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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.
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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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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CitedBAY 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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CitedCCCP 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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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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BMS-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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CitedBX795
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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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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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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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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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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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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BI605906
T14567960293-88-3
BI605906 is an IKKβ inhibitor that inhibits tumor necrosis factor alpha-dependent IkappaB degradation and expression of the pro-inflammatory mediator interleukin-6, which can be used to study inflammatory skin diseases such as psoriasis.
- $30
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Amlexanox 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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CitedBardoxolone 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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CitedGSK319347A
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.
- $67
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Protosappanin A
TJS1779102036-28-2
Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.
- $89
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BAY-985
T104772409479-29-2
BAY-985 is a potent, selective, and orally active ATP-competitive dual inhibitor of TBK1 and IKKε (IC50s: 2 30 and 2 nM for TBK1 (low high ATP) and IKKε) with antitumor efficacy.
- $175
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TRAM-34
T6186289905-88-0
TRAM-34 (Triarylmethane-34) (Kd=20 nM), an effective and specific inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1), does not block cytochrome P450. The selective activity of TRAM-34(TRAM 34) is 200 to 1500-fold than other ion channels.
- $43
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PS-1145
T3094431898-65-6
PS-1145 (IKK Inhibitor X) is a specific IKK inhibitor with IC50 of 88 nM.
- $42
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IMD-0354 Cited
T6141978-62-1
IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor that blocks IκBα phosphorylation in the NF-κB pathway.
- $40
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CitedNF-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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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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CitedWS6
T21061421227-53-3
WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
- $30
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