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Ras Ras

Inhibitors

Cat.No.  Name Information
M2562 ZCL278 ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.
M6282 NSC 23766 NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
M11445 MRTX0902 MRTX0902 is an effective SOS1 inhibitor with an IC50 of 46 nM.
M11442 GDC-6036 Gdc-6036 (compound 17A) is an oral covalently mutated KRAS G12C inhibitor with IC50<0.01 μM against K-Ras G12C. The EC50 of GDC-6036 in K-Ras G12C-alkylated HCC1171 cells was 2 nM.
M11427 RM-018 RM-018 is an inhibitor of the active state of KRASG12C. Rm-018 retains the ability to bind and inhibit KRASG12C/Y96D. Rm-018 combines with GTP-bound to activate the [" RAS(ON) "] state of KRASG12C.
M11263 HJC0197 HJC0197 is a potent antagonist of Epac1 (the exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2). HJC0197 selectively blocked camp-induced Epac activation. HJC0197 inhibited epAC1-mediated RAP1-GDP exchange activity in the presence of isoconcentration of cAMP.
M10600 SAH-SOS1A TFA SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM) and directly and independently blocks nucleotide association.
M10593 MRTX1133 MRTX1133 is a first-in-class, potent and highly selective KRAS G12D inhibitor. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.
M10268 CID-1067700 (ML282) CID-1067700 (ML282) is a competitive inhibitors of nucleotide binding by Ras-related GTPases with a Ki of 13 nM for Rab7.
M9817 MLS000532223 MLS000532223 is a selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM.
M9801 BI-3406 BI-3406 is a highly potent and selective SOS1::KRAS inhibitor (IC50=6 nM), which selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation.
M9586 ZT-12-037-01 ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively.
M9578 BI-2852 BI-2852 is a potent KRAS inhibitor that binds with nanomolar affinity to a pocket.
M9428 MRTX849 (Adagrasib) MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor.
M9359 BAY-293 BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1), blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM.
M9357 AMG-510 racemate AMG-510 racemate is a racemic of AMG-510, which is a potent KRAS G12C covalent inhibitor.
M9356 AMG-510 (Sotorasib) AMG-510 (Sotorasib) is a potent KRAS G12C covalent inhibitor.
M9235 ARS-853 ARS-853 is a selective, covalent KRASG12C inhibitor with an IC50 of 2.5 μM.
M9047 ARS-1630 ARS-1630 is a novel mutant K-ras G12C inhibitor.
M9046 ARS-1323 ARS-1323 is a novel inhibitor of mutant K-ras G12C.
M9045 ARS-1620 ARS-1620 is an atropisomeric selective KRAS-G12C inhibitor with desirable pharmacokinetics.
M9000 ML-098 ML-098 is an activator of the GTP-binding protein Rab7 with EC50 value of 77.6 nM.



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