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Chemical Structure : HC-5404
Catalog No.: PC-21218Not For Human Use, Lab Use Only.
HC-5404 (LY-4) is a potent, selective and orally active inhibitor of PKR-like endoplasmic reticulum kinase (PERK, EIF2AK3) with IC50 of 1 nM.
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HC-5404 (LY-4) is a potent, selective and orally active inhibitor of PKR-like endoplasmic reticulum kinase (PERK, EIF2AK3) with IC50 of 1 nM.
HC-5404 displays >2000-fold biochemical selectivity against the other integrated stress response (ISR) kinases GCN2 (EIF2AK4), HRI (EIF2AK1), and PKR (EIF2AK2) (IC50>2,000 nM), and excellent selectivity against a KINOMEScan binding panel assay with 468 unique kinases.
HC-5404 potently inhibits tunicamycin (1 uM) induced ER stress in HEK-293 cells, inhibits PERK autophosphorylation at Thr982 (pPERK) and suppresses ATF4 levels with IC50 of 23 nM and 88 nM, respectively.
HC-5404 (30 mg/kg, orally BID) suppress tumor growth in the 786-O xenograft model of RCC.
Cotreatment with HC-5404 inhibited PERK in tumors and significantly increased antitumor effects of VEGFR-TKIs across multiple RCC models, resulting in tumor stasis or regression.
| M.Wt | 454.48 | |
| Formula | C24H24F2N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Michael E Stokes, et al. Clin Cancer Res. 2023 Sep 21. doi: 10.1158/1078-0432.CCR-23-1182.
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