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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
8 Results for "
guanine nucleotide exchange factor activity
" in MedChemExpress (MCE) Product Catalog:
Products (8)
8 Results for "guanine nucleotide exchange factor activity" in MCE Product Catalog:
3
3 Cited Publications
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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 .
Synonyms: Paluratide
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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 .
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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-175326
CAS No.: 2767633-04-3
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 .
Cat. No.: HY-186309
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ISRACT-01 is an integrated stress response (ISR) activator. ISRACT-01 has a Kd of 557 nM for eIF2B Δ-latch. ISRACT-01 cooperates with eIF2-P to inhibit guanine nucleotide exchange factor (GEF) activity by specifically binding to and stabilizing the inactive conformation (I-state) of eIF2B. ISRACT-01 can be used in studies related to amyotrophic lateral sclerosis .
Cat. No.: HY-110100R
CAS No.: 310460-39-0
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CPYPP (Standard) is the analytical standard of CPYPP (HY-110100). This product is intended for research and analytical applications. CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-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 .
Cat. No.: HY-183703
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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 .
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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
