SML1806
YU142670
≥98% (HPLC)
别名:
3-（4-吡啶基）-1,2,4-三唑[3,4-b] [1,3,4]噻二唑, 3-（吡啶-4-基）-[1,2,4]三唑[3,4-b] [1,3,4]噻二唑
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选择尺寸
关于此项目
经验公式（希尔记法）:
C8H5N5S
化学文摘社编号:
分子量:
203.22
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
YU142670, ≥98% (HPLC)
InChI key
HRBYAJQMVADJHW-UHFFFAOYSA-N
SMILES string
C12=NN=C(C3=CC=NC=C3)N1N=CS2
assay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
相关类别
Biochem/physiol Actions
选择性 OCRL1/INPP5F 和 OCRL2/INPP5B 抑制剂，导致细胞 PI（4,5）P2 积累和自噬小体-溶酶体融合缺陷。
通过靶向 OCRL 催化域，YU142670 是 OCRL1/INPP5F（IC50 = 0.71 μM；底物为 PI（4,5）P2）和 OCRL2/INPP5B（IC50 = 0.53 和 1.78 μM；底物分别为 PI3 和 INPP5B/PI（4,5）P2））的选择性抑制剂，而不影响 INPP5A、INPP5E、PTEN、SHP1，虾碱性磷酸酶、鞘磷脂酶或 SYNJ1。YU142670 导致人皮肤成纤维细胞中 PI（4,5）P2/PI4P 比率增加（增加 50％；50μM 持续 1 h），并诱导质膜上肌动蛋白成核和皱纹活性上调，而没有明显的细胞毒性。与 PtdIns（4,5）P2 对控制自噬体溶酶体融合的钙通道黏蛋白 1（MCOLN1）的负调节作用相一致，在使用 YU142670（25 μM 持续 3 小时）或 OCRL shRNA 处理的人肾近端肾小管细胞（PTC）中观察到了自噬体积累增强。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Michelle Pirruccello et al.
ACS chemical biology, 9(6), 1359-1368 (2014-04-20)
Phosphoinositides are low abundance membrane phospholipids that have key roles in signaling, membrane trafficking, and cytoskeletal dynamics in all cells. Until recently, strategies for robust and quantitative development of pharmacological tools for manipulating phosphoinositide levels have focused selectively on PI(3,4,5)P3
Stephen J Mills et al.
Biochemistry, 55(9), 1384-1397 (2016-02-09)
The inositol polyphosphate 5-phosphatase INPP5B hydrolyzes the 5-phosphate group from water- and lipid-soluble signaling messengers. Two synthetic benzene and biphenyl polyphosphates (BzP/BiPhPs), simplified surrogates of inositol phosphates and phospholipid headgroups, were identified by thermodynamic studies as potent INPP5B ligands. The
Autophagosome-lysosome fusion triggers a lysosomal response mediated by TLR9 and controlled by OCRL.
Maria Giovanna De Leo et al.
Nature cell biology, 18(8), 839-850 (2016-07-12)
Phosphoinositides (PtdIns) control fundamental cell processes, and inherited defects of PtdIns kinases or phosphatases cause severe human diseases, including Lowe syndrome due to mutations in OCRL, which encodes a PtdIns(4,5)P2 5-phosphatase. Here we unveil a lysosomal response to the arrival
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