IκB/IKK Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S2882	IKK-16	IKK-16 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.	Ann Rheum Dis, 2025, S0003-4967(25)04453-X Nucleic Acids Res, 2025, 53(17)gkaf891 Cell Commun Signal, 2025, 23(1):274
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 Genet, 2025, 10.1038/s41588-025-02221-2 EMBO J, 2025, 10.1038/s44318-025-00412-5 EMBO J, 2025, 10.1038/s44318-025-00561-7
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.	Cell Death Dis, 2025, 16(1):124 Mol Med, 2025, 31(1):197 Cancer Med, 2025, 14(5):e70047
S7352	Bay 11-7085	BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.	JCI Insight, 2025, e186456 J Am Soc Nephrol, 2024, 35(8):998-1015 Theranostics, 2024, 14(2):861-878
S2864	IMD 0354	IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.	Nat Commun, 2025, 16(1):5387 Iran J Basic Med Sci, 2023, 26(8):912-918 Blood, 2022, blood.2021014304
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.	EMBO Rep, 2025, 10.1038/s44319-025-00444-2 EMBO J, 2024, 10.1038/s44318-024-00244-9 mBio, 2023, 10.1128/mbio.02506-23
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.	bioRxiv, 2023, 10.1101/2023.12.15.571909 Int J Mol Sci, 2022, 23(23)15000 Cell Death Differ, 2021, 10.1038/s41418-021-00787-y
S8922	TBK1/IKKε-IN-5	TBK1/IKKε-IN-5 (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.	Autophagy, 2025, 1-23. Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791 Sci Adv, 2024, 10(6):eadk2285
S1681	Mesalazine (5-ASA)	Mesalazine (5-ASA) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.	Nat Commun, 2025, 16(1):1826 Phytomedicine, 2025, 146:157096 J Nutr Biochem, 2024, 136:109804
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
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
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. This compound is also an inhibitor of caspase-11.	Int J Ophthalmol, 2024, 17(4):616-624 PeerJ, 2022, 10:e13766 Exp Eye Res, 2021, 211:108750
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
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.	Theranostics, 2025, 15(6):2523-2543 World J Clin Oncol, 2025, 16(5):105341 Free Radic Biol Med, 2021, S0891-5849(21)00198-2
S8935	BAY-985	BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. This compound 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).	Nat Commun, 2023, 14(1):1399 Mol Cancer, 2022, 21(1):97
S7851	AZD3264	AZD3264 is a novel IKK2 inhibitor.	Redox Biol, 2017, 11:562-576
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. This compound does not inhibit other IKK isoforms at IC50 below 50 μM.	Arthritis Res Ther, 2024, 26(1):181
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.	Int J Mol Sci, 2022, 23(23)15000
E3305	Sophora Flower Extract	Sophora Flower Extract is extracted from dried flowers of Sophora japonica (Huaihua), which is used in China, Japan and Korea for treating haematemesis and bleeding haemorrhoids.
E2507	BI605906	BI605906 is a selective inhibitor of IKKβ with an IC50 of 380 nM when assayed at 0.1 mM ATP, suppressing the phosphorylation and activation of IKKβ, modulating NF-κB signalling. It also inhibits the insulin-like growth factor 1 (IGF1) receptor, with an IC50 of 7.6 μM. This compound effectively blocks TNF-α-dependent IκB degradation and reduces the expression of proinflammatory cytokines, including IL-6, IL-1β, and C-X-C motif ligands CXCL1/2.
E0944	IMD-0560	IMD-0560 is an Inhibitor of nuclear factor kappa-B kinase (IKK) which can suppress the production of inflammatory cytokines and chemokines.
E7464	BMS-345541 hydrochloride	BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of I kappa B kinase (IKK) with an IC50 of 0.3 μM for IKK-2 and 4 μM for IKK-1 IC50. BMS-345541 binds at an allosteric site of IKK.
E1798	HOIPIN-8	HOIPIN-8, is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) and NF-κB signaling with an IC50 value of 11 nM. It serves as a powerful tool for investigating the physiological and cellular functions of LUBAC.
S2913	BAY 11-7082 (BAY 11-7821)	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.	ACS Nano, 2025, 19(20):19057-19079 Adv Sci (Weinh), 2025, 12(28):e2502634 J Med Virol, 2025, 97(8):e70534
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.	Cancer Res, 2025, 10.1158/0008-5472.CAN-25-1791 Cell Rep, 2025, 44(7):115972 EMBO J, 2024, 10.1038/s44318-024-00244-9
S1396	Resveratrol (trans-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.	Aging Cell, 2025, e70075 Biomed Pharmacother, 2025, 190:118393 Breast Cancer Res, 2025, 27(1):186
S8078	Bardoxolone Methyl (RTA 402)	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.	J Clin Invest, 2025, 135(14)e176655 Redox Biol, 2025, 87:103885 Research (Wash D C), 2025, 8:0980
S3648	Amlexanox	Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.	Biomed Pharmacother, 2025, 186:117991 Cell Death Discov, 2025, 11(1):286 Sci Adv, 2025, 11(4):eadq2395
E0796	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).	Front Cell Dev Biol, 2023, 11:1062229 Front Pharmacol, 2022, 13:996667
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. This compound also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. It can blocks autophagy in cells.	Front Pharmacol, 2022, 13:924523 Microbiol Spectr, 2022, e0219321
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.	J Gerontol A Biol Sci Med Sci, 2022, 77-8:1485-1493
S9417	Homoplantaginin	Homoplantaginin (Hispidulin-7-glucoside), a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. This compound inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.	Front Pharmacol, 2025, 16:1526107
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. This compound potently inhibits NF-κB and MAPK activation, as well as IRAK1, TAK1, and IκBα phosphorylation in LPS-stimulated macrophages.	J Exp Clin Cancer Res, 2022, 41(1):174
S1321	Urolithin B	Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. This compound suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. It is also a regulator of skeletal muscle mass.	PLoS Pathog, 2025, 21(8):e1013401
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. This compound exhibits anti-inflammatory activity and induces apoptosis. It is isolated from Hemsleya amabilis.
S6714	INH14	INH14 is an inhibitor of TLR2-mediated NF-κB 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. It binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. This compound significantly reduces myeloperoxidase (MPO) activity and 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. This compound has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. It could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.