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Results for "

guanine nucleotide exchange factor activity

" in MedChemExpress (MCE) Product Catalog:

5

Inhibitors & Agonists

1

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156002
    LUNA18

    Paluratide

    		 Ras ERK Cancer
    LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
    LUNA18
  • HY-110100
    CPYPP
    3 Publications Verification

    		 DOCK Inflammation/Immunology
    CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9 .
    CPYPP
  • HY-153128
    DOCK2-IN-1

    		DOCK Drug Derivative Inflammation/Immunology
    DOCK2-IN-1 (Compound 3) is an analog of CPYPP (HY-110100) and a DOCK2 inhibitor (IC50 = 19.1 μM). DOCK2-IN-1 binds to the DHR-2 domain of DOCK2 and inhibits its mediated Rac guanine nucleotide exchange factor activity. DOCK2-IN-1 blocks chemokine receptor- and antigen receptor-mediated activation of Rac in lymphocytes. DOCK2-IN-1 significantly inhibits chemotaxis and T cell activation. DOCK2-IN-1 can be used in the research of transplant rejection and organ-specific autoimmune diseases .
    DOCK2-IN-1
  • HY-175326
    SOS1-IN-21

    		SOS1 Cancer
    SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
    SOS1-IN-21
  • HY-183703
    ISR activator-4

    		Eukaryotic Initiation Factor (eIF) Mitogen- and Stress-Activated Protein Kinase (MSK) Neurological Disease Metabolic Disease Cancer
    ISR activator-4 is an eIF2B modulator and integrated stress response (ISR) activator with a human eIF2B EC50 of 2.2 μM. ISR activator-4 stabilises the inactive I-state of eIF2B, favours formation of the inhibitory eIF2B-eIF2(αP) complex, and attenuates eIF2B's guanine nucleotide exchange factor activity. ISR activator-4 can be used for the research of cancer, neurologic and metabolic disorders .
    ISR activator-4

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