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IκB/IKK
Choose Selective IκB/IKK Inhibitors
IκB/IKK Signaling Pathway Map
Isoform-selective Inhibitors
IκB/IKK Products
- All (34)
- IκB/IKK Inhibitors (32)
- IκB/IKK Modulators (2)
- New IκB/IKK Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S0425 | TBK1/IKKε-IN-2 | TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. | ||
| 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. | ||
| 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. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively. |
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| S1321 | 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. | ||
| S1396 | Resveratrol (SRT501) | Resveratrol (SRT501, trans-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. |
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| S1681 | Mesalamine (5-ASA) | Mesalamine (5-Aminosalicylic acid, 5-ASA, Mesalazine, Apriso, Asacol, Pentasa, Canasa) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease. | ||
| 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. |
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| S2864 | IMD 0354 | IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. |
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| 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. |
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| 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. |
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| 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 polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S6386New | MRT67307 | MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells. |
||
| 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. | ||
| S7352 | Bay 11-7085 | BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
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| S7691 | PS-1145 | PS-1145 is a specific IKK inhibitor with IC50 of 88 nM. |
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| S7697 | LY2409881 | LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. |
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| S7736 | MLN120B | MLN120B (ML120B) is a potent, selective, reversible, and ATP-competitive inhibitor of IkappaB kinase beta (IKKβ) with an IC50 of 45 nM for recombinant IKKβ. MLN120B does not inhibit other IKK isoforms at IC50 below 50 μM. | ||
| S7851 | AZD3264 | AZD3264 is a novel IKK2 inhibitor. |
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| 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. |
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| 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. |
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| 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. |
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| 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. | ||
| 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). | ||
| 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. Wedelolactone is also an inhibitor of caspase-11. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S0425 | TBK1/IKKε-IN-2 | TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. | ||
| 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. | ||
| 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. BX-795 also is a potent TBK1 inhibitor that blocks both TBK1 and IKKε with IC 50 values of 6 nM and 41 nM, respectively. |
|
|
| S1321 | 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. | ||
| S1396 | Resveratrol (SRT501) | Resveratrol (SRT501, trans-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. |
|
|
| S1681 | Mesalamine (5-ASA) | Mesalamine (5-Aminosalicylic acid, 5-ASA, Mesalazine, Apriso, Asacol, Pentasa, Canasa) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease. | ||
| 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. |
|
|
| S2864 | IMD 0354 | IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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 polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S6386New | MRT67307 | MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells. |
||
| 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. | ||
| S7352 | Bay 11-7085 | BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
|
|
| S7691 | PS-1145 | PS-1145 is a specific IKK inhibitor with IC50 of 88 nM. |
|
|
| S7697 | LY2409881 | LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. |
|
|
| S7736 | MLN120B | MLN120B (ML120B) is a potent, selective, reversible, and ATP-competitive inhibitor of IkappaB kinase beta (IKKβ) with an IC50 of 45 nM for recombinant IKKβ. MLN120B does not inhibit other IKK isoforms at IC50 below 50 μM. | ||
| S7851 | AZD3264 | AZD3264 is a novel IKK2 inhibitor. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| 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). | ||
| 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. Wedelolactone is also an inhibitor of caspase-11. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S6386New | MRT67307 | MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells. |
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