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IκB/IKK Inhibitors (34)
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Catalog No.	Product Name	Information	Product Use Citations
E0796^New	NF-κB-IN-1	NF-κB-IN-1 is a potent NF-κB signaling pathway inhibitor, which acts by directly inhibiting inhibitory κB kinase (IKK).
E0944^New	IMD-0560	IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.
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.	Cell Rep, 2022, 38(7):110373 mBio, 2022, 13(3):e0085422 Microbiol Spectr, 2022, e0219321
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.	Molecules, 2022, 27(11)3542 Placenta, 2022, 122:56-65 Oral Dis, 2022, 10.1111/odi.14286
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.	Front Vet Sci, 2021, 8:670949 Antiviral Res, 2020, 185:104993
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 Cell Biol, 2022, 24(5):766-782 Sci Adv, 2022, 8(12):eabh4050 Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S2864	IMD 0354	IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.	Blood, 2022, blood.2021014304 Int Immunopharmacol, 2022, 110:108944 Transl Oncol, 2022, 18:101362
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.	mBio, 2022, 13(3):e0085422 Int J Biol Sci, 2022, 18(5):2132-2145 PLoS Genet, 2022, 18(6):e1010235
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.	Nat Med, 2022, 28(4):752-765 Gastroenterology, 2022, 162(6):1716-1731.e17 Adv Sci (Weinh), 2022, 10.1002/advs.202104055
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.	Free Radic Biol Med, 2021, S0891-5849(21)00198-2
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.	Front Pharmacol, 2021, 12:641098 Int Immunopharmacol, 2020, 78:106075 J Cell Mol Med, 2019, 23(8):5762-5770
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.	PLoS Pathog, 2022, 18(2):e1010301 Gut, 2021, 70(5):890-899 Biochem Biophys Res Commun, 2021, 560:1-6
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.	Cell Death Differ, 2021, 10.1038/s41418-021-00787-y Biochem Biophys Res Commun, 2021, 560:165-171 Hepatology, 2020, 10.1002/hep.31249
S6386	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.	Microbiol Spectr, 2022, e0219321 Front Pharmacol, 2022, 13:924523
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.	Cancer Cell, 2022, S1535-6108(22)00312-9 Front Pharmacol, 2022, 13:932198 Front Pharmacol, 2022, 13:807440
S7691	PS-1145	PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.	Cell Chem Biol, 2022, 29(7):1113-1125.e6 J Biol Chem, 2018, 293(19):7268-7280 Redox Biol, 2017, 562-576
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
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.	Redox Biol, 2017, 11:562-576
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.	Cancer Res, 2022, 82(10):1991-2002 Microbiol Spectr, 2022, e0219321 Cell, 2021, S0092-8674(21)00885-0
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.	Nat Med, 2022, 28(3):557-567 Cancer Cell, 2022, S1535-6108(22)00312-9 J Clin Invest, 2022, 132(7)e140869
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.	Cancer Commun (Lond), 2022, 10.1002/cac2.12332 Bioorg Med Chem, 2022, 69:116883 Drug Des Devel Ther, 2021, 15:21-35
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.	Cell Death Differ, 2022, 10.1038/s41418-022-00940-1 J Med Chem, 2018, 61(3):760-776
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.	Exp Eye Res, 2021, 211:108750 Int Immunopharmacol, 2019, 73:17-22
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.	Virus Res, 2021, 301:198435
S7442	WS6	WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
E0796^New	NF-κB-IN-1	NF-κB-IN-1 is a potent NF-κB signaling pathway inhibitor, which acts by directly inhibiting inhibitory κB kinase (IKK).
E0944^New	IMD-0560	IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.
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.	Cell Rep, 2022, 38(7):110373 mBio, 2022, 13(3):e0085422 Microbiol Spectr, 2022, e0219321
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.	Molecules, 2022, 27(11)3542 Placenta, 2022, 122:56-65 Oral Dis, 2022, 10.1111/odi.14286
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.	Front Vet Sci, 2021, 8:670949 Antiviral Res, 2020, 185:104993
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 Cell Biol, 2022, 24(5):766-782 Sci Adv, 2022, 8(12):eabh4050 Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S2864	IMD 0354	IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.	Blood, 2022, blood.2021014304 Int Immunopharmacol, 2022, 110:108944 Transl Oncol, 2022, 18:101362
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.	mBio, 2022, 13(3):e0085422 Int J Biol Sci, 2022, 18(5):2132-2145 PLoS Genet, 2022, 18(6):e1010235
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.	Nat Med, 2022, 28(4):752-765 Gastroenterology, 2022, 162(6):1716-1731.e17 Adv Sci (Weinh), 2022, 10.1002/advs.202104055
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.	Free Radic Biol Med, 2021, S0891-5849(21)00198-2
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.	Front Pharmacol, 2021, 12:641098 Int Immunopharmacol, 2020, 78:106075 J Cell Mol Med, 2019, 23(8):5762-5770
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.	PLoS Pathog, 2022, 18(2):e1010301 Gut, 2021, 70(5):890-899 Biochem Biophys Res Commun, 2021, 560:1-6
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.	Cell Death Differ, 2021, 10.1038/s41418-021-00787-y Biochem Biophys Res Commun, 2021, 560:165-171 Hepatology, 2020, 10.1002/hep.31249
S6386	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.	Microbiol Spectr, 2022, e0219321 Front Pharmacol, 2022, 13:924523
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.	Cancer Cell, 2022, S1535-6108(22)00312-9 Front Pharmacol, 2022, 13:932198 Front Pharmacol, 2022, 13:807440
S7691	PS-1145	PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.	Cell Chem Biol, 2022, 29(7):1113-1125.e6 J Biol Chem, 2018, 293(19):7268-7280 Redox Biol, 2017, 562-576
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
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.	Redox Biol, 2017, 11:562-576
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.	Cancer Res, 2022, 82(10):1991-2002 Microbiol Spectr, 2022, e0219321 Cell, 2021, S0092-8674(21)00885-0
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.	Nat Med, 2022, 28(3):557-567 Cancer Cell, 2022, S1535-6108(22)00312-9 J Clin Invest, 2022, 132(7)e140869
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.	Cancer Commun (Lond), 2022, 10.1002/cac2.12332 Bioorg Med Chem, 2022, 69:116883 Drug Des Devel Ther, 2021, 15:21-35
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.	Cell Death Differ, 2022, 10.1038/s41418-022-00940-1 J Med Chem, 2018, 61(3):760-776
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.	Exp Eye Res, 2021, 211:108750 Int Immunopharmacol, 2019, 73:17-22
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.	Virus Res, 2021, 301:198435
S7442	WS6	WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
E0796^New	NF-κB-IN-1	NF-κB-IN-1 is a potent NF-κB signaling pathway inhibitor, which acts by directly inhibiting inhibitory κB kinase (IKK).
E0944^New	IMD-0560	IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.