- IκB
- IKK
IKK 选择性抑制剂 | 调节剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| 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. | Selective | |
| 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. | Selective | TBK1, IC50: 1.0 nM; IKKε, IC50: 5.6 nM |
| 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). | Selective | TBK1, IC50: 2 nM; TBK1, IC50: 30 nM; IKKε, IC50: 2 nM |
| 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. | Selective | IKK2, IC50: 17.9 nM |
| 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. |
Selective | IKKϵ, IC50: 160 nM; TBK1, IC50: 19 nM |
| S7697 | LY2409881 | LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. | Selective | IKK2, IC50: 30 nM |
| 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. | Selective | IKK2, IC50: 40 nM; IKK1, IC50: 200 nM; IKK complex, IC50: 70 nM |
| 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. | Selective | recombinant IKKβ, IC50: 45 nM |
| S7691 | PS-1145 | PS-1145 is a specific IKK inhibitor with IC50 of 88 nM. | Selective | IKK, IC50: 88 nM |
| 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. | Selective | IKKϵ, IC50: 160 nM; TBK1, IC50: 190 nM |
| 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. | Selective | IKK2, IC50: 0.3 μM; IKK1, IC50: 4 μM |
| 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. | Selective | IKK β, IC50: 1 μM |
| 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 po | Selective | IKKβ, IC50: 1 μM |
| 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. | Selective | IKKα, IC50: 8.975 μM; IKKβ, IC50: 3.598 μM |
| 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. | Selective | IKK2, IC50: 3 μM-12 μM |
| 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. | Selective | IKK β, IC50: 12 μM |
| S7441 | WS3 | WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. | Selective | |
| S3648 | Amlexanox | Amlexanox is an anti-inflammatory antiallergic immunomodulator and also an inhibitor of the protein kinases TBK1 and IKK-ε. | Selective | |
| 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. | Selective | |
| S7851 | AZD3264 | AZD3264 is a novel IKK2 inhibitor. | Selective | |
| 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. | Selective | |
| 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. | Selective | |
| S1681 | Mesalazine (5-ASA) | Mesalazine (5-ASA) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease. | Selective | |
| S2864 | IMD 0354 | IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. | Selective | |
| S7442 | WS6 | WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. | Selective | |
| 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. | Pan |
