2. シグナル伝達
  3. GPCR/G Protein
    MAPK/ERK Pathway
  4. Ras
  5. Ras Isoform

Ras

Ras proteins are small GTPases that function as molecular switches, cycling between inactive GDP-bound and active GTP-bound states to regulate intracellular signaling networks controlling cell proliferation, differentiation, migration, survival, and apoptosis[1][2]. Mechanistically, activated Ras transduces signals from cell-surface receptors to major downstream pathways, including the RAF-MEK-ERK cascade, thereby coordinating growth-related transcriptional programs and cellular responses[1][2]. The human RAS family comprises the highly homologous isoforms KRAS, NRAS, and HRAS, which share common effectors yet display distinct signaling outputs, partly due to sequence divergence within regions involved in allosteric communication and membrane interactions[3][4]. Compared with related isoforms, KRAS exhibits unique membrane-targeting characteristics associated with its hypervariable region and is the predominant RAS isoform mutated in human malignancies, whereas NRAS and HRAS show different mutation frequencies and biological distributions across cancer types[4][5][6]. RAS genes are among the most frequently mutated oncogenes in human cancer, and gain-of-function mutations commonly affecting codons 12, 13, and 61 promote persistent Ras activation that drives tumorigenesis in diverse experimental and clinical settings[5][7]. For experimental applications, isoform-selective signaling mechanisms and Ras conformational regulation provide important frameworks for the development and evaluation of Ras-targeted inhibitors and mechanistic cancer models[3][8].

Ras 関連製品 (421):

製品番号 製品名 製品効果 純度
  • HY-132581
    Tadnersen Inhibitor 99.30%
    Tadnersen (BIIB078), an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.
  • HY-156228
    RGB-1 Inhibitor
    RGB-1 selectively binds to and stabilizes RNA G-quadruplex structures, and reduces the expression of the NRAS proto-oncogene in breast cancer cells. RGB-1 can serve as a tool for investigating the cellular functions of RNA G-quadruplex structures and identifying novel mRNA G-quadruplex-forming sequences. RGB-1 is applicable for breast cancer research.
  • HY-P10600A
    BIMAX2 acetate Inhibitor 98.66%
    BIMAX2 acetate is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 acetate can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 acetate can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence.
  • HY-175341
    Rac1-IN-5 Inhibitor 99.84%
    Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer.
  • HY-154959
    AZD4747 Inhibitor 99.07%
    AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRASG12C inhibitor. AZD4747 has the potential to study cancer.
  • HY-158304
    Rac1-IN-4 Inhibitor 98.61%
    Rac1-IN-4 (Cas: 2924486-45-1) is a Rac1 inhibitor.
  • HY-111432
    CCG-232601 Inhibitor 99.00%
    CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma.
  • HY-119264
    PRLX-93936 Inhibitor 98.31%
    PRLX-93936 is a molecular Glues that binds to and reprograms the TRIM21 ubiquitin ligase to degrade nuclear pore complexes. PRLX-93936 binds to TRIM21, forms a ternary complex with TRIM21 and NUP98, and mediates the ubiquitination and proteasomal degradation of NUP98 and other nuclear pore complex proteins. PRLX-93936 induces the loss of short-lived cytoplasmic mRNA transcripts, triggers cancer cell apoptosis (Apoptosis), and inhibits the activated Ras pathway. PRLX-93936 inhibits HIF-1 under hypoxic conditions (IC50 = 0.09 μM in cell-based reporter gene assay). PRLX-93936 suppresses tumor growth in mouse models and improves survival rates in mouse models of multiple myeloma. PRLX-93936 is applicable to research related to pancreatic cancer and multiple myeloma.
  • HY-151523
    KRas G12R inhibitor 1 Inhibitor 98.40%
    KRas G12R inhibitor 1 is a covalent inhibitor targeting the common oncogenic mutant KRas G12R with selectivity for the mutant arginine. KRas G12R inhibitor 1 possesses an α,β-diketoamide and exploits strong nucleophilicity of the mutant cysteine and irreversibly binds in the Switch II region of KRas. KRas G12R inhibitor 1 can be researched for K-Ras (G12R)-driven cancer such as pancreatic ductal adenocarcinoma (PDAC).
  • HY-12656
    SCH 51344 Inhibitor 98.79%
    SCH 51344 inhibits Ras induced malignant transformation and prevents anchorage-independent growth of oncogene transformed fibroblasts.
  • HY-132581A
    Tadnersen sodium Inhibitor 99.30%
    Tadnersen sodium, an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.
  • HY-117149
    MLS000532223 Inhibitor 98.45%
    MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases.
  • HY-15717
    Kobe2602 Inhibitor 98.20%
    Kobe2602 is a Ras-Raf interaction inhibitor. Kobe2602 inhibits the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki of 149 μM. Kobe2602 has antitumor activity.
  • HY-129738
    I942 Agonist 99.47%
    I942 is a first in class, selective non-cyclic nucleotide (NCN) EPAC1 agonist. I942 can attenuate proinflammatory cytokine signalling normally associated with cardiovascular diseases.
  • HY-149464
    ARN22089 Inhibitor 98.18%
    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.
  • HY-18674
    K-Ras-IN-1 Inhibitor 98.00%
    K-Ras-IN-1 is the inhibitor for K-Ras by occupying the binding site of son of sevenless (Sos), preventing the interaction between Sos and K-Ras, inhibiting the Sos-catalyzed GDP to GTP exchange process. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer.
  • HY-114277B
    Sotorasib isomer Control 98.85%
    Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.
  • HY-124808
    IMM-01 Agonist 99.12%
    IMM-01 is a mammalian Diaphanous (mDia)-related formins agonist that inhibits DID-DAD (diaphanous inhibitory domain-diaphanous autoregulatory domain) binding with an IC50 of 140 nM. IMM-01 acts by disrupting the autoinhibitory bond between the DID and DAD domain and thus activates formins. IMM-01 shows anticancer effects.
  • HY-15873A
    FTI 276 TFA Inhibitor 98.31%
    FTI 276 TFA is a farnesyltransferase (FTase) inhibitor with an IC50 of 0.5 nM, and it exhibits selectivity for FTase over geranylgeranyltransferase I (GGTase I). FTI 276 TFA blocks the farnesylation of H-Ras and K-Ras4B, causes inactive Ras-Raf complexes to accumulate in the cytoplasm, and inhibits constitutive MAPK activation. FTI 276 TFA reduces the number, incidence and volume of tumors, and restricts the growth of tumors expressing activated K-ras. FTI 276 TFA can be used in research related to pulmonary adenoma.
  • HY-172581
    Clifutinib Inhibitor 99.59%
    Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.
製品番号 製品名 / Synonyms Application Reactivity