MAPK

FAM49B (190-198) mouse represents a peptide fragment of the mitochondria-localized protein FAM49B, which is instrumental in regulating mitochondrial fission, function, and integrity, in addition to influencing tumor progression. Beyond its role in mitochondrial dynamics, FAM49B serves as a negative regulator of T cell activation by inhibiting GTPase Rac activity and affecting cytoskeleton reorganization.

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.

Endothelin-1 (1-31) is a human-derived vasoconstrictor and hypertensive formed by chymase hydrolysis of big ET-1.

ADT-007 is a pan-RAS inhibitor with potent anticancer activity.

KRAS G12C inhibitor 20 is a KRAS G12C inhibitor.

MRTF-A-IN-1 (compound 14) is an inhibitor of MRTF-A. It effectively suppresses cell proliferation and induces senescence in HCC cells.

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

NecroX-2 is a cell-permeable necrosis inhibitor with antioxidant properties. NecroX-2 selectively suppresses necrotic cell death triggered by oxidative stress. NecroX-2 does not confer protection against apoptosis induced by staurosporine or etoposide but shows protective effects under conditions such as cold shock, hypoxia, and oxidative stress in vitro.

Negative control for LC 2.

14.3.3 protein antagonist, blocks binding to Raf-1/Bad/ASK1/exoenzyme S, competitive, no phosphorylation needed, KD ~80 nM.

Ibetazol is an inhibitor of importin β1 (KPNB1), which functions by binding to Cys585 of importin β1, thus preventing importin β1-mediated nuclear import with an EC50 of 6.1 µM.

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.

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

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

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.

PPM-3, a selective PROTAC ERK5 degrader, exhibits a potent inhibitory concentration (IC 50) of 62.4 nM.

KRAS Inhibitor-38 (Example 18) is a potent inhibitor capable of effectively suppressing the activity of KRAS G12C, KRAS G12D, and KRAS G12V in vivo.

MRTX849 is a KRAS G12C ligand and PROTAC linker for creating potent LC-2, degrading KRAS G12C with DC50 of 0.25-0.76 μM.

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

(S,R,S)-AHPC-Me-C10-Br is a chemically synthesized conjugate and ligand-linker for E3 ligase, MS432 for MEK1/2 inhibitors and a VHL E3 ligase linker.