Merck
CN

SML1781

Sigma-Aldrich

PDD00017273

≥98% (HPLC)

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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
Empirical Formula (Hill Notation):
C23H26N6O4S2
分子量:
514.62
MDL编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to beige

溶解性

DMSO: 10 mg/mL, clear

储存温度

2-8°C

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此商品
SML1061PZ0379SML1984
PDD00017273 ≥98% (HPLC)

Sigma-Aldrich

SML1781

PDD00017273

PF-04856264 ≥98% (HPLC)

Sigma-Aldrich

SML1061

PF-04856264

PF-04827736 ≥98% (HPLC)

Sigma-Aldrich

PZ0379

PF-04827736

GSK9311 ≥98% (HPLC)

Sigma-Aldrich

SML1984

GSK9311

form

powder

form

powder

form

powder

form

powder

color

white to beige

color

white to light brown

color

white to beige

color

white to beige

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 10 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

room temp

storage temp.

−20°C

Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

-

生化/生理作用

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。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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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
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
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
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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