IκB/IKK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
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
S7442 WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
Environ Int, 2025, 204:109820
Mol Hum Reprod, 2025, 31(2)gaaf012
Nat Commun, 2024, 15(1):4739
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
Verified customer review of LY2409881
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
Verified customer review of PS-1145
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
Verified customer review of AZD3264
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
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
Verified customer review of BAY 11-7082 (BAY 11-7821)
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
Verified customer review of BX-795
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.