MAPK Signaling

p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC50 of 68 nM.

ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.

An ERK inhibitor

GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.

MK2-IN-1 (MK2 Inhibitor) is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

ERK-IN-1 (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. ERK-IN-1 hydrochloride can also inhibit RAF.

SJFα is a 13-atom linker PROTAC based on von Hippel-Lindau ligand. SJFα degrades p38α with a DC50 of 7.16nM, but is far less effective at degrading p38δ (DC50=299nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5μM.

SJFδ is a 10-atom linker PROTAC based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC50 of 46.17nM, but does not degrade p38α, p38β, or p38γ.

Balamapimod (MKI 833) (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.

MEK-IN-1 is a MEK inhibitor extracted from patent WO2008076415A1.

Rehmannioside A is an inhibitor of cytochrome P450 enzymes (CYP3A4, 2C9, and 2D6), with IC 50 values of 10.08, 12.62, and 16.43μM, respectively.

Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.

Lidocaine hydrochloride (Lignocaine hydrochloride) is an amino-amide-type local anaesthetic that inhibits voltage-insensitive ‘flicker’ K + channel with an IC 50 value of 220μM.

Isovitexin (Saponaretin) extracted from rice hulls of Oryza sativa , possesses various biological activities, including anti-inflammatory and antioxidant activities.

Omtriptolide (PG490-88) is a derivative prodrug of triptolide purified from the Chinese herb.

TBHQ(tert-Butylhydroquinone) is a powerful phenolic antioxidant capable of reducing oxidative stress and inflammatory reactions.

Talmapimod (SCIO-469) (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod (SCIO-469) shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.

Tauroursodeoxycholate (TUDCA) is a cytoprotective agent in a variety of cells including hepatocytes as well as an inducer of apoptosis in cancer cells[1].

A potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor

GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.

L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.

An ERK5 inhibitor

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of? 5.6 ?M, 8.8 ?M, 29 ?M, and 52 ?M, respectively.