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SML1781

Sigma-Aldrich

PDD00017273

≥98% (HPLC)

Synonym(e):

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

Empirische Formel (Hill-System):
C23H26N6O4S2
CAS-Nummer:
1945950-21-9
Molekulargewicht:
514.62
MDL-Nummer:
MFCD30536372
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 10 mg/mL, clear

Lagertemp.

2-8°C

Biochem./physiol. Wirkung

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).

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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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)
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
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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