SML1781
PDD00017273
≥98% (HPLC), powder, poly(ADP-ribose) glycohydrolase inhibitor
别名:
1-[（1,3-二甲基-1H-吡唑-5-基）甲基] -1,2,3,4-四氢-N-（1-甲基环丙基）-3-[（2-甲基-5-噻唑基]甲基] -2,4-二氧代-6-喹唑啉磺酰胺
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关于此项目
经验公式（希尔记法）:
C23H26N6O4S2
化学文摘社编号:
分子量:
514.62
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
PDD00017273, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
SMILES string
[S](=O)(=O)(NC5(CC5)C)c1cc2c([n]([c]([n]([c]2=O)Cc4[s]c(nc4)C)=O)Cc3[n](nc(c3)C)C)cc1
InChI key
IFWUBRBMMNTBRZ-UHFFFAOYSA-N
Biochem/physiol Actions
PDD00017273 是聚（ADP-核糖）糖水解酶（PARG）的高效和选择性抑制剂，可抑制 ADP-核糖聚合物的 O-糖苷键的水解。
PDD00017273 是聚（ADP-核糖）糖水解酶（PARG）的高效和选择性抑制剂，可抑制 ADP-核糖聚合物的 O-糖苷键的水解。 经证明 PARG 参与单链 DNA 断裂的修复。 PDD00017273 对 PARG 具有选择性，EC50 = 26 nM，相较而言，对 PARP1 和 ARH3 的值为 30 μM
PDD00017273 本质上是细胞可透过性的。它用于特异性杀死某些同源重组（HR）蛋白（例如乳腺癌基因 1/2（BRCA1/2））中有缺陷的细胞。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Dominic I James et al.
ACS chemical biology, 11(11), 3179-3190 (2016-10-01)
The enzyme poly(ADP-ribose) glycohydrolase (PARG) performs a critical role in the repair of DNA single strand breaks (SSBs). However, a detailed understanding of its mechanism of action has been hampered by a lack of credible, cell-active chemical probes. Herein, we
Radiosensitization with an inhibitor of poly (ADP-ribose) glycohydrolase: A comparison with the PARP1/2/3 inhibitor olaparib.
Gravells P, et al.
DNA Repair, 61, 25-36 (2018)
Evgeniia Prokhorova et al.
Molecular cell, 81(12), 2640-2655 (2021-05-22)
ARH3/ADPRHL2 and PARG are the primary enzymes reversing ADP-ribosylation in vertebrates, yet their functions in vivo remain unclear. ARH3 is the only hydrolase able to remove serine-linked mono(ADP-ribose) (MAR) but is much less efficient than PARG against poly(ADP-ribose) (PAR) chains in vitro.
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML1781-25MG | 04061832275468 |
| SML1781-5MG | 04061832275475 |