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)
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
Quality Level
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
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)
Polly Gravells et al.
DNA repair, 61, 25-36 (2017-11-28)
Upon DNA binding the poly(ADP-ribose) polymerase family of enzymes (PARPs) add multiple ADP-ribose subunits to themselves and other acceptor proteins. Inhibitors of PARPs have become an exciting and real prospect for monotherapy and as sensitizers to ionising radiation (IR). The
Tanay Thakar et al.
Nature communications, 11(1), 2147-2147 (2020-05-03)
Upon genotoxic stress, PCNA ubiquitination allows for replication of damaged DNA by recruiting lesion-bypass DNA polymerases. However, PCNA is also ubiquitinated during normal S-phase progression. By employing 293T and RPE1 cells deficient in PCNA ubiquitination, generated through CRISPR/Cas9 gene editing
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
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.
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