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Ras inhibitors and related small GTPase modulators act on KRAS and on the Rac, Rho and Cdc42 proteins. Small GTPases of the Ras superfamily work as molecular switches. They cycle between an active form bound to guanosine triphosphate (GTP) and an inactive form bound to guanosine diphosphate (GDP). Oncogenic KRAS mutations such as G12C keep the protein in its signaling state. ARS-853 and KRas G12C inhibitor 4 target the mutant cysteine of KRAS G12C, while Kobe2602 interferes with binding of Ras to Raf. Salirasib, a farnesylcysteine mimetic, disrupts the membrane association of Ras. Rho-family tools include NSC 23766 and EHT 1864, which inhibit Rac, and CASIN, which targets Cdc42.
EHT 1864 is an antiproliferative chemical shown to inhibit Rac family GTPases.
Synonyms: Zometa; Zomera; Aclasta and Reclast
Zoledronic acid is a bisphosphonate which used to multiple myeloma and prostate cancer treament.
Synonyms: S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
Salirasib is an inhibitor of prenylated protein methyltransferase (PPMTase) with Ki value of 2.6 uM.
ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
NSC 23766 is a selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC50 ~ 50 μM) without affecting Cdc42 or RhoA activation.
Kobe2602 is an analog of Kobe0065. Exhibits potent activity to competitively inhibit the binding of H-Ras??GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.
EHop-016 is a potent and specific inhibitor of Rac1 and Rac3 GTPase activity that inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
Synonyms: MKI833
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor.
Kobe0065 inhibits anchorage-dependent and -independent growth, blocks MEK/ERK activity and induces apoptosis in H-rasG12V transformed NIH3T3 cells.
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
Synonyms: SOS1-IN-1
SOS1-IN-1 is a SOS1 inhibitor.
ZCL-278 is a selective inhibitor of Cdc42. Targets the binding site of the Cdc42 guanine nucleotide exchange factor, intersectin (ITSN). Inhibits Cdc42-mediated cellular effects, including microspike formation in 3T3 fibroblasts and neuronal branching in primary neonatal cortical neurons. Also suppresses cell motility and migration in PC3 cells, without cytotoxic effects.
Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
Synonyms: NSC 23766
NSC 23766 is a cell-permeable, reversible inhibitor of Rac1 activation by the Rac-specific GEFs TrioN and Tiam 1 (IC50 = 50 uM).
K-Ras(G12C) inhibitor 6 is an irreversible inhibitor of oncogenic K-Ras(G12C), subverting the native nucleotide preference to favour GDP over GTP.
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
CCG-1423 is a specific inhibitor of Rho pathway-mediated signaling and activation of serum response factor (SRF) transcription.
BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
Synonyms: CID-7345532
ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM).
