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Ras

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Cat. No. Product Name Field of Application Chemical Structure
DC45326 CCG-100602 Featured 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.
DC45688 Atrovastatin-PEG3-FITC Featured Atrovastatin-PEG3-FITC (compound S31) is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay.
DC45689 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), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.
DC46410 StRIP16 StRIP16, bioavailable StRIP3 analogue, is a double-stapled peptide which can bind to Rab8a GTPase, with a Kd of 12.7 μM.
DC46924 MRTX849 acid MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2. LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM).
DC47181 MRTX1133 formic MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. 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.
DC47210 JDQ-443 Featured JDQ443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1).
DC47351 ASP2453 Featured ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
DC47352 KRAS mutant protein inhibitor 1 KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer.
DC47353 KRAS G12C inhibitor 18 KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities.
DC47354 RTIL 13 RTIL 13 is a potent inhibitor of dynamin GTPase, with an IC50 of 2.3 µM for dynamin I GTPase. RTIL 13 also targets pleckstrin homology lipid binding domain. RTIL 13 can inhibit receptor-mediated and synaptic vesicle endocytosis, with IC50s of 9.3 μM and 7.1 μM, respectively.
DC47355 RM-018 RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C.
DC58063 HG106 Featured HG106 is a potent SLC7A11 inhibitor and enhances ROS generation, ER stress, and ultimately growth arrest specifically in KRAS-mutant lung adenocarcinoma (LUAD).
DC48354 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.
DC48826 SOS1-IN-3 SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1).
DC48952 SOS1-IN-4 SOS1-IN-4 is a potent SOS1 inhibitor with an IC50 of 56 nM for KRAS-C12C/SOS1 interaction (WO2021228028 A1, example 65).
DC49008 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 (extracted from patent WO2021203768A1, compound 4).
DC49060 KRAS G12C inhibitor 24 KRAS G12C inhibitor 24 is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 24 inhibits KRAS G12C/SOS1 interaction with an IC50 of＜50 nM (CN113563323A, compound 1).
DC49086 KRAS G12C inhibitor 27 KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737).
DC49087 KRAS G12C inhibitor 26 KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737).
DC49132 KRAS G12C inhibitor 23 KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1).
DC49137 KRAS G12C inhibitor 25 KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3.
DC49138 KRAS G12C inhibitor 22 KRAS G12C inhibitor 22 is a KRAS G12C inhibitor extracted from patent WO2021219072A1, example 120.
DC49148 KRAS G12C inhibitor 28 KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1).
DC49149 KRAS G12C inhibitor 20 KRAS G12C inhibitor 20 is a KRAS G12C inhibitor extracted from patent CN112694475A, example 1.
DC49155 KRAS G12C inhibitor 21 KRAS G12C inhibitor 21 is a KRAS G12C inhibitor extracted from patent WO2021219090A1, example 7.
DC50080 KRAS G12C inhibitor 29 KRAS G12C inhibitor 29 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 3. KRAS G12C inhibitor 29 can be used for the research of cancer.
DC50081 KRAS inhibitor-11 KRAS inhibitor-11 (compound 12) is a KRAS inhibitor.
DC50082 K20 K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity.
DC50083 KRAS G12D inhibitor 14 KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.

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