GSK 2606414 (CAS 1337531-36-8)
Alternate Names:
7-Methyl-5-[1-[[3-(trifluoromethyl)phenyl]acetyl]-2,3-dihydro-1H-indol-5-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number:
1337531-36-8
Molecular Weight:
451.44
Molecular Formula:
C24H20F3N5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GSK 2606414, serves as a selective inhibitor of protein kinase R-like ER kinase (PERK), displaying an IC50 value of 0.4 nM. In lung carcinoma A549 cells, it effectively inhibits thapsigargin-induced PERK phosphorylation. Moreover, GSK2606414 demonstrates the ability to attenuate the growth of subcutaneous human pancreatic tumor xenografts in mice. Considering that PERK plays a role in the unfolded protein response pathway, which is involved in neurotoxicity and cancer, inhibiting PERK signaling holds potential applications in cancer treatment and cognitive degeneration. Specifically designed as a selective PERK inhibitor, GSK 2606414 effectively hinders PERK activation in cells. This inhibition translates into the suppression of a human tumor xenograft′s growth in mice.
GSK 2606414 (CAS 1337531-36-8) References
- Constitutive and ligand-induced EGFR signalling triggers distinct and mutually exclusive downstream signalling networks. | Chakraborty, S., et al. 2014. Nat Commun. 5: 5811. PMID: 25503978
- Inhibition of endoplasmic reticulum (ER) stress sensors sensitizes cancer stem-like cells to ER stress-mediated apoptosis. | Fujimoto, A., et al. 2016. Oncotarget. 7: 51854-51864. PMID: 27322083
- Silver nanoparticles induce irremediable endoplasmic reticulum stress leading to unfolded protein response dependent apoptosis in breast cancer cells. | Simard, JC., et al. 2016. Apoptosis. 21: 1279-1290. PMID: 27586505
- Isochaihulactone-induced DDIT3 causes ER stress-PERK independent apoptosis in glioblastoma multiforme cells. | Tsai, SF., et al. 2017. Oncotarget. 8: 4051-4061. PMID: 27852055
- Cleavage of caspase-12 at Asp94, mediated by endoplasmic reticulum stress (ERS), contributes to stretch-induced apoptosis of myoblasts. | Song, J., et al. 2018. J Cell Physiol. 233: 9473-9487. PMID: 29943814
- Glucose-6-phosphate dehydrogenase blockade potentiates tyrosine kinase inhibitor effect on breast cancer cells through autophagy perturbation. | Mele, L., et al. 2019. J Exp Clin Cancer Res. 38: 160. PMID: 30987650
- Urokinase-Type Plasminogen Activator Protects Cerebral Cortical Neurons from Soluble Aβ-Induced Synaptic Damage. | Diaz, A., et al. 2020. J Neurosci. 40: 4251-4263. PMID: 32332118
- KSHV infection skews macrophage polarisation towards M2-like/TAM and activates Ire1 α-XBP1 axis up-regulating pro-tumorigenic cytokine release and PD-L1 expression. | Gilardini Montani, MS., et al. 2020. Br J Cancer. 123: 298-306. PMID: 32418990
- Simvastatin Induces Unfolded Protein Response and Enhances Temozolomide-Induced Cell Death in Glioblastoma Cells. | Dastghaib, S., et al. 2020. Cells. 9: PMID: 33105603
- Cyclical aggregation extends in vitro expansion potential of human mesenchymal stem cells. | Bijonowski, BM., et al. 2020. Sci Rep. 10: 20448. PMID: 33235227
- PERK/ATF4-Dependent ZFAS1 Upregulation Is Associated with Sorafenib Resistance in Hepatocellular Carcinoma Cells. | Lin, JC., et al. 2021. Int J Mol Sci. 22: PMID: 34072570
- Gut microbe-derived metabolite trimethylamine N-oxide activates PERK to drive fibrogenic mesenchymal differentiation. | Kim, SJ., et al. 2022. iScience. 25: 104669. PMID: 35856022
- Non-essential amino acid availability influences proteostasis and breast cancer cell survival during proteotoxic stress. | Sannino, S., et al. 2023. Mol Cancer Res.. PMID: 36961392
Inhibitor of:
(eukaryotic translation initiation factor) eIF, (eukaryotic translation initiation factor) eIF1, (eukaryotic translation initiation factor) eIF2, (eukaryotic translation initiation factor) eIF3, (eukaryotic translation initiation factor) eIF4, (eukaryotic translation initiation factor) eIF5, C1orf122, CCDC47, CREB3L2, eIF1AY, eIF2α, eIF2Bδ, eIF3M, eIF4B, eIF5A1, FAM75A1, GCN1L1, HIV GAG, HRI, KIAA0141, Membralin, P-Selectin, scotin, Sec13, SIL1, SLITRK1, SPCS2, TMCO4, and Torsin3A.Activator of:
ERp29, HRI, TGIF2LX, TGIF2LY, and VSTM1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK 2606414, 5 mg | sc-490182 | 5 mg | $160.00 | |||
GSK 2606414, 25 mg | sc-490182A | 25 mg | $561.00 |