Ras

RMC-6236 is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

Glecirasib (JAB-21822) is an orally active KRAS G12C inhibitor that selectively binds to and inhibits the activity of KRAS G12C mutants, thereby inhibiting KRAS G12C-dependent signaling. In animal models, KRAS G12C inhibitor 36 showed a favorable safety profile and potential to inhibit tumor growth.

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

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

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.

CCG-222740 is an inhibitor of Rho MRTF pathway

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

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]

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

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

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

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.

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).

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.

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.

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

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.

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

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

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.

pan activator of Ras-related GTPases

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.

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.

GGTI298 Trifluoroacetate (GGTI 298 TFA salt) is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.

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

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.

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

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

Nexinhib20 is an inhibitor of exosome synthesis and transport with anti-inflammatory activity, inhibits RAB27A and neutral sphingomyelinase 2 (nSMase2) nsMase2, inhibits IL-8-induced β(2) integrin-dependent adhesion of human neutrophils in the subfluidic phase, and inhibits neutrophil adhesion and β(2) integrin activation through antagonism of the rac-1-guanosine 5'-triphosphate interaction. beta(2) integrin activation.

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.

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

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

APS6-45 inhibits RAS MAPK signaling and exhibits anti-tumor activity.

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

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).

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-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.

(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.

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

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

Rasarfin inhibits Ras and ARF6.

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

ZCL278 is a selective Cdc42 GTPase inhibitor.

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.

HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 is an effective exchange protein. Which straightly activated by cAMP (Epac) antagonist (IC50=5.9 μM for Epac2).

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.