IκB/IKK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

IκB/IKK Products

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

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 (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.

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.

S2864

IMD 0354

IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

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 (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.

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.

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.

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.

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 (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.

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. Wedelolactone is also an inhibitor of caspase-11.

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.

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.

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).

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.

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.

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.

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.

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.

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.

S3168New

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

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 (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.

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.

S2864

IMD 0354

IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

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 (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.

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.

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.

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.

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 (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.

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. Wedelolactone is also an inhibitor of caspase-11.

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.

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.

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).

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.

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.

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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S3168New

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.

Catalog No. Information Product Use Citations Product Validations
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.