MAPK

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

KRAS inhibitor-42 (compound 8) is an effective USP7 inhibitor that exhibits high affinity for GDP-bound KRASG12D, with a Ki value of 2.7 μM.

SOS1-IN-11 is an effective inhibitor of SOS1 (IC50 = 30 nM).

RAS/RAS-RAF-IN-1: Potent RAS & RAS-RAF inhibitor, KD 5-15μM for CYPA, antitumor properties.

PROTACKRAS G12D degrader 2 is a peptidomimetic molecule capable of inducing the degradation of SARS-CoV-2 3-chymotrypsin-like protease (3CLPro). Designed as a PROTAC molecule, it combines a dipeptidyl 3CLPro ligand based on GC-376 with a pomalidomide moiety, linked through a piperazine-piperidine linker.

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.

KRAS G12C inhibitor 18 is a potent, orally active compound that inhibits KRAS G12C and exhibits anti-tumor activities.

Andrographolide derivative 31 is an anti-inflammatory that blocks NF-κB, PI3K/Akt, and ERK1/2 MAPK, and restores GSH levels to protect the liver.

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

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.

MRTX1133: Selective inhibitor of KRAS G12D, effective in all protein states, targeting mutant cells.

NK7-902 is a CRBN molecular glue degrader of NEK7. It fully degrades NEK7 in human primary monocytes and whole blood, yet only partially inhibits NLRP3-dependent IL-1β production. NK7-902 results in profound and lasting degradation of NEK7, but only temporarily blocks NLRP3 inflammasome activation in non-human primates via oral administration. The compound demonstrates activity in mouse systems.

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 inhibitor-33 (compound 115a) is a pyrido[2,3-d]pyrimidine derivative that serves as an effective inhibitor of KRAS, exhibiting an IC50 value of ≤ 100nM.

KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer.

HPK1-IN-39 (Compound 10n), a selective inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1) with an inhibitory concentration (IC50) of 29 nM, impedes the

YN14 is a highly potent and selective KRASG12C proteolysis targeting chimera (PROTAC) capable of forming a stable KRASG12C: YN14: VHL ternary complex with low

Sos1, a GEF, activates ERK by converting Ras-GDP to Ras-GTP via Grb2. The PVPPR peptide inhibits this by blocking Sos1/Grb2 binding.

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.

p38 MAP Kinase Inhibitor Ⅵ is a potent p38 MAP Kinase inhibitor with anti-inflammatory activity.

HPK1-IN-19 is a potent inhibitor of hematopoietic progenitor kinase 1 (HPK1).

(+)-Oxanthromicin, an enantiomer of the rare Streptomyces metabolite (−)-oxanthromicin, demonstrates inhibitory activity against K-Ras plasma membrane localization in MDCK cells, exhibiting an IC50 value of 62.5 μM.

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

Antimicrobial agent-21 is a potent mitogen activated protein kinase inhibitor with antibacterial, anti-inflammatory and antitumor activity for the treatment of

A unique collection of 2720 kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;

Pan-KRAS degrader 5 (compound 102) is a cereblon-based PROTAC KRAS degrader with a DC50 value less than 100 nM, exhibiting anticancer activity.

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

Atrovastatin-PEG3-FITC (compound S31) functions as a ligand in fluorescence anisotropy assay. Its primary role is as a KRAS-PDEδ interaction inhibitor.

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.

G12Si-5: covalent K-RasG12S inhibitor, Ki 26 μM, targets S-IIP domain, hinders oncogenic signaling, lowers ERK phosphorylation in mutant cells.

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

4′-Demethylnobiletin, a bioactive metabolite, activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and

PROTAC KRAS G12C degrader-2 (compound 432) acts as a bifunctional modulator, enhancing the hydrolysis of K-Ras protein. One end of this compound features a cereblon inhibitor of apoptosis proteins (IAP), while the other end contains a moiety that binds to KRAS [1].

PROTAC SOS1 Degrader-4 (compound 10) is a potent degrader of SOS1 and exhibits antiproliferative activity [1].

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.

RTIL 13 inhibits dynamin GTPase (IC50: 2.3 μM), targets its lipid binding domain, and suppresses endocytosis (IC50: 9.3 & 7.1 μM).

Braftide is an allosteric inhibitor of BRAF kinase that exerts its effect by targeting the surface of BRAF kinase dimers, thereby preventing their formation. It inhibits both wild-type BRAF and oncogenic BRAFG469A, with IC50 values of 364 nM and 172 nM, respectively. When combined with the TAT sequence, Braftide can suppress the MAPK signaling pathway, inhibiting the proliferation of KRAS-mutant tumor cells, with EC50 values of 7.1 μM for HCT116 and 6.6 μM for HCT-15.

XY-02-082 is a covalent guanosine-mimetic inhibitor targeting G12C KRAS.

6-Thio-GTP (tetrasodium) is an inhibitor of Vav1-Rac. It can suppress TCR-induced T cell proliferation and CD28-mediated T cell survival. In a murine model of allogeneic heart transplantation, 6-Thio-GTP (tetrasodium) demonstrates immunosuppressive effects, which can prolong the survival time of heart transplants.

SIAIS562055, a potent cereblon-based SOS1PROTAC, exhibits a dissociation constant (Kd) of 95.9 nM. It effectively degrades SOS1 and inhibits the downstream ERK pathway. SIAIS562055 disrupts the interaction between KRASG12C or KRASG12D and SOS1, with IC50 values of 95.7 nM and 134.5 nM, respectively. This compound demonstrates strong anticancer activity.

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

ERK1/2 inhibitor 3, a strong ERK1/2 blocker, may aid in cancer and inflammation research.

KRAS inhibitor-24 (compound 115c), a pyrido-pyridine class KRAS inhibitor, exhibits potent activity against KRas G12V, KRas WT, and KRas G12R, with IC50 values all below 100 nM.

KRAS G12D inhibitor 7, is a highly potent inhibitor specifically targeting KRAS G12D.

Pan-KRAS-IN-10 (Compound 58) acts as an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells, specifically AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.7 and 0.24 nM, respectively.

D-JBD19 is a non-permeable peptide with neuroprotective effects.