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

Ras

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-148278
    BI-0474
    Inhibitor 99.83%
    BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.
    BI-0474
  • HY-112491
    KRas G12C inhibitor 1
    Inhibitor
    KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
    KRas G12C inhibitor 1
  • HY-164493
    KRASG12C IN-13
    Inhibitor 99.01%
    KRASG12C IN-13 (LY3499446) is a potent KRAS G12C inhibitor. KRASG12C IN-13 is promising for research of advanced solid tumors including non-small cell lung cancer and colorectal cancer.
    KRASG12C IN-13
  • HY-153413
    Kras4B G12D-IN-1
    Inhibitor 98.01%
    Kras4B G12D-IN-1 is a Kras4B G12D inhibitor with anticancer effects. Kras4B G12D-IN-1 decreases Kras protein expression in mouse embryonic fibroblasts (MEF) expressing Kras4B G12D (WO2016179558A1, Comp 994566).
    Kras4B G12D-IN-1
  • HY-143212
    18:0-22:6 DG
    99%
    18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (Ki = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease.
    18:0-22:6 DG
  • HY-136197
    StRIP16
    Inhibitor
    StRIP16, bioavailable StRIP3 analogue, is a double-stapled peptide which can bind to Rab8a GTPase, with a Kd of 12.7 μM.
    StRIP16
  • HY-12408A
    6H05 TFA
    Inhibitor 99.02%
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
    6H05 TFA
  • HY-B0105S1
    Ketoconazole-d4
    Inhibitor 99.63%
    Ketoconazole-d4 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole-d<sub>4</sub>
  • HY-176489
    PROTAC pan-KRAS degrader-1
    Inhibitor
    PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc. Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);
    PROTAC pan-KRAS degrader-1
  • HY-153662
    TH-Z816
    Inhibitor 98.92%
    TH-Z816 is a reversible inhibitor againstKRAS(G12D)mutation with an IC50 value of 14 μM, which can be used in cancer research.
    TH-Z816
  • HY-158310
    SOS1/EGFR-IN-1
    Inhibitor 99.54%
    SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM).
    SOS1/EGFR-IN-1
  • HY-B0105S
    Ketoconazole-d8
    Inhibitor 99.79%
    Ketoconazole-d8 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
    Ketoconazole-d<sub>8</sub>
  • HY-139402
    MRTX849 acid
    Inhibitor 99.84%
    MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM).
    MRTX849 acid
  • HY-181555
    IACS-56676
    Inhibitor
    IACS-56676 is a selective NRASG12D inhibitor with a target IC50 of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity against wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used in the research of melanoma, hematologic malignancies and thyroid cancer.
    IACS-56676
  • HY-154959A
    (9R,12aR)-AZD4747
    Control 98.90%
    (9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRASG12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer.
    (9R,12aR)-AZD4747
  • HY-P4869
    Biotin-KRpep-2d acetate
    Inhibitor 99.13%
    Biotin-KRpep-2d acetate is a biotin-labeled KRpep-2d (HY-P3277).
    Biotin-KRpep-2d acetate
  • HY-158107A
    (4R)-BBO-8520
    Inhibitor
    (4R)-BBO-8520 (Compound 314), an isomer of BBO-8520 (HY-158107), is a selective KRAS G12C inhibitor. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRASG12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state. (4R)-BBO-8520 can be used for the research of cancer.
    (4R)-BBO-8520
  • HY-P11294
    KLVVVGADGVGKSALTI
    98.26%
    KLVVVGADGVGKSALTI is a KRAS G12D targeting peptide that can be used in tumor research.
    KLVVVGADGVGKSALTI
  • HY-153078
    MRTF/SRF-IN-1
    Inhibitor 99.68%
    MRTF/SRF-IN-1 (example 41) is an inhibitor of both myocardin-related transcription factor and serum response factor (MRTF/SRF). MRTF/SRF-IN-1 can be used for research for preventing cancer and fibrosis.
    MRTF/SRF-IN-1
  • HY-117935
    GGTI-286 hydrochloride
    Inhibitor
    GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). 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.
    GGTI-286 hydrochloride
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