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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PERK-HC-5404
HC-5404

Chemical Structure : HC-5404

CAS No.: 2247396-91-2

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HC-5404 (HC5404, LY-4)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 454.48
分子式 C24H24F2N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-2-amino-5-(4-(2-(3,5-difluorophenyl)-2-hydroxyacetamido)-2-methylphenyl)-N-isopropylnicotinamide

参考文献

1. Michael E Stokes, et al. Clin Cancer Res. 2023 Sep 21. doi: 10.1158/1078-0432.CCR-23-1182.

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