The hydrolysis of guanosine triphosphate (GTP) is a key process in numerous vital processes. Intracellular signal transduction, protein synthesis, vesicular and nucleocytoplasmic transport, protein targeting, growth control and differentiation, are all, among other processes, controlled enzymatically by the conversion of GTP into GDP and inorganic phosphate. GTPases are the molecular switches that catalyze this reaction. They cycle between two conformational states: one bound to GTP ('active' state), the other bound to GDP ('inactive' state), and they hydrolyze GTP to GDPand inorganic phosphate. In the 'on' (GTP) state, GTPases recognize target proteins and generate a response until GTP hydrolysis returns the switch to the 'off' state[1]. GTPases can be classified into six families of heterotrimeric G-protein, small monomeric, protein-synthesizing, signal-recognition-particle, dynamin, and tubulin GTPases (EC – EC respectively). GTP-hydrolysis by GTPases is intrinsically very slow but can be accelerated by orders of magnitude upon interaction with GTPase-activating proteins (GAPs)[2]. In order to bring the GTPase back in the GTP bound ‘on’ state, so called guanine nucleotide exchange factors (GEFs), which cause the GDP to dissociate from the GTPase, leading to its association with  new GTP.

[1] S. Etienne-Manneville, A. Hall. Rho GTPases in cell biology. Nature 2002, 420, 629-635.
[2] K. Scheffzek, M.R. Ahmadian, Wittinghofer. GTPase-activating proteins: helping hands to complement an active site. Trends Biochem Sci. 1998, 23, 257-262.

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Axon ID Name Description From price
3575 AMG510 Highly potent, selective, and orally bioavailable KRAS-G12C inhibitor €90.00
3084 ARS-1620 Potent, selective, and orally bioavailable covalent KRAS-G12C inhibitor €145.00
3053 BAY-293 Potent, selective and cell-active inhibitor of KRAS-SOS1 interaction €140.00
3471 BI-3406 Inhibitor of KRAS/Son of Sevenless 1 (SOS1) interaction Inquire
2397 BQU 57 Inhibitor of the RAS-like small GTPases RalA and RalB €125.00
3987 CASIN Selective Cdc42 inhibitor €140.00
2753 CCG 232601 Rho/MRTF/SRF transcriptional pathway inhibitor €160.00
1931 CCG 50014 Inhibitor of RGS proteins (RGS4 selective) €90.00
3092 CCG-203971 Rho/MRTF/SRF transcriptional pathway inhibitor €60.00
3069 CCG-222740 Potent and selective Rho/MRTF/SRF transcriptional pathway inhibitor €145.00
2184 CID 1067700 First inhibitor of Rab7 GTPase €125.00
3879 Dynasore Noncompetitive cell-permeable dynamin inhibitor €80.00
2351 EHop 016 Rac GTPase inhibitor specific for Rac1 and Rac3 €85.00
2829 Fendiline hydrochloride KRAS inhibitor; Ca2+ channel blocker (L-type voltage gated) €50.00
3768 GDC-6036 Inhibitor of KRAS G12C Inquire
4197 Golgicide A Potent, highly specific and reversible inhibitor of GBF1  Recently added €95.00
4160 IGGi-11me Membrane permeable prodrug of IGGi-11; GIV-Gαi inhibitor  Recently added €140.00
2302 Kobe 0065 HRAS inhibitor €70.00
2777 MBQ-167 Dual Rac and Cdc42 inhibitor €105.00
2017 ML 210 Chemical probe that selectively kills cells induced to express mutant RAS €115.00
3761 MRTX1133 First-in-class, noncovalent, selective & reversible inhibitor of KRASG12D mutant €220.00
3733 MRTX1257 Irreversible covalent inhibitor of KRAS G12C Inquire
4036 MRTX849 Potent, mutation-selective, and irreversible covalent inhibitor of KRAS-G12C Inquire
3622 NAV-2729 Dual Arf1/Arf6 inhibitor; FATP2 inhibitor €80.00
1578 NSC 23766 Rac1 inhibitor €110.00
2393 NSC 756093 Potent in vitro inhibitor of GBP1:PIM1 interaction €125.00
2396 RBC 8 Inhibitor of the RAS-like small GTPases RalA and RalB €105.00
2138 ZCL 278 Cdc42 GTPase inhibitor, targeting Cdc42–ITSN interaction €105.00
3790 ZINC69391 Specific Rac1 inhibitor €110.00

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