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APY29

产品编号:4086570
规格:≥97% (HPLC)
CAS NO:1216665-49-4
包装规格:5 MG,25 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品编号包装单位单价(元)国内现货国外库存询价单
40865705 MG847
408657025 MG3270
产品别名

1216665-49-4

APY29

N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine

APY29 (type I kinase inhibitor)

N2-(1H-Benzo[d]imidazol-6-yl)-N4-(3-cyclopropyl-1H-pyrazol-5-yl)pyrimidine-2,4-diamine

APY 29

APY-29

结构式
基本信息
Empirical Formula【经验(实验)分子式】
C17H16N8
Molecular weight
332.36
MDL number
MFCD27991280
General description【一般描述】
APY29 is considered as a type I kinase inhibitor of inositol requiring kinase enzyme 1 α (IRE1α).
Biochem/physiol Actions【生化/生理作用】
APY29 is a small molecule that inhibits the kinase activity of IRE1α (in vitro autophosphorylation IC50 = 280 nM) by targeting its active site ATP-binding pocket, while simultaneously acting as an allosteric activator of IRE1α RNase activity (EC50 = 460 nM) by keeping the active site in an open conformation. When applied 1 hr prior to stress induction by 4-hr 6 nM thapsigargin treatment, APY29 significantly potentiates stress-induced unfolded protein response (UPR) in rat insulinoma INS-1 cultures (XBP1 mRNA processing induction = 54% without vs. 78% with 1-hr 3 μM APY29 pretreatment).
APY29 has the ability to enhance inositol requiring kinase enzyme 1 α (IRE1α) (P830L)′s oligomeric state to rescue RNase activity.
产品性质
Assay【测定】
≥97% (HPLC)
form【形式】
powder
color【颜色】
white to beige
solubility【溶解性】
DMSO: 2 mg/mL, clear
storage temp.【储存温度】
−20℃
SMILES string
C1(NC2=CC(C3CC3)=NN2)=CC=NC(NC4=CC=C(N=CN5)C5=C4)=N1
安全信息
Storage Class Code【储存分类代码】
13 - Non Combustible Solids
WGK
WGK 3
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