412512
4μ8C
≥95% (HPLC), selective inhibitor of IRE1α, powder
别名:
IRE1抑制剂 III, 4μ8C
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关于此项目
经验公式（希尔记法）:
C11H8O4
化学文摘社编号:
分子量:
204.18
UNSPSC Code:
12352200
NACRES:
NA.28
MDL number:
Assay:
≥95% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
产品名称
IRE1抑制剂 III, 4μ8C, IRE1 Inhibitor III, CAS 14003-96-4, is a cell-permeable. Covalent inhibitor of IRE1 RNase activity (IC50 = 550 and 45 nM, respectively, with 0 & 16 min preincubation in RNA cleavage assays).
Quality Level
assay
≥95% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 25 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
O=C(C=C1C)OC2=C1C=CC(O)=C2C=O
InChI
1S/C11H8O4/c1-6-4-10(14)15-11-7(6)2-3-9(13)8(11)5-12/h2-5,13H,1H3
InChI key
RTHHSXOVIJWFQP-UHFFFAOYSA-N
General description
一种细胞可渗透的香豆素邻羟基醛化合物，通过席夫碱的形成共价靶向IRE1 Lys907，以时间和剂量依赖性方式抑制IRE1 RNase活性（在基于FRET的RNA裂解试验中进行0、2、4、8、16分钟的药物预孵育，IC50分别为550、230、180、100和45 nM），可有效防止ER应激诱导的位点特异性mRNA剪接以及衣霉素（目录号654380）治疗后MEF培养物中RIDD（受调节的IRE1依赖性降解）mRNA降解（针对Xbp1剪接和Scara3降解，IC50分别为6.9和4.1 µM）。还证明可抑制大鼠AR42J肿瘤胰腺腺泡细胞给药后的ER扩张（有效浓度为32 µM）和淀粉酶分泌(IC50<2 µM) upon stress induction by Dexamethasone (Cat. No. 265005)。结构分析表明，IRE1天然构象中水对Lys907的可及性降低，这说明了Lys907席夫碱形成的异常稳定性，并形成了4μ8C和STF083010（目录编号412510）选择性抑制IRE1 RNase的基础。尽管在没有ADP的情况下，4μ8C（而非STF083010）也显示出通过与IRE1 Lys599形成席夫碱来抑制IRE1自磷酸化，但细胞核苷酸阻止4μ8C靶向IRE1 Lys599并在细胞内抑制IRE1激酶活性。
一种细胞可渗透的香豆素邻羟基醛，通过席夫碱的形成共价靶向IRE1 Lys907，以时间和剂量依赖性方式抑制IRE1 RNase活性（在RNA裂解试验中进行0和16分钟的药物预孵育，IC50分别为550和45 nM），可有效防止ER应激诱导的位点特异性mRNA剪接以及衣霉素（目录号654380）治疗后MEF培养物中RIDD（受调节的IRE1依赖性降解）mRNA降解（针对Xbp1剪接和Scara3降解，IC50分别为6.9和4.1 µM）。与STF083010（目录编号412510）相比，在无细胞测定中，4μ8C还显示出在不存在ADP的情况下通过与IRE1 Lys599形成席夫碱来抑制IRE1自磷酸化，但是细胞核苷酸阻止4μ8C在细胞内靶向IRE1 Lys599。
Biochem/physiol Actions
主要靶标
IRE1
IRE1
可逆性：是
细胞可渗透性：是
Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻保存（-20°C）。储备液可稳定保存6个月。
Other Notes
Cross, B.C.S., et al. 2012.Proc.Natl. acad.Sci. USA109, E869.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
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存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Rohit B Sharma et al.
The Journal of biological chemistry, 295(41), 14164-14177 (2020-08-14)
Success or failure of pancreatic beta cell adaptation to ER stress is a determinant of diabetes susceptibility. The ATF6 and IRE1/XBP1 pathways are separate ER stress-response effectors important to beta cell health and function. ATF6α. and XBP1 direct overlapping transcriptional
José P Guirao-Abad et al.
mSphere, 5(5) (2020-10-23)
The unfolded protein response (UPR) is a signaling network that maintains homeostasis of the endoplasmic reticulum (ER). In the human-pathogenic fungus Aspergillus fumigatus, the UPR is initiated by activation of an endoribonuclease (RNase) domain in the ER transmembrane stress sensor
Robert Thomas Schinzel et al.
Cell, 179(6), 1306-1318 (2019-11-26)
Cells have evolved complex mechanisms to maintain protein homeostasis, such as the UPRER, which are strongly associated with several diseases and the aging process. We performed a whole-genome CRISPR-based knockout (KO) screen to identify genes important for cells to survive
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| 412512-25MG | 04055977188189 |