| 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. |
| M8999 | CCG-1423 | CCG-1423 is a novel specific inhibitor of RhoA transcriptional signaling. |
| M30551 | Diazepinomicin | Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models. |
| M30401 | 8-CPT-2Me-cAMP sodium | 8-CPT-2Me-cAMP sodium is a selective activator of exchange proteins activated by cAMP (Epac), the cAMP sensitive guanine nucleotide exchange factors (GEFs) for the small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50> 10 μM). 8-CPT-2Me-cAMP sodium stimulates Epac-mediated Ca2+ release in pancreatic β-cells in vitro. |
| M30161 | UC-857993 | UC-857993 is a selective SOS1-Ras inhibitor (Kd=14.7 μM, His6-SOS1cat), suppressing catalytic activity. UC-857993 also inhibits ERK and Ras activation, suppresses the growth of mouse embryonic fibroblasts (MEFs). |
| M29990 | RBC10 | RBC10 is an anti-cancer agent. RBC10 inhibits the binding of Ral to its effector RALBP1. RBC10 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines. |
| M29868 | ZINC69391 | ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects. |
| M29863 | ESI-08 | ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation. |
| M29862 | KRAS inhibitor-9 | KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells. |
| M29777 | SOS1-IN-5 | SOS1-IN-5 is a potent inhibitor of SOS1. SOS1-IN-5 is a pyrimidobicyclic derivative. SOS1-IN-5 blocks the activation of KRAS by interfering with RAS-SOS1 interaction, and achieves the purpose of broad-spectrum inhibition of KRAS activity. SOS1-IN-5 has the potential for the research of cancer diseases. |
| M29770 | Spiclomazine hydrochloride | Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis. |
| M29747 | Fulzerasib | Fulzerasib is a potent KRAS inhibitor that downregulates KRAS protein activation by covalently and irreversibly modifying cysteine residues of the KRAS G12C protein mutant and inhibiting GTP/GDP exchange mediated by the protein. |
| M29638 | ARS-1323-alkyne | ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRASG12C nucleotide state in living cells. |
| 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). |
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