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-115489
    GGTI-286
    Inhibitor
    GGTI-286, a potent and cell-permeable GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276 (HY-15873A). GGTI-286 selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s=2 and >30 μM, respectively). GGTI-286 also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM.
    GGTI-286
  • HY-U00417
    ARS-1630
    Inhibitor 98.10%
    ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
    ARS-1630
  • HY-157031S
    KRASG12D-IN-2
    Inhibitor 98.11%
    KRASG12D-IN-2 (compound 28) is a KRASG12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition.
    KRASG12D-IN-2
  • HY-145928B
    Divarasib adipate
    Inhibitor
    Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
    Divarasib adipate
  • HY-139894
    KRAS G12D inhibitor 5
    Inhibitor
    KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential research of pancreatic cancer.
    KRAS G12D inhibitor 5
  • HY-142460
    KRAS G12C inhibitor 28
    Inhibitor 99.94%
    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).
    KRAS G12C inhibitor 28
  • HY-163939
    RGT-018
    Inhibitor 99.77%
    RGT-018 is a potent and orally active SOS1 inhibitor with anti-tumor effects. RGT-018 exerts anti-cancer cell proliferation activity by inhibiting KRAS activation.
    RGT-018
  • HY-119230
    Kobe2601
    Inhibitor 99.66%
    Kobe2601 is a Kobe0065 (HY-15716) analogue. Kobe2601 can be used to probe the Kobe family of compounds' mechanism of action.
    Kobe2601
  • HY-114569
    6-CEPN
    Inhibitor 99.17%
    6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase).
    6-CEPN
  • HY-145962
    MRTX-EX185
    Inhibitor
    MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC50 of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC50s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) .
    MRTX-EX185
  • HY-18606
    K-Ras G12C-IN-3
    Inhibitor 99.94%
    K-Ras G12C-IN-3 (Compound VI-5) is an irreversible small molecule inhibitor of mutant K-Ras G12C. K-Ras G12C-IN-3 can be used in the research of cancers.
    K-Ras G12C-IN-3
  • HY-124944
    APS6-45
    Inhibitor 99.58%
    APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
    APS6-45
  • HY-138294
    RAS/RAS-RAF-IN-1
    Inhibitor 99.81%
    RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
    RAS/RAS-RAF-IN-1
  • HY-134811
    KRAS G12D inhibitor 1
    Inhibitor
    KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    KRAS G12D inhibitor 1
  • HY-129189
    RAS GTPase inhibitor 1
    Inhibitor 99.70%
    RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
    RAS GTPase inhibitor 1
  • HY-P10051A
    Cyclorasin 9A5 TFA
    Inhibitor 99.57%
    Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM.
    Cyclorasin 9A5 TFA
  • HY-171255
    KRAS G12D inhibitor 26
    Inhibitor
    KRAS G12D inhibitor 26 is a modulator of Kras, targeting Kras(G12D) with an IC50 ≤ 100 nM.
    KRAS G12D inhibitor 26
  • HY-W549903
    p67phox-IN-1
    Inhibitor 99.80%
    p67phox-IN-1 (Formula IIIa Compound) is an inhibitor targeting the interaction between Rac GTPase and p67phox protein.
    p67phox-IN-1
  • HY-152095
    PPI-GIT1/β-Pix PPI-IN-1
    Inhibitor 99.01%
    PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a KD value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer.
    PPI-GIT1/β-Pix PPI-IN-1
  • HY-164350
    KRAS inhibitor-27
    Inhibitor
    KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway.
    KRAS inhibitor-27
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