n-ras

Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9 5.2 2.8 nM).

Pan-RAS-IN-1 is an inhibitor of pan-Ras. It disrupts the interaction of Ras proteins and their effectors.

Pan-RAS-IN-7 (Compound D101) is a broad-spectrum RAS inhibitor used in the synthesis of antibody-drug conjugates (ADCs). It is also applicable in cancer research.

Pan-RAS-IN-2 (compound 6A) is a molecular glue that specifically targets RAS molecules, exhibiting significant inhibitory activity on the proliferation of RAS-mutated cell lines. It forms a ternary complex with cyclophilin A (CYPA) and RAS(ON) proteins, which blocks the downstream binding of RAF to RAS, thereby exerting antitumor effects.

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.

LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8 1.2 2.0 nM toward H N K-ras).

UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) is a potent ICMT inhibitor with an IC50 of 2 μM which is selective against the other enzymes involved in the post-translational modifications of Ras.

K-Ras-IN-1, a K-Ras inhibitor, is characterized by its chemical formula C20H19ClN4O2S and is also known as N-[(1S)-3-cyclopropyl-1-[(6-fluoro-1H-benzimidazol-2-yl)sulfanyl]-2-oxo-1-(phenylmethyl)propyl]-4-fluorobenzenesulfonamide (compound [18, dashboard 819041] in brackets).

THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a polyethylene glycol (PEG)-based PROteolysis TArgeting Chimera (PROTAC) linker used in synthesizing PROTAC K-Ras Degrader-1, as documented in reference [1].

THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, aids in the synthesis of PROTAC K-Ras Degrader-1[1].

BBO-10203 (Compound 758) binds to the RBD region of PI3Kα, hindering the interaction of K-, H-, and N-Ras with PI3Kα. It inhibits pAKT with an IC50 of less than 0.1 pM in BT474 cells.

(Rac)-Lonafarnib (Sch66336 racemate) is the racemic form of the potent, orally active farnesyl transferase (FTase) inhibitor, Lonafarnib. It effectively inhibits H-ras, K-ras, and N-ras with IC50 values of 1.9 nM, 5.2 nM, and 2.8 nM, respectively, and exhibits activities against the hepatitis delta virus (HDV).

ABD957, a potent and selective covalent inhibitor of the ABHD17 depalmitoylase family, exhibits an IC 50 value of 0.21 µM against ABHD17B. This compound effectively inhibits N-Ras signaling and suppresses the growth of NRAS-mutant AML cells.

ICMT-IN-7 (compound 74), with an IC50 value of 0.015 µM, functions as an ICMT inhibitor, promotes cytoplasmic accumulation of ICMT in HCT-116 cells in a dose-dependent manner and suppresses the proliferation of various cancer cell lines harboring K-Ras and N-Ras mutations [1].

ICMT-IN-1 (compound 75) is a potent ICMT inhibitor with an IC50 of 0.0013 μM; it promotes dose-dependent cytoplasmic accumulation of ICMT in HCT-116 cells and effectively inhibits the proliferation of various cancer cell lines expressing K-Ras and N-Ras [1].

BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM. BC-LI-0186 competitively binds the RagD interaction site of LRS with Kd of 42.1 nM and has no effect on LRS-vps34, LRS-eprs, RagB-RagD association, mTORC1 complex formation. BC-LI-0186 potently inhibits the activity of tumor-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 can be used for lung cancer-related research.