MAPK

Rac1 Inhibitor F56, control peptide TFA, is a peptide containing Rac1 residues 45-60. It features a mutation from Trp56 to Phe56. This inhibitor does not affect the interaction between Rac1 and guanine nucleotide exchange factors (GEFs).

ERK2IN-5 (Compound 5g) is an inhibitor of ERK2 and demonstrates good affinity for both ERK2 and JNK3, with Ki values of 86 nM and 550 nM, respectively.

GGDPS-IN-1 (Compound 37) is an inhibitor of geranylgeranyl diphosphate synthase (GGDPS) with an IC50 of 49.4 nM, disrupting protein geranylgeranylation in myeloma cells.

KRASG12C IN-14 (compound 15), a potent inhibitor specifically designed for the KRAS G12C mutation, exhibits impressive efficacy in impeding CYPA-dependent KRAS-BRAF interaction and ERK phosphorylation in NCI-H358 cells, both with an IC 50 of 0.002 μM.

Z16078526 promotes Ucp1, p38 MAPK, lipolysis, thermogenic genes, and mitochondrial activity in mouse brown adipocytes.

PDE4-IN-26 (Compound A5) is an orally active, highly selective inhibitor of PDE4. It exhibits anti-inflammatory properties by inhibiting p38 MAPK phosphorylation. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 reduces lung inflammation, damage, and fibrosis, while promoting sputum secretion and alleviating cough. It is useful for researching lung injury-related diseases.

DS03090629, an orally active MEK inhibitor, functions by competitively inhibiting MEK activity in the presence of ATP. This compound demonstrates strong binding affinity to both MEK and phosphorylated MEK, with dissociation constants (Kd) of 0.11 and 0.15 nM, respectively. It has shown efficacy in suppressing the proliferation of melanoma cell lines that overexpress BRAF mutations, achieving IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 is thus considered promising for anti-melanoma therapies.

KRAS G12D inhibitor 17, a quinazoline-linked prolinamide, degrades mutant KRAS protein; a PROTAC.

Eicosapentaenoic acid is metabolized, in part, through cytochrome P450-catalyzed epoxidation followed by conversion to the vicinal diols by epoxide hydrolases.

NK7-902 TFA is a CRBN molecular glue degrader of NEK7. It effectively degrades NEK7 in human primary monocytes and whole blood, yet only partially inhibits NLRP3-dependent IL-1β production. While NK7-902 TFA achieves deep and lasting NEK7 degradation, it temporarily blocks NLRP3 inflammasome activation in non-human primates when administered orally. Additionally, NK7-902 TFA demonstrates activity in mouse systems.

A unique collection of 365 compounds targeting MAPK signaling for drug discovery in MAPK related diseases;

Tagarafdeg (CFT1946) is a PROTAC degradator targeting mutant BRAF, capable of degrading BRAF V600E, G469A, G466V mutations, anti proliferation.

IPS-06061 is an orally active molecular glue that forms a ternary complex with CRBN and KRASG12D, capable of degrading KRAS G12D, with a DC50 of less than 500 nM.

Inactive analog of U0126(MEK-1/2 inhibitor), used as a negative control

SHP2-IN-38 is an innovative green fluorescent inhibitor targeting SHP2, exhibiting IC50 values as follows: 2.89 μM (SHP2), 8.73 μM (SHP1), 11.08 μM (PTP1B), and 33.07 μM (TCPTP). It impedes the SHP2-mediated ERK signaling pathway and inhibits MV4-11 cell proliferation in vitro with an IC50 of 7.90 μM. The excitation wavelength of SHP2-IN-38 is 360 nm, with a maximum emission wavelength of 550 nm in DMSO and 540 nm in DMF. Additionally, it demonstrates green fluorescent imaging in HeLa cells and zebrafish.

PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2

JNK3 inhibitor-8: potent, selective, oral, BBB-penetrating, IC50: JNK3=21 nM, JNK2=2203 nM, JNK1>10,000 nM; potential in Alzheimer's research.

HPK1-IN-8 is an allosteric, inactive, conformation-selective triazolopyrimidine ketone HPK1 inhibitor.

MS432 is a highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2.

Negative control for LC 2.