2. Signaling Pathways
  3. GPCR/G Protein
    MAPK/ERK Pathway
  4. Ras

Ras

Ras

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Ras is the name given to a family of related proteins which is ubiquitously expressed in all cell lineages and organs. All Ras protein family members belong to a class of protein called small GTPase, and are involved in transmitting signals within cells. Ras is the prototypical member of the Ras superfamily of proteins, which are all related in 3D structure and regulate diverse cell behaviours. When Ras is 'switched on' by incoming signals, it subsequently switches on other proteins, which ultimately turn on genes involved in cell growth, differentiation and survival. As a result, mutations in ras genes can lead to the production of permanently activated Ras proteins. This can cause unintended and overactive signalling inside the cell, even in the absence of incoming signals. Because these signals result in cell growth and division, overactive Ras signaling can ultimately lead to cancer. The 3 Ras genes in humans (HRAS,KRAS, and NRAS) are the most common oncogenes in human cancer; Ras inhibitors are being studied as a treatment for cancer, and other diseases with Ras overexpression.

Ras Isoform Specific Products:

Ras Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-153488
    ISIS 2503
    		Inhibitor
    ISIS-2503 is a 20-mer antisense oligonucleotide that inhibits Ha-Ras expression
    ISIS 2503
  • HY-156555
    pan-KRAS-IN-3
    pan-KRAS-IN-3 (Example 84) is a pan-KRAS inhibitor. pan-KRAS-IN-3 can be used for research of cancers. pan-KRAS-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    pan-KRAS-IN-3
  • HY-183355
    KRAS G12D-IN-37
    		Inhibitor
    KRAS G12D-IN-37 is a KRASG12D inhibitor. KRAS G12D-IN-37 shows antiproliferative activity against KRASG12D mutant tumor cells and minimal cytotoxicity toward normal cells. KRAS G12D-IN-37 binds stably to KRASG12D via hydrogen bond interactions with residues His 95, Arg 68, and Asp 12, and inhibits downstream ERK/AKT signaling pathways. KRAS G12D-IN-37 elevates ROS levels, induces apoptosis, disrupts mitochondrial membrane potential. KRAS G12D-IN-37 downregulates the level of anti-apoptotic protein Bcl-2, and upregulates the levels of pro-apoptotic proteins Bax and caspase 3. KRAS G12D-IN-37 can be used for the research of cancer, such as gastric adenocarcinoma and colorectal cancer.
    KRAS G12D-IN-37
  • HY-182994
    pan-KRAS-IN-20
    		Inhibitor
    pan-KRAS-IN-20 is a pan-KRAS inhibitor. pan-KRAS-IN-20 can be used for the researches of cancer, tumors, inflammatory diseases, autoimmune diseases or immune-mediated diseases.
    pan-KRAS-IN-20
  • HY-160445
    KRAS G12D inhibitor 19
    		Inhibitor
    KRAS G12D inhibitor 19 (Compound 7) is a KRAS G12D inhibitor. KRAS G12D inhibitor 19 can be used for the research of cancer.
    KRAS G12D inhibitor 19
  • HY-P10594
    Myr-Arf1(2–17)
    Myr-Arf1(2–17) is a sarcosinated peptide that mimics the localization and function of Arf1 protein on the cell membrane. Myr-Arf1(2–17) can be used to study the desensitization mechanism of luteinizing hormone/chorionic gonadotropin receptor (LH/CGR).
    Myr-Arf1(2–17)
  • HY-180885S
    KRAS G12D-IN-35
    		Inhibitor
    KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer.
    KRAS G12D-IN-35
  • HY-117807
    A-176120
    		Inhibitor
    A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion.
    A-176120
  • HY-179534
    G13Ci-22
    		Inhibitor
    G13Ci-22 is a MRTX1133 (HY-134813) based KRAS G13C inhibitor. G13Ci-22 can be used for non-small cell lung cancer (NSCLC) research.
    G13Ci-22
  • HY-180607
    KRAS-IN-50
    		Inhibitor
    KRAS-IN-50 (Compound 136a) is a KRAS inhibitor. KRAS-IN-50 has an anti-proliferative effect on KRAS mutant cells. KRAS-IN-50 has anti-cancer activity against colon cancer.
    KRAS-IN-50
  • HY-172917
    Rho GTPase inhibitor 1
    		Inhibitor
    Rho GTPase inhibitor 1 (compound 7) is a potent Rho GTPase inhibitor. Rho GTPase inhibitor 1 exhibits high affinity on Cdc42, Rac1 and RhoA with KDs of 151, 352, and 232 μM, respectively. Rho GTPase inhibitor 1 reduces cell migration on glioma cell line.
    Rho GTPase inhibitor 1
  • HY-19539
    NSC-658497
    		Inhibitor
    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.
    NSC-658497
  • HY-162366
    KRAS G12D inhibitor 20
    		Inhibitor
    KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor. KRAS G12D inhibitor 20 has antitumor activity.
    KRAS G12D inhibitor 20
  • HY-183625
    PCA-IN-1
    		Inhibitor
    PCA-IN-1 is a polyisoprenylated cysteinyl amide (PCA) inhibitor that acts on multiple KRAS mutant subtypes. PCA-IN-1 dissociates KRAS4B from its transport chaperones, prevents its localization to the plasma membrane, and blocks downstream oncogenic signaling pathways. PCA-IN-1 inhibits colony formation of KRAS-mutant lung cancer cells, induces sustained long-term growth inhibition, and suppresses cell migration. PCA-IN-1 is applicable to the research of KRAS-mutant lung cancer.
    PCA-IN-1
  • HY-181491
    Tubulin-IN-64
    		Inhibitor
    Tubulin-IN-64 is a sulfonated styrylquinazoline derivative with high selectivity antitumor activity. Tubulin-IN-64 targets tubulin, inhibits the EGFR/Akt/mTOR and EGFR/Ras signaling pathways, induces cell cycle arrest, apoptosis and autophagy. Tubulin-IN-64 exhibits significant antitumor efficacy in the zebrafish GBM xenograft model. Tubulin-IN-64 can be used for the research on glioblastoma and leukemia.
    Tubulin-IN-64
  • HY-163515
    Anticancer agent 207
    		Inhibitor
    Anticancer agent 207 (compound 10b) is a potent anticancer agent. Anticancer agent 207 bounds to the NRAS rG4 with a KD value of 2.31 µM. Anticancer agent 207 shows cytotoxicity and decreases the expression of NRAS protein. Anticancer agent 207 shows antitumor activity.
    Anticancer agent 207
  • HY-175244
    SOS1-IN-20
    		Inhibitor
    SOS1-IN-20 (Compound 12f) is an orally active SOS1 inhibitor with an IC50 of 5.11 nM against KRASG12C::SOS1. By disrupting the interaction between KRAS and SOS1, SOS1-IN-20 inhibits KRAS activation and downstream signal transduction. SOS1-IN-20 has an IC50 of 253 nM for p-ERK in PC-9 cells and 16.71 μM for hERG channel . SOS1-IN-20 can inhibit the proliferation of tumor cells and has antitumor activity.
    SOS1-IN-20
  • HY-179300A
    KRAS-IN-48
    		Inhibitor
    KRAS-IN-48 (Compound 1-01) is a KRAS mutant inhibitor, with Kd values of 2.58 nM and 5.49 μM for KRAS-G12D and KRAS-G12V, respectively. KRAS-IN-48 can be used in the research of cancer.
    KRAS-IN-48
  • HY-116428
    L-744832
    		Modulator
    L-744832 is a farnesyl transferase inhibitor. L-744832 effectively inhibits the farnesylation of H-Ras and N-Ras, but has little effect on K-Ras treatment. L-744832 not only directly targets the oncogenic pathway by inhibiting Ras farnesylation, but also enhances radiosensitivity by restoring TGF-β signaling through epigenetic reprogramming. L-744832 can induce cell cycle arrest and apoptosis. L-744832 can be used in combination therapy studies for Ras-driven tumors such as pancreatic cancer.
    L-744832
  • HY-151968
    KRAS G12C inhibitor 57
    		Inhibitor
    KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis.
    KRAS G12C inhibitor 57
Cat. No. Product Name / Synonyms Application Reactivity
Ras Isoform Comparison

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