MAPK Signaling

R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α.

RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.

SD-06 is a p38 MAP kinase inhibitor; inhibits p38α with an IC50 value of 170 nM and inhibits LPS-stimulated TNF-release in rats (83% inhibition at 1mg/kg, po).IC50 value: 170 nM.

UM-164 is a highly potent inhibitor of c-Src with a Kd of 2.7 nM.

A potent inhibitor of cyclic AMP-dependent protein kinase

A dual inhibitor

LUT014 is a topical B-Raf Inhibitor

Nimbolide is a triterpene derived from the leaves and flowers of Azadirachta indica L. Nimbolide inhibits NF- κ B induces tumor cell apoptosis. Nimbolide inhibited CDK4 / Cdk6 kinase activity. Nimbolide inhibits NF- κ B. Wnt, PI3K Akt, MAPK and JAK-STAT signaling pathways.

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

CompK (compound K), a potent and selective hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) small molecule inhibitor, significantly improves human T-cell functions, with enhanced T-cell receptor avidity to recognize tumor-associated antigens and tumor cytolytic activity by CD8+ T cells.

Fipexide (hydrochloride) is a psychoactive drug of the piperazine class.

IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux.

Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.

D-JNKI-1 (AM-111) (AM-111) is a highly potent and cell-permeable peptide inhibitor of JNK.

p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

trans-Zeatin is a natural cytokinin, a plant growth regulator that plays a central role in plant cell growth, differentiation, and division.

Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.

p38 MAPK-IN-2 is an inhibitor of p38 kinase.

Skatole(3-Methylindole) is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38.

MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC50 of 620 nM.

An activator of TrkB and TrkC

Warangalone (Scandenolone) is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively.

SR-3306 is a selective, potent, highly brain penetrant JNK inhibitor.

DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM.