MAPK

KRAS G12C Inhibitor 60 (compound 23), a selective inhibitor targeting the Kras-G12C mutation, is utilized in the investigation of lung, colorectal, and

HPK1-IN-4 is an HPK1 (MAPK41) inhibitor with an IC 50 of 0.061 nM. HPK1-IN-4 is often used as a preclinical immunotherapy tool compound.

Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.

MEK/RAF-IN-1 (Compound 16b) serves as an inhibitor targeting both MEK and RAF, demonstrating potent efficacy with IC 50 values reported at 28 nM for MEK1, and 3 nM for both BRAF and BRAFV600E. This compound exhibits significant antitumor capabilities, effectively curbing cell proliferation in vitro in MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Furthermore, MEK/RAF-IN-1 significantly restricts tumor growth in xenograft mouse models employed in the study of colorectal cancer.

Klotho-derived peptide 1 (KP1 human) hydrochloride inhibits the interaction between TGF-β and TGF-β receptor 2, suppressing the activation of TGF-β-induced Smad2/3 and mitogen-activated protein kinase (MAPK). Additionally, it exhibits antifibrotic and renal protective effects in mouse models.

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.

Mitogen-activated protein kinase 1 (MAPK1) activates the p38/NF-κB pathway and regulates cellular processes in sepsis-associated diseases.

HSND80 (Compound 1) is an orally active MNK/p70S6K inhibitor, exhibiting a Kd value of 44 nM for MNK1 and 4 nM for MNK2. The residence time of HSND80 on MNK1 and MNK2 is 45 minutes and 58 minutes, respectively. HSND80 effectively inhibits non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppresses the growth of triple-negative breast cancer (TNBC) cells in vitro.

NUCC-0200808 (Compound 12g) is an MNK1 inhibitor with an IC₅₀ of 42 nM. It reduces eIF4E phosphorylation and cell viability in AML cells and induces apoptosis. NUCC-0200808 shows potential for research in the field of leukemia.

Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib which is a selective MEK inhibitor.

A unique collection of xnum cancer cell differentiation inducing compounds for high throughput and high content screening;

BI1701963 is an orally effective inhibitor that targets the SOS1 and KRAS interaction, specifically inhibiting the activation of KRAS by blocking its GTP loading. This compound is utilized in cancer research to explore potential therapeutic effects against KRAS-driven malignancies.

KRAS G12C inhibitor 20 is a KRAS G12C inhibitor.

Fluconazole-PEG6-XMU-MP-9, PEG-linked conjugate, fluconazole antifungal plus XMU-MP-9, promotes Nedd4-1 mediated K-Ras mutant degradation.

PPARγagonist-21 (Compound 9a) is a PPARγ agonist with an EC₅₀ of 3.12 μM. It inhibits NF-κB by activating PPAR-γ and reduces the assembly of the NLRP3 inflammasome. PPARγagonist-21 blocks interactions between NLRP3-ASC and NLRP3-NEK7, alleviating the severity of gouty arthritis.

Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the ubiquitination and proteasomal degradation of the oncogenic protein.

TAT-PAK18 R192A is an inactive Tat-Pak peptide. It does not influence Rac1 translocation triggered by any tested proteins.

(RS)-G12Di-1 is a selective covalent inhibitor of K-Ras-G12D.

KRAS-IN-43 (Compound 9) is a broad-spectrum KRAS inhibitor with IC50 values of 0.15 μM for KRASG12V, 0.14 μM for KRASG12C, and 0.47 μM for wild-type KRAS. It disrupts the interaction between KRAS and cRAF and suppresses ERK phosphorylation. KRAS-IN-43 shows potential for research in KRAS mutation-associated cancers, including pancreatic, colorectal, and lung cancers.

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