Ibetazol is an inhibitor for importin β1 (KPNB1), that inhibits that binds to Cys585 of importin β1, inhibits the importin β1 mediated nuclear import with an EC50 of 6.1 µM.

AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model.

6-Thio-GTP (tetrasodium) is a Vav1-Rac inhibitor. 6-Thio-GTP (tetrasodium) inhibits TCR-stimulated T cell proliferation and CD28-mediated T cell survival. 6-Thio-GTP (tetrasodium) has an immunosuppressive effect in a mouse cardiac allograft transplant model and prolongs cardiac allograft survival.

IODVA1 is a small molecule with cellular inhibitory activity against several transformed cell lines including Ras-driven cells, targets Rac activation and signaling instead of Ras; IODVA1 inhibits ST8814 cell proliferation with GI50 of 1 uM, similar results were observed with MCF7, MDA-MB-231, and T47D cells with estimated GI50s <1 uM. IODVA1 significantly decreases number of colonies of the breast cancer cells in soft agar at 1 and 3 uM. IODVA1 probably does not bind Ras and that its mechanism of action is likely Ras-independent, inhibits lamellipodia and circular dorsal ruffle (CDR) formation in MDA-MB-231 cells and decreases Rac activation. IODVA1 inhibits Rac activation and downstream signaling leading to inhibition of lamellipodia and CDR formation; IODVA1 inhibits cell-substratum and cell-cell interactions, does not target kinases, and reduces tumor burden of solid tumors in vivo.

BC-DXI-32982 is a potent inhibitor of the interaction between DX2 and KRAS4B with a half-maximal inhibitory concentration (IC50) of 0.18 μM, showing little effect on the PRKACA-PRKAR2A interaction.

DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.

KAL-21404358 (KAL21404358) is a small-molecule, allosteric inhibitor of K-Ras(G12D), binds to K-Ras(G12D) P110 site with KD of 88 uM in MST assay; KAL-21404358 disrupts the K-RasG12D-B-Raf interaction using a NanoBiT split luciferase assay, and to impair the Raf-MEK-ERK and the PI3K-AKT signaling pathways. KAL-21404358 exhibited specificity for K-RasG12D over K-RasWT, H-RasWT, Rap1a, R-Ras and R-Ras2.

Ras binder 2C07 is a switch-II binding ligand which binds Ras GDP and GTP states.

RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.

Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.

LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the  KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively.

SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.

SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.

SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein.

RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.

G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.

Fulzerasib is a potent selective inhibitor of KRAS gene mutation.

ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.

CSC01 is a small molecule inhibitor of oncogenic KRAS mutant G13D (KRAS-G13D).

BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.

ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells.

ADT-007 (ADT007) is a potent, specific pan-RAS inhibitor, shows potential to circumvent resistance to mutant-specific KRAS inhibitors and activates antitumor immunity.

ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.

6H05 is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C), an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors..

A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..

RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively.

ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound..

ARS-1323 is a novel inhibitor of mutant K-ras G12C.

LY-3537982 (LY3537982) is a highly selective and potent KRAS-G12C inhibitor, selectively inhibits growth of KRAS G12C mutant cells (IC50=1-60 nM).LY-3537982 does not inhibit growth of KRAS G12S/G13C/G12D mutant cells and WT KRAS cells (CI50>10 uM).LY-3537982 displays high selectivity for proteome-wide cysteine residues was evaluated using competitive chemical proteomics (8866 peptides).LY3537982 inhibits the growth of subcutaneous EL3187 NSCLC PDX tumors in nude mice in a dose dependent manner.LY3537982 demonstrates robust tumor regression in combination with other agents in KRAS G12C in vivo models.LY3537982 is a promising KRAS G12C inhibitor predicted to deliver >90% KRAS G12C target occupancy in the clinic.

MRTX0902 is a potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).