MAPK Signaling

EF24 is a novel synthetic curcumin analog.

B-Raf IN 2 is a potent and selective BRAF inhibitor extracted from patent WO2021116055A1, compound Ia. B-Raf IN 2 can be used for the research of cancer.

MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2).

MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1.

PLX7922, a RAF inhibitor, can bind with BRAFV600E. PLX7922 inhibits pERK in BRAFV600E cell lines, and activates pERK in mutant NRAS cell lines.

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2.

TRi-1 is a potent, specific, and irreversible inhibitor of TXNRD1 and TXNRD2 with IC 50 values of 18nM and 44nM.

MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.

DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96).

Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei.

EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively.

Andrograpanin, a bioactive compound from Andrographis paniculata, exhibits anti-inflammatory and anti-infectious properties.

GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers.

B-Raf IN 10 (Compound C09) is a BRAF inhibitor with an IC50 between 50 and 100 nM. B-Raf IN 10 shows antitumor activity.

ACA-28 (compound 2a) is an effective ERK MAPK signaling regulator. ACA-28 induces apoptosis through excessive activation of ERK and selectively inhibits cancer cell growth. ACA-28 inhibits the growth of melanoma cells (SK-MEL-28) and normal melanocytes (NHEM), with IC50 values of 5.3 and 10.1 μM, respectively.

Anti-inflammatory agent 35 (compound 5a27) is an orally effective curcumin analogue with anti-inflammatory activity. It can block the signaling of mitogen-activated protein kinase (MAPK) and nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits neutrophil infiltration and proinflammatory cytokine production in vitro. In vivo studies have shown that Anti-inflammatory agent 35 significantly alleviates acute lung injury (ALI) induced by lipopolysaccharide (LPS).

BSJ-04-122 is a covalent dual inhibitor of MKK4/7. It inhibits both MKK4 and MKK7 with IC50 values of 4 nM and 181 nM, respectively. BSJ-04-122 can be used in cancer research.

Cyclocurcumin is an effective inhibitor of p38α. It has anti-rheumatic, anti-vasoconstrictive and antioxidant activities.