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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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