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)
DMSO アルコール
S1274 BX-795 <1 mg/mL 100 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
S2864 IMD 0354 <1 mg/mL 10 mg/mL 77 mg/mL
S0949 Cucurbitacin IIb ' 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
S8935 BAY-985 ' mg/mL
S6714 INH14 <1 mg/mL 48 mg/mL 18 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
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

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.

S2913

BAY 11-7082

BAY 11-7082 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.

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.

S2824

TPCA-1

TPCA-1 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.

S2864

IMD 0354

IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

S0949

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

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

TBK1/IKKε-IN-2

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

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).

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.

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.

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.

S4907

SC-514

SC-514 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.

S1681

Mesalamine

Mesalamine (5-Aminosalicylic acid) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.

S7352

Bay 11-7085

BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

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.

S7851

AZD3264

AZD3264 is a novel IKK2 inhibitor.

S7697

LY2409881

LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.

S7691

PS-1145

PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.

S3648

Amlexanox

Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.

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.

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.

S9417

Homoplantaginin

Homoplantaginin, 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) 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.

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

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.

S2913

BAY 11-7082

BAY 11-7082 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.

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.

S2824

TPCA-1

TPCA-1 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.

S2864

IMD 0354

IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

S0949

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

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

TBK1/IKKε-IN-2

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

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).

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.

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.

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.

S4907

SC-514

SC-514 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.

S1681

Mesalamine

Mesalamine (5-Aminosalicylic acid) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.

S7352

Bay 11-7085

BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.

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.

S7851

AZD3264

AZD3264 is a novel IKK2 inhibitor.

S7697

LY2409881

LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.

S7691

PS-1145

PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.

S3648

Amlexanox

Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.

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.

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.

S9417

Homoplantaginin

Homoplantaginin, 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) 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.

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.

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
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.

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
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.