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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
25 Results for "
GCN2
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "GCN2" in MCE Product Catalog:
63
63 Publications Verification
Research Areas:
GCN2iB is an ATP-competitive, selective GCN2 inhibitor with an IC50 of 2.4 nM. GCN2iB inhibits the activation of the GCN2 pathway and upregulates GPX4. GCN2iB enhances the anticancer effect of ASNase against acute lymphoblastic leukemia. GCN2iB increases left ventricular ejection fraction, while reducing fasting blood glucose and myocardial fibrosis. GCN2iB can be used in research related to acute lymphoblastic leukemia, acute myeloid leukemia and diabetic cardiomyopathy [2].
27
27 Cited Publications
Research Areas:
GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay .
12
12 Cited Publications
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy [2].
3
3 Cited Publications
Research Areas:
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
Research Areas:
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo .
Cat. No.: HY-160196
CAS No.: 2803470-63-3
Synonyms: GCN2 modulator-1
Research Areas:
HC-7366 (GCN2 modulator-1) is an orally effective GCN2 activator. HC-7366 can effectively compete and occupy the ATP binding pocket of GCN2, with its IC50 being 72 nM. This binding triggers the conformational activation of GCN2, leading to the upregulation of downstream signals (such as ATF4, ASNS) in the integrated stress response (ISR) pathway, ultimately exerting anti-tumor effects. HC-7366 also has inhibitory activity against ZAK, with its IC50 being 47 nM. HC-7366 can be used for research on fibrosarcoma and acute myeloid leukemia .
Cat. No.: HY-W319647
CAS No.: 315705-10-3
Research Areas:
GCN2 activator-1 (Compound 20) is a GCN2 activator. GCN2 activator-1 binds within the ATP-pocket of GCN2 and activates GCN2 in a GCN1-independent manner. GCN2 activator-1 activates Integrated Stress Response (ISR) in cells. GCN2 activator-1 inhibits PKR with an IC50 of 3.75 µM. GCN2 activator-1 can be used for research of pulmonary veno-occlusive disease (PVOD) .
Cat. No.: HY-162730
CAS No.: 2131210-15-4
Research Areas:
OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor .
Cat. No.: HY-117938
CAS No.: 2209057-94-1
Target:
Research Areas:
T-3861174 is an inhibitor of prolyl-tRNA synthetase (PRS, Aminoacyl-tRNA Synthetase) without completely inhibiting its translation process. T-3861174 activates the GCN2-ATF4 pathway and induces death in multiple tumor cell lines, including SK-MEL-2. T-3861174 demonstrated significant antitumor activity in multiple xenograft models without significantly affecting body weight .
Cat. No.: HY-175880
CAS No.: 1644664-11-8
Research Areas:
AMG-34 is a GCN2-targeting agent with IC50 values of 0.395 μM, 0.010 μM, 1.07 μM and ＞ 10 μM for GCN2, PERK, HRland PKR, respectively .
Cat. No.: HY-175877
CAS No.: 2396467-34-6
Research Areas:
RAPT-37-Me is a GCN2-targeting agent with IC50 values of 0.002μM, ＞ 10 μM,4.40 μM and 1.31 μM for GCN2, PERK, HRl and PKR, respectively .
Cat. No.: HY-112654A
CAS No.: 2183470-13-3
Research Areas:
GCN2iB acetate is an ATP-competitive, selective GCN2 inhibitor with an IC50 of 2.4 nM. GCN2iB acetate inhibits the activation of the GCN2 pathway and upregulates GPX4. GCN2iB acetate enhances the anticancer effect of ASNase against acute lymphoblastic leukemia. GCN2iB acetate increases left ventricular ejection fraction, while reducing fasting blood glucose and myocardial fibrosis. GCN2iB acetate can be used in research related to acute lymphoblastic leukemia, acute myeloid leukemia and diabetic cardiomyopathy [2].
Cat. No.: HY-208758A
CAS No.: 1627177-37-0
Research Areas:
(S)-GCN2-IN-8 is a general control nonderepressible 2 (GCN2, EIF2AK4) inhibitor. (S)-GCN2-IN-8 inhibits signal transduction by the stress response kinase GCN2. (S)-GCN2-IN-8 can be used for the research of cancer .
Cat. No.: HY-208758
CAS No.: 1627180-54-4
Research Areas:
GCN2/GSK3α-IN-1 is a GCN2 and GSK3α inhibitor with an IC50 of less than 1 μM for both targets. GCN2/GSK3α-IN-1 can be used in cancer research .
Cat. No.: HY-175878
Research Areas:
EMD-C02602 is a GCN2-targeting agent with IC50 values of 0.023 μM, 4.52 μM, ＞ 10 μM and 0.048 μM for GCN2, PERK, HRland PKR, respectively .
Cat. No.: HY-P705590
Synonyms: eIF-2-alpha kinase GCN2; Eukaryotic translation initiation factor 2-alpha kinase 4; GCN2-like protein; GCN2; KIAA1338; EC:2.7.11.1
Species:
Source:
Cat. No.: HY-181959
CAS No.: 2752441-61-3
Research Areas:
APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia .
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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
