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S7441