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NF-κBIκB/IKK
The IκB kinase (IKK) is an enzyme complex that is involved in propagating the cellular response to inflammation.The IκB kinase enzyme complex is part of the upstream NF-κB signal transduction cascade. The IκBα (inhibitor of nuclear factor kappa B) protein inactivates the NF-κB transcription factor by masking the nuclear localization signals (NLS) of NF-κB proteins and keeping them sequestered in an inactive state in the cytoplasm. Specifically, IKK phosphorylates the inhibitory IκBα protein. This phosphorylation results in the dissociation of IκBα from NF-κB. NF-κB, which is now free, migrates into the nucleus and activates the expression of at least 150 genes; some of which are anti-apoptotic.
Resveratrol
Cited
T1558501-36-0
Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.
- $36
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Cited
T15243251303-04-5In house
Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.
- $84
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BAY 11-7082 Cited
T190219542-67-7
BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that suppresses TNFα-induced IκBα phosphorylation (IC50=10 μM) and also inhibits the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19 0.96 μM).
- $43
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CitedKurarinone
T5S099334981-26-5
Kurarinone is a flavonoid extracted from the shrub Sophora flavescens, which has anti-tumor, estrogenic and anti-inflammatory activities, and also has a strong inhibitory effect on immune responses.
- $39
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CCCP Cited
T7081555-60-2
CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.
- $41
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CitedRosmarinic acid Cited
T276520283-92-5
Rosmarinic acid (Labiatenic acid) is widely found in plants and has antioxidant, anti-inflammatory, and antibacterial activities. It inhibits MAO-A, MAO-B, and COMT with IC50 of 50.1, 184.6, and 26.7 μM respectively.
- $36
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CitedBMS-345541 Cited
T6326445430-58-0In house
BMS-345541 (IKK Inhibitor III) is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.
- $32
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CitedGSK8612
Cited
T55402361659-62-1
GSK8612 is a highly selective and potent inhibitor of Tank-binding Kinase-1 (TBK1, pIC50: 6.8).
- $39
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CitedAllicin
T3123539-86-6
Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.
- $40
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Peramivir
T21339330600-85-6
Peramivir (BCX1812) is a highly selective influenza A and B neuraminidase inhibitor with antiviral activity and anti-cytokine effects, which can be used in the study of novel coronavirus and influenza virus infections.
- $30
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BX795
T1830702675-74-9
BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
- $54
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Plantainoside D
T5796147331-98-4
Plantainoside D (Isoplantamajoside) shows potent antioxidative effects as those of ascorbic acid, it shows angiotensin-converting enzyme (ACE) inhibitory inhibitory activity in vitro with the IC(50) value of 2.17 mM, it also shows inhibitory activity against PKCalpha with the IC50 value14.8microM.
- $122
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Bay 11-7085 Cited
T1934196309-76-9
Bay 11-7085 can irreversibly inhibit the IκBα phosphorylation induced by TNFα (IC50: 10 μM).
- $30
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CitedIKK 16
T6176873225-46-8
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, respectively.
- $34
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T628262519537-70-1
HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. As a derivative of HOIPIN-1, it exhibits 255-fold greater inhibition of both petit-LUBAC and TNF-α-mediated NF-κB activation compared to HOIPIN-1. HOIPIN-8 is a promising tool to explore cellular functions of LUBAC.
- $64
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Bardoxolone Methyl Cited
T6165218600-53-4
Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway with potential anti-tumor and anti-inflammatory activities.
- $39
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CitedDehydrocostus Lactone Cited
T2833477-43-0
Dehydrocostus Lactone ((-)-Dehydrocostus lactone) shows anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.
- $39
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CitedADU-S100
T10252L31638241-89-0
ADU-S100 (MIW815) is a cyclic dinucleotide (CDN) class STING agonist that significantly induces the production of IFN-β and pro-inflammatory cytokines TNF-α, IL-6, and MCP-1, induces TBK1 and IRF3 phosphorylation, and exhibits antitumour activity.
- $499
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TPCA-1 Cited
T3049507475-17-4
TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes.
- $38
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CitedAmlexanox Cited
T163968302-57-8
Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.
- $32
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CitedMLN120B
TQ0306783348-36-7
MLN120B is a selective and ATP competitive IKKβ inhibitor (IC50: 60 nM).
- $45
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GSK319347A
T15558862812-98-4
GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma.
- $64
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NF-κB-IN-1
T91051227098-15-8
NF-κB-IN-1 (1,6-Heptadiene-3,5-dione, 1,7-bis(3,4-dimethoxyphenyl)-4-[(4-hydroxy-3-methoxyphenyl)methylene]-, (1E,6E)-) is a potent NF-κB signaling pathway inhibitor. It is a 4-arylidene crucumin analogue. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
- $169
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Desmethoxyyangonin
T5S073415345-89-8
1. Desmethoxyyangonin (5,6-Dehydrokavain) protects LPS or LPS D-GalN-induced damages in cell or liver tissues mainly through de-regulating IKK NFκB and Jak2 STAT3 signaling pathways. 2. The induction of CYP3A23 by dihydromethysticin and Desmethoxy yangonin involves transcription activation, probably through a PXR-independent or PXR-involved indirect mechanism.
- $58
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