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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
58 Results for "
nucleotide exchange
" in MedChemExpress (MCE) Product Catalog:
Products (58)
58 Results for "nucleotide exchange" in MCE Product Catalog:
58
58 Publications Verification
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 .
35
35 Cited Publications
11
Target:
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 .
7
7 Cited Publications
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 .
3
3 Cited Publications
Target:
Research Areas:
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 .
2
2 Cited Publications
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 .
2
2 Cited Publications
Cat. No.: HY-P5985
CAS No.: 593267-11-9
1
1 Cited Publications
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 .
Synonyms: Paluratide
Target:
Research Areas:
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 .
Research Areas:
ISR-IN-1 is an integrated stress response (ISR) inhibitor targeting eIF2B. ISR-IN-1 enhances eIF2B guanine nucleotide exchange factor activity, stabilizes eIF2B heteropentamer dimers via symmetrical protein-protein interface binding, and releases global protein synthesis inhibition from phosphorylated eIF2α α. ISR-IN-1 can be used for the research of prion disease .
Cat. No.: HY-168624
CAS No.: 3050683-29-6
Target:
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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 .
Cat. No.: HY-129189
CAS No.: 2252242-32-1
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 .
Cat. No.: HY-179414
CAS No.: 3102130-17-3
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 .
Cat. No.: HY-120816
CAS No.: 1702378-78-6
Target:
Research Areas:
WU-07047, a simplified analog of YM-254890 (HY-111557), is a selective Gαq/11 inhibitor. WU-07047 can inhibit nucleotide exchange .
Cat. No.: HY-162446
CAS No.: 3033637-76-9
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
Cat. No.: HY-P1382
CAS No.: 1095179-01-3
Cat. No.: HY-134263
CAS No.: 190522-24-8
Research Areas:
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 .
Cat. No.: HY-134813A
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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
