SML3049
AMG PERK 44
≥98% (HPLC)
同義詞:
4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1H-pyrazol-3(2H)-one hydrochloride, 4-[2-Amino-4-methyl-3-(2-methyl-6-quinolinyl)benzoyl]-1,2-dihydro-1-methyl-2,5-diphenyl-3H-pyrazol-3-one hydrochloride, AMG′44, AMG44, Compound 44, PERK inhibitor 44, PERK-IN-1
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About This Item
經驗公式（希爾表示法）:
C34H28N4O2 · xHCl
CAS號碼:
分子量：:
524.61 (free base basis)
分類程式碼代碼:
12352200
NACRES:
NA.77
推薦產品
![PERK抑制剂I，GSK2606414 GSK2606414 is a cell-permeable, highly potent inhibitor of EIF2AK3/PERK (IC₅₀ = 0.4 nM; [ATP] = 5 µM). Targets PERK in its inactive DFG conformation at the ATP-binding region.](/deepweb/assets/sigmaaldrich/product/structures/180/559/efa716dc-d5fe-4339-a6f0-0103084fc04a/640/efa716dc-d5fe-4339-a6f0-0103084fc04a.png)
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
O=C1N(N(C(C2=CC=CC=C2)=C1C(C3=CC=C(C(C4=CC=C5N=C(C=CC5=C4)C)=C3N)C)=O)C)C6=CC=CC=C6.[xHCl]
生化／生理作用
AMG PERK 44 (AMG44) is an orally active (F = 46% (mouse) & 55% (rat) post 2.5 mg/kg po.), active site-targeing, potent and highly selective PERK (EIF2AK3) inhibitor (IC50 = 6 nM; GCN2 IC50 = 7.3 μM, b-Raf IC50 >1 μM, <65% inhibition at 1 μM against 387 kinases). AMG44 inhibits cellular PERK autophosphorylation (pT980 IC50 = 84 nM; HT1080 T-REx-PERK-FLAG transfectants) and ER stress-induced bulk protein synthesis (IC50 = 400 nM; U2OS), as well as PERK pT980 in HT1080 Matrigel plug implant in mice in vivo (ED50 = 3 mg/kg & ED90 = 60 mg/kg 4 hr post po.).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號，寫有 ‘Lot’或‘Batch’.。
Adrian L Smith et al.
Journal of medicinal chemistry, 58(3), 1426-1441 (2015-01-15)
The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploration both in vitro
Natalia M Peñaranda-Fajardo et al.
Cell death & disease, 10(10), 690-690 (2019-09-20)
Patients with aggressive brain tumors, named glioblastoma multiforme (GBM), have a poor prognoses. Here we explored if the ER stress/unfolded protein response (UPR) is involved in the pathophysiology of GBM and may provide novel therapeutic targets. Immunohistochemical analyses of a
Manar G Helal et al.
Life sciences, 239, 117017-117017 (2019-11-05)
Saxagliptin (Saxa), a dipeptidyl dipeptidase-4 (DPP-4) inhibitor, is widely used for the treatment of type 2 diabetes mellitus. It has been documented to have immunomodulatory and anti-inflammatory actions. Our objective was to delineate the protective effect and the underlying mechanism
Diego Rojas-Rivera et al.
Cell death and differentiation, 24(6), 1100-1110 (2017-04-30)
Accumulation of unfolded proteins in the endoplasmic reticulum (ER) causes a state of cellular stress known as ER stress. The cells respond to ER stress by activating the unfolded protein response (UPR), a signaling network emerging from the ER-anchored receptors
Mohamed Mahameed et al.
Cell death & disease, 10(4), 300-300 (2019-04-02)
IRE1, PERK, and ATF6 are the three transducers of the mammalian canonical unfolded protein response (UPR). GSK2606414 is a potent inhibitor of PERK, while KIRA6 inhibits the kinase activity of IRE1. Both molecules are frequently used to probe the biological
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