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-N2438
    Methylophiopogonanone B
    		Activator 99.84%
    Methylophiopogonanone B, homoisoflavonoid, is extracted from the root of Ophiopogon japonicas, shows high antioxidant ability. Methylophiopogonanone B increases GTP-Rho and acts via the Rho signaling pathway, inducing cell morphological change via actin cytoskeletal reorganization, including dendrite retraction and stress fiber formation.
    Methylophiopogonanone B
  • HY-128522
    ARS-1323-alkyne
    		Inhibitor 99.59%
    ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy, providing tool support for the development of combination treatment strategies.
    ARS-1323-alkyne
  • HY-12646A
    Rhosin
    		Inhibitor
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
    Rhosin
  • HY-144661
    KRAS G12D inhibitor 14
    		Inhibitor 99.39%
    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.
    KRAS G12D inhibitor 14
  • HY-156228
    RGB-1
    		Inhibitor 98.07%
    RGB-1 is a polycyclic aromatic hydrocarbon molecule and a stabilizer of RNA G-quadruplexes. RGB-1 can promote the inhibition of RNA translation and reduce the expression of NRAS proto-oncogene in breast cancer cells.
    RGB-1
  • HY-126133
    AM-001
    		Inhibitor 99.95%
    AM-001 is a non-competitive inhibitor of Epac1 that blocks the activation of Rap1, a downstream effector of Epac1, in cultured cells. AM-001 can be used in heart disease-related research.
    AM-001
  • HY-149464
    ARN22089
    		Inhibitor 98.73%
    ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model.
    ARN22089
  • HY-151881
    SOS1-IN-15
    		Inhibitor 99.51%
    SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer.
    SOS1-IN-15
  • HY-153606
    SOS1 agonist-1
    		Activator
    SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role[1].
    SOS1 agonist-1
  • HY-158304
    Rac1-IN-4
    		Inhibitor 98.61%
    Rac1-IN-4 (Cas: 2924486-45-1) is a Rac1 inhibitor.
    Rac1-IN-4
  • HY-123673
    MCP110
    		Inhibitor 99.82%
    MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors.
    MCP110
  • HY-119264A
    PRLX-93936 dihydrochloride
    		Inhibitor 99.83%
    PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma.
    PRLX-93936 dihydrochloride
  • HY-U00416
    ARS-1323
    		Inhibitor 99.67%
    ARS-1323 (Example 30, No. 227) is the racemate of ARS-1620. ARS-1323 is a novel inhibitor of mutant K-ras G12C.
    ARS-1323
  • HY-141477
    RM-018
    		Inhibitor 98.03%
    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.
    RM-018
  • HY-138295
    KRAS inhibitor-10
    		Inhibitor 99.92%
    KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
    KRAS inhibitor-10
  • HY-125987
    RBC6
    		Inhibitor 98.88%
    RBC6 is an inhibitor of GTPases RalA. RBC6 inhibits binding of Ral to its effector RALBP1. RBC6 also inhibits Ral-mediated cell spreading of murine embryonic fibroblasts, as well as anchorage-independent growth of human cancer celllines.
    RBC6
  • HY-132581
    Tadnersen
    		Inhibitor
    Tadnersen (BIIB078), an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.
    Tadnersen
  • HY-P2265A
    SAH-SOS1A TFA
    		Inhibitor
    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). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.
    SAH-SOS1A TFA
  • HY-126247B
    (R)-BI-2852
    		Control
    (R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
    (R)-BI-2852
  • HY-111671
    VUBI1
    		Activator 98.01%
    VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer.
    VUBI1
Cat. No. Product Name / Synonyms Application Reactivity
Ras Isoform Comparison

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