IκB/IKK

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IκB/IKK製品

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  • IκB/IKK阻害剤 (34)
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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.
Nat Cancer, 2024, 10.1038/s43018-023-00712-x
Redox Biol, 2024, 70:103072
Cell Death Dis, 2024, 15(1):70
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.
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
Cell Rep, 2023, 42(2):112127
S1396 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.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
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.
Life Sci Alliance, 2024, 10.26508/lsa.202101282
Cell, 2023, 186(22):4851-4867.e20
J Clin Invest, 2023, 133(4)e162190
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.
Theranostics, 2024, 14(3):1224-1240
Cell Mol Gastroenterol Hepatol, 2024, S2352-345X(24)00005-5
Nat Commun, 2023, 14(1):8082
S7352 Bay 11-7085 BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
Theranostics, 2024, 14(2):861-878
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
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 Commun, 2023, 14(1):8082
Clin Cancer Res, 2023, 29(16):3151-3161
Clin Cancer Res, 2023, 29(16):3151-3161
S2864 IMD 0354 IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.
Iran J Basic Med Sci, 2023, 26(8):912-918
Blood, 2022, blood.2021014304
J Immunother Cancer, 2022, 10(7)e005063
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.
Nat Commun, 2023, 14(1):3648
Redox Biol, 2023, 60:102632
Cell Rep, 2023, 42(12):113431
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.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
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
S3648 Amlexanox Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
Signal Transduct Target Ther, 2023, 8(1):246
Signal Transduct Target Ther, 2023, 8(1):246
Nucleic Acids Res, 2022, 50(15):8700-8718
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
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.
Sci Adv, 2024, 10(6):eadk2285
Cell Rep, 2023, 42(2):112127
J Nat Prod, 2023, acs.jnatprod.2c00843
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
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
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.
PeerJ, 2022, 10:e13766
Exp Eye Res, 2021, 211:108750
Int Immunopharmacol, 2019, 73:17-22
S1681 Mesalazine (5-ASA) Mesalazine (5-ASA) 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
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
S7442 WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
Nature, 2022, 10.1038/s41586-022-04967-9
Cancers -Basel, 2021, 13-246181
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).
Nat Commun, 2023, 14(1):1399
Nat Commun, 2023, 14(1):1399
Mol Cancer, 2022, 21(1):97
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.
Front Pharmacol, 2022, 13:924523
Microbiol Spectr, 2022, e0219321
S7851 AZD3264 AZD3264 is a novel IKK2 inhibitor.
Redox Biol, 2017, 11:562-576
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
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
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
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.
J Exp Clin Cancer Res, 2022, 41(1):174
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
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.
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.
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.
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.
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-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. 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.
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 Cancer, 2024, 10.1038/s43018-023-00712-x
Redox Biol, 2024, 70:103072
Cell Death Dis, 2024, 15(1):70
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.
Vet Microbiol, 2024, 290:109973
Cell Rep, 2023, 10.1016/j.celrep.2023.113352
Cell Rep, 2023, 42(2):112127
S1396 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.
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
Cell Death Dis, 2023, 14(6):367
Antiviral Res, 2023, 216:105674
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.
Life Sci Alliance, 2024, 10.26508/lsa.202101282
Cell, 2023, 186(22):4851-4867.e20
J Clin Invest, 2023, 133(4)e162190
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.
Theranostics, 2024, 14(3):1224-1240
Cell Mol Gastroenterol Hepatol, 2024, S2352-345X(24)00005-5
Nat Commun, 2023, 14(1):8082
S7352 Bay 11-7085 BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM.
Theranostics, 2024, 14(2):861-878
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
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 Commun, 2023, 14(1):8082
Clin Cancer Res, 2023, 29(16):3151-3161
Clin Cancer Res, 2023, 29(16):3151-3161
S2864 IMD 0354 IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.
Iran J Basic Med Sci, 2023, 26(8):912-918
Blood, 2022, blood.2021014304
J Immunother Cancer, 2022, 10(7)e005063
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.
Nat Commun, 2023, 14(1):3648
Redox Biol, 2023, 60:102632
Cell Rep, 2023, 42(12):113431
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.
mBio, 2023, 10.1128/mbio.02506-23
Viruses, 2023, 15(5)1112
Cancer Res, 2022, 82(10):1991-2002
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
S3648 Amlexanox Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε.
Signal Transduct Target Ther, 2023, 8(1):246
Signal Transduct Target Ther, 2023, 8(1):246
Nucleic Acids Res, 2022, 50(15):8700-8718
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
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.
Sci Adv, 2024, 10(6):eadk2285
Cell Rep, 2023, 42(2):112127
J Nat Prod, 2023, acs.jnatprod.2c00843
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
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
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.
PeerJ, 2022, 10:e13766
Exp Eye Res, 2021, 211:108750
Int Immunopharmacol, 2019, 73:17-22
S1681 Mesalazine (5-ASA) Mesalazine (5-ASA) 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
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
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).
Nat Commun, 2023, 14(1):1399
Nat Commun, 2023, 14(1):1399
Mol Cancer, 2022, 21(1):97
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.
Front Pharmacol, 2022, 13:924523
Microbiol Spectr, 2022, e0219321
S7851 AZD3264 AZD3264 is a novel IKK2 inhibitor.
Redox Biol, 2017, 11:562-576
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
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
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.
J Exp Clin Cancer Res, 2022, 41(1):174
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
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.
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.
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.
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.
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-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. 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.
S7442 WS6 WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
Nature, 2022, 10.1038/s41586-022-04967-9
Cancers -Basel, 2021, 13-246181
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

IκB/IKK阻害剤の選択性比較

Tags: IκB/IKK inhibitor|IκB/IKK agonist|IκB/IKK activator|IκB/IKK inducer|IκB/IKK antagonist|IκB/IKK signaling pathway|IκB/IKK assay kit