Structure of GSK2606414
CAS No.: 1337531-36-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM.
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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Chen, Long ; Shi, Yiping ; Xiao, Danrui ; Huang, Yijie ; Jiang, Yangjing ; Liang, Min , et al.
Abstract: Rupture of vulnerable carotid atherosclerotic plaque is one of the leading causes of ischemic stroke. However, the mechanisms driving the transition from stable to vulnerable plaques have not yet been elucidated. NR4A1 is an orphan nuclear receptor that functions in various inflammatory diseases. To explore the role of NR4A1 in vulnerable plaque formation, we generated a vulnerable plaque mouse model by combining partial ligation of the left common carotid artery and left renal artery in ApoE−/− and ApoE−/−;NR4A1−/− mice. Our research revealed that NR4A1 deficiency significantly worsened the pathology of vulnerable plaque, increasing intraplaque hemorrhage, rupture with thrombus, and the occurrence of multilayer with discontinuity. Moreover, NR4A1 deficiency exacerbated macrophage infiltration, inflammation, and oxidative stress. Mechanistically, we identified Bcat1 as the target of NR4A1. NR4A1 modulated the integrated stress response (ISR) in macrophages by transcriptionally inhibiting Bcat1, thus influencing the progression of vulnerable plaque. ISR inhibitor GSK2606414 or Bcat1 inhibitor ERG240 significantly ameliorated atherosclerotic plaque formation and increased plaque stability. Notably, supplementation with Celastrol, an herbal extract, stabilized atherosclerotic plaques in mice. These findings suggest that NR4A1 deficiency exacerbates vulnerable plaque by activating ISR via targeting Bcat1. The NR4A1/Bcat1/ISR axis is therefore an important therapeutic target for stabilizing atherosclerotic plaque.
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Keywords: NR4A1 ; Integrated stress response ; Vulnerable plaque ; Bcat1
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CAS No. : | 1337531-36-8 |
Formula : | C24H20F3N5O |
M.W : | 451.44 |
SMILES Code : | FC(C1=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3)=O)=CC=C1)(F)F |
MDL No. : | MFCD25976926 |
InChI Key : | SIXVRXARNAVBTC-UHFFFAOYSA-N |
Pubchem ID : | 53469448 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
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In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
INS-1E cells | 0.5 μM | To investigate the effect of GSK2606414 on ER stress-induced PPP1R15B expression, results showed that GSK2606414 prevented the induction of PPP1R15B expression. | PMC4713904 | |
PDAC cells | 10μM | 0–72 h | GSK2606414 significantly inhibited the cell viability of BZW1 high expression organoids | PMC9436032 |
pancreatic cancer cells T3M-4 | 250 nM | 4 h | To investigate the effect of GSK2606414 on mitochondrial morphology induced by ER stress, results showed that GSK2606414 partially reversed mitochondrial morphology in Sc cells | PMC7217954 |
mouse vascular smooth muscle cell (VSMC) | 2 μM | 24 h | GSK2606414 inhibited TMAO-induced ROS generation, indicating that PERK plays a crucial role in TMAO-enhanced Ang II responses. | PMC8408632 |
Bone marrow-derived macrophages (BMMs) | 0.01, 0.05, 0.1 μM | 4 days | GSK2606414 significantly inhibited osteoclast formation and bone resorption function, and reduced the number of F-actin rings | PMC7554039 |
FaDu cells | 2 μM and 5 μM | 72 h | GSK2606414 enhanced the efficacy of reovirus in FaDu cells, as evidenced by significantly reduced cell viability. | PMC7047134 |
HN5 cells | 2 μM and 5 μM | 72 h | GSK2606414 enhanced the efficacy of reovirus in HN5 cells, as evidenced by significantly reduced cell viability. | PMC7047134 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
nude mice | subcutaneous xenograft model | oral | 100mg/kg | twice a week, until after tumor development | GSK2606414 significantly suppressed tumor growth and prolonged the survival time of nude mice | PMC9436032 |
Mice | Ovariectomy model (OVX) | Intragastric gavage | 50 mg/kg | Every 2 days for 6 weeks | GSK2606414 significantly alleviated bone loss in OVX mice and inhibited osteoclast formation | PMC7554039 |
NSG mice | HN5 cell subcutaneous xenograft model | Oral | 50 mg/kg | Once daily for 5 days, followed by 2 days off, repeated for 3 cycles | GSK2606414 significantly enhanced the antitumor efficacy of reovirus in the HN5 cell xenograft model, as evidenced by a significant reduction in tumor volume. | PMC7047134 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.22mL 0.44mL 0.22mL |
11.08mL 2.22mL 1.11mL |
22.15mL 4.43mL 2.22mL |
Tags: GSK2606414 | GSK 2606414 | GSK-2606414 | PERK | eIF2α kinase | PKR-like kinase | ER stress | protein synthesis inhibition | unfolded protein response | Apoptosis | Protein kinase R-like endoplasmic reticulum kinase | PKR-like endoplasmic reticulum kinase | 1337531-36-8
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