GSK 2606414

Based on 18 reference(s) in Google Scholar 9 10 18

Axon 2233

CAS [1337531-36-8]

MF C24H20F3N5O
MW 451.44

  • Purity: 99%
  • Soluble in DMSO

GSK 2606414

Description

Potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK or EIF2AK3) with IC50 value of 0.4 nM and >1000 fold selectivity over EIF2AK1 (HRI) and EIF2AK2 (PKR). Overall, good selectivity was observed, with only 20 protein kinases inhibited >85% by GSK 2606414 at 10 μM during screening against a panel of 294 kinases. It inhibits the growth of a human tumor xenograft in mice with good oral bioavailability and blood-brain barrier penetration.PERK is a type I ER membrane protein and one of three primary effectors of the unfolded protein response (UPR), which has a demonstrated role in tumor growth and angiogenesis.
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5 mg €99.00 In Stock
25 mg €345.00 In Stock
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2 x 5 mg €160.00 In Stock
2 x 25 mg €560.00 In Stock
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The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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