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SML1781

Sigma-Aldrich

PDD00017273

≥98% (HPLC), powder, poly(ADP-ribose) glycohydrolase inhibitor

Sinónimos:

1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide

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About This Item

Fórmula empírica (notación de Hill):
C23H26N6O4S2
Número de CAS:
1945950-21-9
Peso molecular:
514.62
MDL number:
MFCD30536372
UNSPSC Code:
12352200
NACRES:
NA.77

product name

PDD00017273, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

PDD00017273 is a potent and selective inhibitor of Poly(ADP-ribose) glycohydrolase (PARG), which catalyses hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, reversing the effects of poly(ADP-ribose) polymerases (PARPs). PARG has been shown to be involved in the repair of single strand DNA breaks. PDD00017273 is selective for PARG, with EC50 = 26 nM, compared to values of 30 μM for PARP1 and ARH3.
PDD00017273 is cell permeable in nature. It is used for specific killing of cells defective in certain homologous recombination (HR) proteins such as breast cancer gene 1/2 (BRCA1/2).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

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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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