Ras

RMC-6236 is a potent RAS(ON)MULTI inhibitor with broad-spectrum inhibitory activity against RAS-GTP and can be used in cancer research.

Rhosin hydrochloride is a specific inhibitor of the RhoA subfamily Rho GTPases and inhibits the RhoA-GEF interaction. Rhosin hydrochloride can significantly induce cell apoptosis without affecting cell cycle progression. [1]

EHT 1864 (EHT 1864 2HCl) is a Rac family GTPase inhibitor that blocks activation by direct binding to Rac1, Rac1b, Rac2, and Rac3 (Kd=40 50 60 250 nM). EHT 1864 inhibits Rac, Ras, and Tiam-induced growth transformation of NIH-3T3 fibroblasts.

Digeranyl bisphosphonate (DGBP) is a potent geranylgeranyl pyrophosphate (GGPP) synthase inhibitor that impedes the geranyl pyrophosphorylation of Rac1 and induces autophagy without causing apoptosis.

ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 value of 77.6 nM.

Atranorin shows significant antinociceptive and antiinflammatory activities, it has a relevant redox-active action, acting as a pro-oxidant or antioxidant agent depending on the radical, also, it will exert cytoprotective effects on cells under oxidative

ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).

Ketoconazole (R-41400), a CYP3A4 inhibitor, is an imidazole anti-fungal agent.

ML-210 (CID 49766530) is a glutathione peroxidase 4 (GPX4) inhibitor (EC50=30 nM) that is covalent and selective. ML-210 has antitumor activity and induces ferroptosis.

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3.

ARS-853 is an inhibitor of K-RASG12C(IC50 : 2.5 μM), a mutant form of K-RAS that accumulates in the active GTP-bound state in certain cancer cells

CCG-100602 inhibits RhoA C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells (IC50 :9.8 μM).

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).

CCG-222740 is an inhibitor of Rho MRTF pathway

CASIN (Pirl1-related Compound 2) is a specific inhibitor of GTPase Cdc42 (IC50: 2 uM).

FTI-277 hydrochloride (FTI 277 HCl) is an effective and specific farnesyltransferase (FTase) inhibitor (IC50: 500 pM); this selectivity is about 100-fold than the closely related GGTase I.

Salirasib (Farnesyl Thiosalicylic Acid)(Ki=2.6 μM), an effective competitive prenylated protein methyltransferase (PPMTase) inhibitor, inhibits Ras methylation with potential antineoplastic activity.

BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction (IC50: 21 nM).

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

Zt-12-037-01 is a ATP competitive STK19 inhibitor（IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N),respectively).

NSC 23766 trihydrochloride (Rac1 Inhibitor) is an inhibitor of Rac GTPase targeting Rac activation by GEFs (IC50: ~50 μM); no inhibitory for the closely related targets, RhoA or Cdc42.

pan activator of Ras-related GTPases

MBQ-167 is a dual inhibitor of Rac Cdc42 (IC50s: 103 nM for Rac 1 2 3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively).

CID-1067700 is one of the first identified competitive inhibitors of nucleotide binding by Ras-related GTPases（Rab7 with a Ki of 13 nM).

MCP110 is an inhibitor of the interaction of Ras with Raf-1 and can be used in studies about the treatment of human tumors.

Cysmethynil is an indole-based time-dependent inhibitor of Icmt with antitumour activity and inhibitory effects on RAS membrane-binding and EGF signalling.Cysmethynil induces cell cycle arrest in G1 phase and induces cellular autophagy, and can be used for the study of solid tumours.

ZCL278 is a selective Cdc42 GTPase inhibitor.

Rasarfin inhibits Ras and ARF6.

Kobe0065 is a novel and effective small-molecule compound that inhibits the Ras-Raf interaction by structure-based drug design (SBDD); it displays potent activity, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.

K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of the oncogenic K-Ras(G12C) protein.

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

MLS-573151 is a selective inhibitor of GTPase Cdc42(EC50 of 2 μM). It is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42.

XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.

RBC8 is a specific GTPases RalA/RalB inhibitor by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases RhoA and Ras.

1. Methylophiopogonanone B (MOPB) induces cell morphological change and Rho activation via melanocyte dendrite retraction and stress fiber formation.

(S)-(−)-Perillyl alcohol (Perillyl alcohol), a monoterpene found in lavender, inhibits Ras farnesylation, upregulates the mannose-6-phosphate receptor, induces apoptosis, and exhibits anti-cancer activity.

Kobe 2602 is an inhibitor of Ras that exhibits anticancer chemotherapeutic activities.

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50: 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. This compound also inhibits PC-3 cell migration (IC50: 4.2 μM), as determined by a scratch wound assay. CCG-203971(CCG203971) causes no cytotoxicity when evaluated by the WST-1 assay. It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.

Ras Inhibitory Peptide acetate is a peptide involved in the Ras-dependent signaling pathway that plays an important role in human cancers initiated by oncogenic receptors.

Oncrasin 1 is a potent inhibitor of anticancer that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations

Y16 is a G protein-coupled Rho GEFs inhibitor that synergizes with Rhosin G04 to inhibit LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling. Y16 is also a specific inhibitor of LARG with a Kd of 76 nM.

MLS000532223 is a selectiveRho family GTPases inhibitor(EC50 : 16 μM to 120 μM).

(R)-BI-2852 can be used as (R)-5-isoindolin-1-one is used as an inhibitor of the RAS family of proteins and as a compound for the treatment and prevention of tumours. (R)-BI-2852 has Antiproliferative and antitumour agent activity.

CCG-257081 (MRTF/SRF-IN-1) is an inhibitor of cardiac myosin-related transcription factor and serum response factor (MRTF/SRF) that acts by inhibiting the Rho/MRTF/SRF pathway.CCG-257081 has shown efficacy in preventing bleomycin-induced fibrosis in several mouse models. CCG-257081 can be used in cancer prevention and fibrosis research.

SCH-54292 is a GDP exchange inhibitor.

The compound inhibits Ras function and therefore inhibits the abnormal growth of cells.

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).