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]

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

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.

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

CCG-222740 is an inhibitor of Rho MRTF pathway

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.

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

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

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.

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

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).

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.

pan activator of Ras-related GTPases

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).

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.

BQU57 selectively inhibits Ral over Ras or Rho and suppresses xenograft tumor growth.

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).

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

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

ACBI3 is a selective pan-KRAS degrader with anticancer activity that degrades oncogenic KRAS. ACBI3 inhibits the growth of most cancer cell lines driven by KRAS mutations.

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

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.

DCC-3116 is an orally active, selective and potent ULK1 2 inhibitor with anticancer activity.DCC-3116 inhibits autophagy and can be used in cancer research.

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

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.

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.

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.

ZCL278 is a selective Cdc42 GTPase inhibitor.

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

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.

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

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

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

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

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

ADT-007 is an orally active and selective pan-RAS inhibitor with potent anticancer activity.ADT-007 blocks GTP activation of RAS and MAPK AKT signaling by binding to anucleotide RAS.ADT-007 is used in the study of gastrointestinal cancers.

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.

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

(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.