IKK Inhibitor

BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC₅₀ of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription.

IMD-0560 is a novel IκB kinase β inhibitor.

Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.

TLR4/NF-κB-IN-1 (Compound 7x) is an orally available inhibitor that specifically targets the TLR4/NF-κB signaling pathway, offering anti-inflammatory effects and the ability to cross the blood-brain barrier. TLR4/NF-κB-IN-1 can reduce acute neuroinflammation in mice caused by LPS (HY-D1056) and downregulate the expression of TLR4, P-NF-κB and P-IκB-α proteins.

HPN-01 is a potent and selective IKK inhibitor, with pIC₅₀ values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.

LLVK TFA is a selective IκB phosphorylation inhibitor. LLVK TFA reduces LPS-induced pro-inflammatory cytokines (IL-1β, IL-6, TNF-α). LLVK TFA is promising for research of inflammatory bowel disease and rheumatoid arthritis.

IKKβ-IN-4 (compound 14) is an IkappaB kinase-β ( IKKβ ) inhibitor with IC₅₀ value of 1.9 μM. IKKβ is a key enzyme in the NF-κB signaling pathway and is involved in the development of many diseases.

PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC₅₀ of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model.

Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC₅₀ values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.

(9S,13R)-12-Oxo phytodienoic acid ((9S,13R)-12-OPDA) is a mPGES-1 inhibitor and Nrf2 activator. (9S,13R)-12-Oxo phytodienoic acid selectively inhibits mPGES-1 expression and reduces inducible PGE₂ production without affecting COX-1 or COX-2. (9S,13R)-12-Oxo phytodienoic acid inhibits the phosphorylation of IKKβ, IκBα, and NF-κB (p65), blocks the nuclear translocation of p65, increases the nuclear translocation of Nrf2, and upregulates HO-1 expression. (9S,13R)-12-Oxo phytodienoic acid inhibits the differentiation of M0 macrophages toward the M1 phenotype and promotes differentiation toward the M2 phenotype. (9S,13R)-12-Oxo phytodienoic acid decreases the levels of NO, PGE₂, IL-1β, IL-6, iNOS, and PGD₂. (9S,13R)-12-Oxo phytodienoic acid can be used for inflammation research.

Lucidenic acid B is a triterpenoid compound. Lucidenic acid B inhibits the activities of ERK1/2, AP-1, NF-kB, and IKK, suppresses PMA (Phorbol 12-myristate 13-acetate) (HY-18739)-induced MMP-9 expression and cell invasion, and induces apoptosis in leukemia cells via the mitochondrial pathway. Lucidenic acid B inhibits the growth of various cancer cell lines without affecting normal lymphocytes and does not induce G1 phase arrest or necrosis. Lucidenic acid B can be used in research on hepatocellular carcinoma, human acute promyelocytic leukemia, and skin tumor promotion.

5-(3',4'-Dihydroxyphenyl)-γ-valerolactone is an intestinal microbiota metabolite of (-)-Epicatechin (HY-N0001). 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone downregulates TNF-α-stimulated phosphorylation of IKK and IκBα, inhibits the transcriptional activation of NF-κB, and suppresses the expression of adhesion molecules and chemokines. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone promotes autophagy, alleviates oxidative stress, maintains osteoblast differentiation, induces G₁ phase arrest, inhibits adipogenesis, and scavenges ABTS free radicals. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone inhibits the adhesion of uropathogenic Escherichia coli to bladder epithelial cells; when used in combination with Curcumin (HY-N0005), it downregulates the NLRP3 and NOX2/Nrf2 signaling pathways, thereby reducing microglial activation. 5-(3',4'-Dihydroxyphenyl)-γ-valerolactone can be used in research related to diabetes, atherosclerosis, osteoporosis, obesity, neurodegenerative diseases involving microglial activation, and urinary tract infections.

CDDO-biotin is an IKKβ inhibitor with cancer cell inhibitory activity. CDDO-biotin directly interacts with and oxidizes Cys-179 in the activation loop of IKKβ, forming an adduct with wild-type IKKβ. CDDO-biotin can be used in the research of myeloid leukemia, osteosarcoma, multiple myeloma, lung cancer, breast cancer and pancreatic cancer.

4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.

MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC₅₀ of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.

Vinpocetine (Standard) is the analytical standard of Vinpocetine. This product is intended for research and analytical applications. Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na⁺ channels. The IC₅₀ value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.

MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC₅₀s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC₅₀s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.

PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model.

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC₅₀s of 9 nM and 72 nM, respectively.

(Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC₅₀ of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects.