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nucleotide exchange

" in MedChemExpress (MCE) Product Catalog:

34

Inhibitors & Agonists

1

Biochemical Assay Reagents

6

Peptides

2

Antibodies

4

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12495A
    ISRIB
    25+ Cited Publications

    		 Biochemical Assay Reagents Eukaryotic Initiation Factor (eIF) Neurological Disease
    ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .
    ISRIB
  • HY-134813
    MRTX1133
    45+ Cited Publications

    		 Ras Cancer
    MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
    MRTX1133
  • 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-100540
    Golgicide A
    10+ Cited Publications

    GCA

    		 Enterovirus Infection Cancer
    Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1 . Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species .
    Golgicide A
  • 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-114398
    BAY-293
    2 Publications Verification

    		 SOS1 Ras Cancer
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS .
    BAY-293
  • HY-12649
    Y16
    5+ Cited Publications

    		 Ras Cancer
    Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP .
    Y16
  • 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-P5985
    mSIRK
    2 Publications Verification

    		 ERK Others
    mSIRK (G-Protein βγ Binding Peptide) is an cell-permeable activator of ERK1/2, with EC50 of 2.5-5 μM. mSIRK disrupts the interaction between α and βγ subunits and promotes α subunit dissociation without stimulating nucleotide exchange .
    mSIRK
  • HY-168624
    VAV1 degrader-2

    		Molecular Glues Inflammation/Immunology
    VAV1 degrader-2 is a molecular glue degrader based on targeting Vav guanine nucleotide exchange factor 1 (VAV 1) with a DC50 of 4.41 nM. VAV1 degrader-2 can be used in the study of inflammatory and autoimmune diseases .
    VAV1 degrader-2
  • HY-129189
    RAS GTPase inhibitor 1

    		Ras Cancer
    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-P1382A
    Rac1 Inhibitor W56 TFA

    		Ras Cancer
    Rac1 Inhibitor W56 TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 TFA inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam .
    Rac1 Inhibitor W56 TFA
  • HY-179414
    KRAS G12D-IN-34

    		Ras Cancer
    KRAS G12D-IN-34 (Compound 13) is a KRAS (G12D) inhibitor with IC50 values for KRAS (G12D) and KRAS (WT) of 1.05 nM and 1.59 μM respectively. KRAS G12D-IN-34 can be used for research on non-small cell lung cancer .
    KRAS G12D-IN-34
  • HY-120816
    WU-07047

    		Calcium Channel Cardiovascular Disease
    WU-07047, a simplified analog of YM-254890 (HY-111557), is a selective Gαq/11 inhibitor. WU-07047 can inhibit nucleotide exchange .
    WU-07047
  • HY-162446
    pan-KRAS-IN-13

    		Ras Cancer
    pan-KRAS-IN-13 (compound 2) is a potent inhibitor of KRAS, with IC50s of 2.75 nM and 2.89 nM for G12D and G12V, respectively
    pan-KRAS-IN-13
  • HY-P1382
    Rac1 Inhibitor W56

    		Ras Cancer
    Rac1 Inhibitor W56 is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor W56 inhibits Rac1 interaction with guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam .
    Rac1 Inhibitor W56
  • HY-111550
    Bragsin2
    1 Publications Verification

    		 Ras MDM-2/p53 Cancer
    Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells .
    Bragsin2
  • HY-134263
    8-Br-cAMP-AM

    		PKA Ras Cardiovascular Disease
    8-Br-cAMP-AM is a cyclic adenosine monophosphate (cAMP) analog that activates two major signal transduction pathways in the heart by mimicking the effects of cAMP: protein kinase A (PKA) and guanosine nucleotide exchange factor (Epac), which is directly activated by cAMP. 8-Br-cAMP-AM can be used to study cardiac ischemia and reperfusion injury .
    8-Br-cAMP-AM
  • HY-134813A
    MRTX1133 formic

    		Ras Cancer
    MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
    MRTX1133 formic
  • HY-162321
    ZINC57632462

    		Ras Cancer
    ZINC57632462 (ACA-6) is a non-covalent allosteric KRAS inhibitor. ZINC57632462 disrupts nucleotide exchange and inhibits RAS-effector interaction. ZINC57632462 can be used for the research of cancer .
    ZINC57632462
  • HY-168480
    SOS2 ligand 1

    		Ras Cancer
    SOS2 ligand 1(compound 2) is a selective ligand of son of sevenless 2 (SOS2) with an KD value of 4.6 µM .
    SOS2 ligand 1
  • HY-173341
    SOF-436

    		Ras Cancer
    SOF-436 is a KRAS inhibitor that inhibits SOS1-mediated KRAS nucleotide exchange (IC50 = 60 μM) and the binding of KRAS to the effector protein RAF. SOF-436 can be used in cancer research .
    SOF-436
  • HY-100540A
    (Rac)-Golgicide A

    (Rac)-GCA

    		 Enterovirus Infection
    (Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A. Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1 .Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species .
    (Rac)-Golgicide A
  • 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-P1383A
    Rac1 Inhibitor F56, control peptide TFA

    		Ras Others
    Rac1 Inhibitor F56, control peptide TFA is a peptide containing residues 45-60 of Rac1. Rac1 Inhibitor F56, control peptide TFA contains a Trp 56 to Phe 56 mutation. Rac1 Inhibitor F56, control peptide TFA has no effect on Rac1 interaction with its guanine nucleotide exchange factors (GEFs) .
    Rac1 Inhibitor F56, control peptide TFA
  • HY-122685
    UC-773587

    		SOS1 Cancer
    UC-773587 is a selective SOS1 catalytic activity inhibitor. UC-773587 binds to the catalytic site of Sos1 over HRas and ITSN (a RhoGEF) and inhibits nucleotide exchange with an IC50 value of 4.5 μM. UC-773587 mappes to the Ras switch II interaction region of the Sos1 catalytic site. UC-773587 can be used for the study of prostate cancer .
    UC-773587
  • HY-134318B
    8-Azido-ADP disodium

    		DNA/RNA Synthesis Others
    8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP . 8-Azido-ADP (disodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    8-Azido-ADP disodium
  • HY-175290
    Arf1-GEFs-IN-1

    		Arf Family GTPase Cancer
    Arf1-GEFs-IN-1 is a potent and orally active ADP-ribosylation factor 1- guanine nucleotide exchange factors (Arf1-GEFs) inhibitor with an IC50 value of 40.85 μM against CT26 cells. Arf1-GEFs-IN-1 primarily mediates tumor regression by triggering anti-tumor immune responses, rather than through direct cytotoxicity. Arf1-GEFs-IN-1 effectively promotes CCL5 expression, demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 can be used for the study of colon cancer .
    Arf1-GEFs-IN-1
  • 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
  • HY-124755
    RAS activator compound 1

    		Ras SOS1 Cancer
    RAS activator compound 1 (Compound 7c) is a RAS activator targeting the guanine nucleotide exchange factor (GEF) son of sevenless homologue 1 (SOS1). RAS activator compound 1 can activate the nucleotide exchange process and increase levels of active RAS-GTP in HeLa cells. RAS activator compound 1 can be used for research of RAS-driven tumor .
    RAS activator compound 1
  • HY-118692
    DCAI

    		Ras Cancer
    DCAI is Ras protein binder. DCAI can inhibit the Ras activation and nucleotide exchange mediated by SOS. DCAI can be used for the research of cancer associated with Ras mutations .
    DCAI
  • HY-180920
    KRAS G12D-IN-36

    		Ras ERK Cancer
    KRAS G12D-IN-36 (Compound 53a) is a highly selective and orally active KRAS-G12D inhibitor with an IC50 of 1.63 nM. KRAS G12D-IN-36 effectively inhibits p-ERK with an IC50 of 8.4 nM. KRAS G12D-IN-36 shows potent anti-proliferative activity against AsPC-1 cells. KRAS G12D-IN-36 can be used for research on pancreatic cancer .
    KRAS G12D-IN-36
  • HY-181965
    KRAS G12C-IN-78

    		Ras ERK p38 MAPK Cancer
    KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
    KRAS G12C-IN-78
  • HY-183365
    SL43

    		SOS1 Ras p38 MAPK ERK MEK Apoptosis Cancer
    SL43 is an orally active and potent SOS1 inhibitor with a Kd of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model .
    SL43

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