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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
22 Results for "
eIF2α phosphorylation
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "eIF2α phosphorylation" in MCE Product Catalog:
47
47 Publications Verification
Research Areas:
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).
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 .
3
3 Cited Publications
Synonyms: 1-Methylpseudouridine; N1-methyl-pseudouridine
Research Areas:
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:
Research Areas:
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 .
1
1 Cited Publications
Cat. No.: HY-156675A
Purity: 99.34%
Target:
Microtubule/Tubulin Eukaryotic Initiation Factor (eIF) HSP Caspase Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
Plecstatin-1 hydrochloride is a metal complex that drives the aggregation and collapse of the plectin network, and disrupts the cytoskeletal structures of α‑tubulin and F‑actin. Plecstatin-1 hydrochloride triggers oxidative stress, mediates the phosphorylation of eIF2α, and induces molecular features associated with immunogenic cell death, including calreticulin membrane exposure, membrane localization of HSP70/HSP90, ATP secretion, and HMGB‑1 release. Plecstatin-1 hydrochloride induces apoptosis via the intrinsic mitochondrial pathway and exerts anti-invasive activity. Plecstatin-1 hydrochloride inhibits sphere proliferation and reduces clonogenicity in the 3D tumor spheroid model of colon cancer cells. Plecstatin-1 hydrochloride is applicable to relevant research on colorectal cancer .
Research Areas:
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) .
Cat. No.: HY-W010451
CAS No.: 533-73-3
Synonyms: Hydroxyhydroquinone
Cat. No.: HY-101997
CAS No.: 455311-98-5
Target:
BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) modulator. BEPP hydrochloride enhances the phosphorylation levels of PKR and eIF2α, activates caspase-3, upregulates the pro-apoptotic protein BAX, and downregulates the anti-apoptotic protein Bcl-2. BEPP hydrochloride inhibits vaccinia virus replication and exhibits selective cytotoxicity in cells expressing PKR. BEPP hydrochloride can be used in research related to cancer and viral infections .
Cat. No.: HY-172815
CAS No.: 3079913-81-5
Research Areas:
IDB-001 is a human ribosomal peptidyl transferase center (PTC) inhibitor that induces conformational changes and blocks translational elongation in specific sequence contexts through complementary interactions with Asp/Glu residues in nascent polypeptides. IDB-001 preferentially stalls ribosomes at positions containing acidic peptide motifs, thereby inhibiting cancer cell proliferation, and activates the integrated stress response via eIF2α phosphorylation at high concentrations. In addition, IDB-001 mildly triggers ribotoxic stress responses through phosphorylation of JNK and p38. IDB-001 has been applied to mechanistic studies of triple-negative breast cancer .
Research Areas:
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 .
Cat. No.: HY-13559
CAS No.: 123018-47-3
Synonyms: Azaspirane ; SKF 106615-12; SKF 106615A12
Target:
STAT Apoptosis Autophagy Reactive Oxygen Species (ROS) Caspase Bcl-2 Family p62 Atg8/LC3 PARP NF-κB PERK JAK
Research Areas:
Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
Cat. No.: HY-156675
CAS No.: 2119725-22-1
Target:
Microtubule/Tubulin Eukaryotic Initiation Factor (eIF) HSP Caspase Reactive Oxygen Species (ROS) Apoptosis
Research Areas:
Plecstatin‑1 is a metal complex that drives the aggregation and collapse of the plectin network, and disrupts the cytoskeletal structures of α‑tubulin and F‑actin. Plecstatin-1 triggers oxidative stress, mediates the phosphorylation of eIF2α, and induces molecular features associated with immunogenic cell death, including calreticulin membrane exposure, membrane localization of HSP70/HSP90, ATP secretion, and HMGB‑1 release. Plecstatin-1 induces apoptosis via the intrinsic mitochondrial pathway and exerts anti-invasive activity. Plecstatin‑1 inhibits sphere proliferation and reduces clonogenicity in the 3D tumor spheroid model of colon cancer cells. Plecstatin-1 is applicable to relevant research on colorectal cancer .
Cat. No.: HY-110102
CAS No.: 130065-61-1
Synonyms: Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615
Research Areas:
Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
Cat. No.: HY-13559A
CAS No.: 183063-72-1
Synonyms: Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate
Target:
STAT Apoptosis Caspase Interleukin Related Autophagy Reactive Oxygen Species (ROS) Atg8/LC3 p62 JAK
Research Areas:
Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
Cat. No.: HY-W010451R
CAS No.: 533-73-3
Synonyms: Hydroxyhydroquinone (Standard)
Category:
Cat. No.: HY-18956A
CAS No.: 32597-86-7
Synonyms: (E/Z)-Sephin1 hydrochloride; (E/Z)-IFB-088 hydrochloride
Target:
Research Areas:
(E/Z)-Icerguastat hydrochloride ((E/Z)-Sephin1 hydrochloride) is a selective inhibitor with activity that prolongs the phosphorylation effects of eIF2α. (E/Z)-Icerguastat hydrochloride protects cells from defects in proteostasis. (E/Z)-Icerguastat hydrochloride was shown to significantly extend the survival of infected prion mice in a mouse model. (E/Z)-Icerguastat hydrochloride effectively reduces PrPSc expression and prion sequence activity in various neuronal cell lines persistently infected with different prion strains .
Cat. No.: HY-138844
CAS No.: 1184391-57-8
Research Areas:
3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research .
Cat. No.: HY-159494
Target:
Research Areas:
PROTAC sEH degrader-1 is a PROTAC degrader targeting soluble epoxide hydrolase (sEH) with a DC50 of 0.5 nM, and it also possesses sEH inhibitory activity. PROTAC sEH degrader-1 has an IC50 of 3.8 nM against human sEH and an IC50 of 210 nM against mouse sEH. PROTAC sEH degrader-1 relies on the ubiquitin-proteasome system to achieve target protein degradation, and it selectively degrades cytoplasmic sEH. PROTAC sEH degrader-1 rapidly reduces endoplasmic reticulum stress in cells, downregulates the phosphorylation levels of IRE1α, PERK and eIF2α, enhances cell viability, and alleviates Thapsigargin (HY-13433)-induced apoptosis. PROTAC sEH degrader-1 effectively degrades sEH in mouse liver and brown adipose tissue. PROTAC sEH degrader-1 can be used in studies related to metabolic disorders and inflammation .
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 .
Cat. No.: HY-184599
Research Areas:
OICR-403184 is a selective RNA-dependent protein kinase (PKR) inhibitor with limited brain penetration, with an IC50 of 263 nM. OICR-403184 blocks the phosphorylation of eIF2α downstream of PKR. OICR-403184 is applicable to the research of inflammatory bowel disease .
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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
