Transcription Factors

BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.

Sivelestat sodium tetrahydrate is a specific inhibitor of neutrophil elastase with an IC 50 value of 14nM.

Ginsenoside CK, a secondary ginsenoside biotransformed from major ginsenosides, is more bioavailable and soluble than its parent ginsenosides and holds great significance.

(±)8(9)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid.

(±)8(9)-EET is biosynthesized in rat and rabbit liver microsomes by CYP450.

2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is a compound that structurally mimics 2-oxoglutarate (2-OG, also known as α-ketoglutarate) and chelates zinc, thus affecting a range of enzymes.

Cancer cell survival appears partly dependent on antioxidative enzymes, whose expression is regulated by the Keap1-Nrf2 pathway, to quench potentially toxic reactive oxygen species generated by their metastatic transformation.

Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).

Berteroin is a sulforaphane analog found in cruciferous vegetables including Chinese cabbage, rucola salad leaves, and mustard oil.

BMS 345541 is a cell permeable inhibitor of the IκB kinases IKKα and IKKβ (IC50s = 4 and 0.3 μM).

BMS 470539 (hydrochloride) is a highly selective and potent melanocortin-1 receptor (MC-1R) agonist. In cAMP accumulation assays, its EC 50 values for human and mouse MC1R are 16.8 and 11.6nM, respectively.

ETS variant 1 (ETV1) is a transcription factor oncogene implicated in several cancers where it has been altered by chromosomal translocation, gene amplification, or lineage dysregulation.

Butyrolactone I is an ATP competitive inhibitor of cyclin-dependent kinase 1 (CDK1) with oral activity (the IC 50 value of cdc2 kinase in PC-14 cells was 20μg/ml).

C8 Galactosylceramide is a synthetic C8 short-chain derivative of known membrane microdomain-forming sphingolipids.

CAY10575 (Compound 8) is an IKK2 inhibitor with an IC50 of 0.075 μM.

Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer.

(±)-Nutlin-3 blocks the interaction of p53 with its negative regulator Mdm2 (IC50 = 90 nM), inducing the expression of p53-regulated genes and blocking the growth of tumor xenografts in vivo.

CCG-232601 is an inhibitor of the Rho/MRTF/SRF transcriptional pathway and a derivative of CCG-203971.

D,L-1′-Acetoxychavicol acetate is a natural compound first isolated from the rhizomes of ginger-like plants.

Nrf2 activation of the antioxidant response element (ARE) is central to cytoprotective gene expression against oxidative and/or electrophilic stress.

An inhibitor of Mediator/Pdr1 interactions

Inhibitor of NF-κB kinase 2 (IKK2, also known as IKKβ) acts as part of an IKK complex in the canonical NF-κB pathway, phosphorylating inhibitors of NF-κB (IκBs) to initiate signaling.

ML-180 is an inverse agonist of liver receptor homolog-1 (LRH-1, IC50 = 3.7 μM) with maximum efficacy of 64% repression.

NF-κB inhibitor is a synthetic peptide corresponding to the nuclear localization sequence (NLS) of NF-κB p105 subunit (also known as p50) appended to a hydrophobic sequence to facilitate import into living cells.