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Ras Ras

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.
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.
M20741 Antineoplaston A10 Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
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.
M20013 MRTX0902 MRTX0902 is an oral brain penetrating SOS1:KRAS protein-protein interaction inhibitor.
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.
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.



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