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. |
M41922 | MRTF/SRF-IN-1 | MRTF/SRF-IN-1 is an inhibitor of both myocardin-related transcription factor and serum response factor (MRTF/SRF). |
M41921 | Spiclomazine | Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. |
M41920 | KRAS G12D modulator-1 | KRAS G12D modulator-1 is a potent KRAS G12D modulator with IC50 values of 1-10 μM for NEA-G12D, PPI-G12D, and p ERK-AGS, respectively. |
M41919 | pan-KRAS-IN-2 | pan-KRAS-IN-2 is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and >10 μM for KRAS G13D, respectively. |
M40563 | AZD4747 | AZD4747 is an orally active, potent, and selective KRAS G12C inhibitor that crosses the blood-brain barrier and can be used in studies related to solid tumors with KRAS G12C mutations. |
M40562 | LUNA18 | LUNA18 is an orally active RAS cyclic peptide inhibitor that selectively targets, binds and inhibits Ras, thereby inhibiting Ras-dependent signaling and ultimately suppressing the proliferation of Ras-overexpressing tumor cells. It can be used in studies related to solid tumors. |
M38969 | (-)-Rasfonin | (-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line). |
M31040 | GGTI-286 TFA | GGTI-286 TFA, 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 TFA selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 TFA also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM. |
M30865 | NSC-658497 | NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation. |
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. |
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