1. Cell Cycle/DNA Damage
  2. IRE1
  3. APY29

APY29 

目录号: HY-17537 纯度: 99.54%
产品使用指南

APY29 是 ATP 竞争性抑制剂,一种特异性的 IRE1α 别构调节剂,通过结合到 ATP 结合口袋来抑制 IRE1α 的自主磷酸化,IC50 值为 280 nM。APY29 也可以变构激活 IRE1α 相邻 RNase 域。

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APY29 Chemical Structure

APY29 Chemical Structure

CAS No. : 1216665-49-4

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

Size Price Stock Quantity
10 mM * 1  mL in DMSO ¥1535 In-stock
10 mg ¥1395 In-stock
50 mg ¥6045 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

    APY29 purchased from MCE. Usage Cited in: Food Chem Toxicol. 2018 Feb 10;114:52-60.

    (A) The p-IRE1a, IRE1a and XBP1s protein expression levels were determined in rat livers. (B, C, D) The expression of p-IRE1a, IRE1a, XBP1s, MTTP and p65 were detected in cells (n=3). A: APY-29; A+Q: APY-29+Quercetin; A+S: APY-29+STF-083010.

    APY29 purchased from MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    IRE1 kinase activity inhibitor represses JNK activation induced by viral infection in HEC-1-A cells. HEC-1-A cells were pretreated or mock-pretreated with APY29, only or both APY29, and STF-083010 for 30 min and then infected or mock-infected with HSV-1.

    APY29 purchased from MCE. Usage Cited in: Viruses. 2017 Aug 23;9(9). pii: E235. 

    Inhibition of IRE1 kinase activity has an inhibitory effect on HSV-1 replication in HEC-1-A cells. Cells are presence or absence of APY29 or STF-083010 or both of two drugs and then infected with HSV-1 (HF). Total cellular cells lysates are prepared at 24 h p.i. and subject to Western blot analysis against.

    APY29 purchased from MCE. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.

    Immunocytochemistry for expression of β III tubulin showing reduces expression in IRE1α knockdown cells in the presence of kaempferol and APY29.

    APY29 purchased from MCE. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.

    STF083010 pretreatment reduces the number of neurite bearing cells in both kaempferol (KFL) and APY29 treated conditions further.

    APY29 purchased from MCE. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.

    Immunocytochemistry for expression of β III tubulin showing reduces expression upon pretreatment of cells with STF083010 50 μM in the presence of kaempferol and APY29.

    APY29 purchased from MCE. Usage Cited in: FEBS J. 2019 Apr;286(7):1375-1392.

    Western blot analysis shows the increase in expression of neuronal marker proteins NSE and NDRG1 with increased XBP1s levels in kaempferol and APY29 treated conditions.
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    • 参考文献

    Description

    APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain[1].

    IC50 & Target

    IC50: 280 nM (IRE1α)

    In Vitro

    APY29 divergently modulates the RNase activity and oligomerization state of IRE1α. APY29 is exerting their opposing effects on RNase activity through the same binding site. APY29 divergently affects IRE1α oligomerization. APY29 demonstrates opposing dose-dependent effects on ER stress-induced activation of the RNase of endogenous IRE1α[1].

    Molecular Weight

    332.36

    Formula

    C₁₇H₁₆N₈

    CAS No.

    1216665-49-4

    SMILES

    C1(NC2=CC=C3N=CNC3=C2)=NC=CC(NC4=NNC(C5CC5)=C4)=N1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (300.88 mM)

    H2O : 5 mg/mL (15.04 mM; ultrasonic and adjust pH to 3 with HCl)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0088 mL 15.0439 mL 30.0879 mL
    5 mM 0.6018 mL 3.0088 mL 6.0176 mL
    10 mM 0.3009 mL 1.5044 mL 3.0088 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (7.52 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (7.52 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (7.52 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    References

    Purity: 99.54%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    APY29APY 29APY-29IRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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    产品名称:
    APY29
    目录号:
    HY-17537
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