MAPK

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

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-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.

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

KRAS G12C inhibitor 20 is a KRAS G12C inhibitor.

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

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

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

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.

MC 976 is a derivative of Vitamin D3.

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

Peptide (45-60) blocks Rac1 binding with TrioN, GEF-H1, Tiam1 GEFs.

KRASG12C IN-2 (compound 17) is an orally active inhibitor of KRAS G12C, which effectively suppresses tumor growth in mice [1].

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.

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.

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.

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

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.

(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.

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