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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. |
| M14058 | Y16 | Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. |
| M14057 | RAS inhibitor Abd-7 | RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. |
| M14056 | PHT-7.3 | PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). |
| M14055 | Pan-RAS-IN-1 | Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors. |
| M14054 | MRTX-1257 | MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. |
| M14053 | Deltarasin hydrochloride | Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with Kd of 38 nM for binding to purified PDEδ. |
| M14052 | CCG-100602 | CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF. |
| M14051 | 1A-116 | 1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes . |
| M13363 | CCG-222740 | CCG-222740 is an inhibitor of the Rho/MRTF pathway. CCG-222740 is also an effective α -smooth muscle actin protein expression inhibitor. CCG-222740 effectively reduces skin fibrosis and prevents melanoma metastasis. |
| 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. |
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