| 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. |
| M9356 | AMG-510 (Sotorasib) | AMG-510 (Sotorasib) is a potent KRAS G12C covalent inhibitor. |
| M9428 | MRTX849 (Adagrasib) | MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor. |
| M29422 | SOS1 activator 1 | SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS. |
| M29335 | APS6-45 | APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity. |
| M28909 | GGTI-286 hydrochloride | GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276. GGTI-286 hydrochloride selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s =2 and >30 μM, respectively). GGTI-286 hydrochloride also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM. |
| M28833 | SCH 51344 | SCH 51344 inhibits Ras induced malignant transformation and prevents anchorage-independent growth of oncogene transformed fibroblasts. |
| M28832 | GGTI-286 | GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276. GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM. |
| M27882 | Rhosin | Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability. |
| M27640 | KRA-533 | KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells. |
| M25594 | BI-2493 | |
| M21503 | MRTX849 acid | MRTX849 acid can be used to synthesize PROTAC LC-2. LC-2 is a potent, first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50, between 0.25 and 0.76 μM). |
| M21369 | BDP9066 | BDP9066 is a potent and selective MRCK inhibitor, reducing substrate phosphorylation. |
| M21220 | ASP2453 | ASP2453 is a potent, selective and covalent inhibitor of KRAS G12C. ASP2453 inhibits Son of Sevenless (SOS)-mediated interactions between KRAS G12C and Raf with an IC50 value of 40 nM. |
| M21080 | AZD4625 | AZD4625 is a highly potent, selective, covalent and metabotropic inhibitor of the mutant GTPase KRASG12C. AZD4625 has high oral bioavailability. It is being developed to study advanced solid malignancies. |
| M21078 | LY-3537982 | LY3537982 is a selective KRASG12C inhibitor. |
| M20725 | MCP110 | MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors. |
| M20708 | K-Ras-IN-1 | K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
| 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). |
| 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. |
| 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 . |
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