MAPK Signaling

A potent inhibitor of B-Raf

CHPG Sodium salt is a selective metabotropic glutamate receptor 5 (mGlu5) agonist.

MEK1/2 inhibitor

A RAF inhibitor

Yoda1 is an effective selective agonist of Piezo1 with an EC 50 value of 17.1μM in mice.

Lysophosphatidylcholines is an important class of phospholipid molecules, which are the products of phosphatidylcholine hydrolysis by phospholipase A2.

GNE-495 is an orally bioavailable, potent, and selective MAP4K4 inhibitor (IC50 = 3.7 nM).

SB 202190 is a potent, selective, and cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.

Skyrin is a fungal metabolite characterized by a bisanthraquinone structure.

p38 MAPK Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively.

Damaged DNA in humans is detected by sensor proteins that transmit a signal through checkpoint kinases (Chks) Chk1 and Chk2.

Reticulol is an isocoumarin derivative produced by certain species of Streptomyces that inhibits cAMP phosphodiesterase (IC50 = 41 uM).

Obscurolide A1 is a natural butyrolactone isolated from S.

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 uM for p38α.

ASK1-IN-1 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.

AZD-0364 (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

BGB-283 is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 uM, 0.38±0.06 uM and 3.9±1 uM for GRK2, GRK5 and GRK1, respectively.

CCT196969, a pan-Raf inhibitor, inhibits B-Raf with an IC50 of 0.1 uM.

Tomivosertib is an orally active MNK1/2 inhibitor (IC 50 = 1–2nM).

GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM.

LXH254 is a potent CRAF inhibitor extracted from patent WO2018051306A1, Compound A.

LY3214996 (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. LY3214996 shows potent antitumor activities in cancer models with MAPK pathway alterations.

NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.