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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
138 Results for "
eIF2
" in MedChemExpress (MCE) Product Catalog:
Products (138)
138 Results for "eIF2" in MCE Product Catalog:
47
47 Publications Verification
Forschungsgebiete:
ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
43
43 Cited Publications
Target:
Forschungsgebiete:
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation . Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis [2]. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5 .
42
42 Cited Publications
Forschungsgebiete:
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
35
35 Cited Publications
9
9 Cited Publications
GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation .
4
4 Cited Publications
Forschungsgebiete:
2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .
4
4 Cited Publications
Art. -Nr.: HY-15969
CAS. Nr.: 1164470-53-4
Target:
Forschungsgebiete:
Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal .
4
4
4 Cited Publications
Synonyms: Sephin1; IFB-088
Target:
Forschungsgebiete:
Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect [2] .
3
3 Cited Publications
Synonyms: 1-Methylpseudouridine; N1-methyl-pseudouridine
Forschungsgebiete:
N1-methyl-pseudouridine (1-Methylpseudouridine), a methylpseudouridine, outperforms 5 mC and 5 mC/N1-methyl-pseudouridine in translation. N1-methyl-pseudouridine in mRNA enhances translation through eIF2α-dependent and independent mechanisms by increasing ribosome density .
3
3 Cited Publications
Target:
Forschungsgebiete:
BTdCPU is a potent heme regulated inhibitor kinase (HRI) activator that promotes eIF2α phosphorylation and induces apoptosis in Dexamethasone (HY-14648) (Dex)-resistant cancer cells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma [2].
3
3 Cited Publications
Forschungsgebiete:
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells) . GCN2-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
2
2 Cited Publications
Art. -Nr.: HY-P81190
Synonyms: p-PERK(Thr980); PERK(Phospho Thr980); PERK(Phospho T980); mo(Thr980)/hu (Thr982)/rat (Thr974); HRI; HsPEK; Pancreatic eIF2-alpha kinase; PEK; PRKR like endoplasmic reticulum kinase; WRS; DKFZp781H1925; EC 2.7.11.1; eIF2AK3; Eukaryotic translation initiation factor 2 alpha kinase 3; Heme regulated eIF2 alpha kinase.
1
1 Cited Publications
Art. -Nr.: HY-W050044
CAS. Nr.: 2133-34-8
Forschungsgebiete:
DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases [2] .
Forschungsgebiete:
HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia) [2].
Forschungsgebiete:
ATF4-IN-1 (Compound 21) is an ATF4 inhibitor and also an eIF2B activator. ATF4-IN-1 can be used in research on neurodegenerative diseases .
Art. -Nr.: HY-W054424
CAS. Nr.: 1638767-25-5
Target:
Forschungsgebiete:
tert-Butyl (3-aminobicyclo[1.1.1]pentan-1-yl) carbamate is a pharmaceutical intermediate used in the synthesis of various active compounds, such as for the preparation of tetrazole-based eIF2B activators .
Art. -Nr.: HY-W010451
CAS. Nr.: 533-73-3
Synonyms: Hydroxyhydroquinone
Forschungsgebiete:
EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively .
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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
