PDD00017272

CAT: 0804-HY-133531-01Size: 5 mgDry Ice: NoHazardous: No

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CAT#:0804-HY-133531-01Size:5 mg

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Description

PDD00017272 is an inhibitor of poly (ADP-ribose) glycohydrolase (PARG) (EC50=4.8 nM) and an activator of PARP1/2. PDD00017272 inhibits its activity of hydrolyzing poly (ADP-ribose) (pADPr), resulting in the accumulation of pADPr on chromatin, interfering with DNA damage repair and replication processes, and inducing PARP1/2-dependent cytotoxicity. PDD00017272 can be used in cancer models with DNA repair defects (such as BRCA mutations) or resistance to PARP inhibitors. PDD00017272 has a PARG expression level-correlated inhibitory potency with EC50 of 9.2 nM (PARG cells), the tumor cells with lower PARG expression are more sensitive[1][2].

CAS Number

1945950-20-8

UNSPSC

12352005

Target

Poly (ADP-ribose) Glycohydrolase (PARG)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pdd00017272.html

Concentration

10mM

Purity

99.47

Solubility

DMSO : ≥ 25 mg/mL

Smiles

O=S(C1=CC2=C(N(CC3=C(C)N=C(C)S3)C(N(CC4=CN=C(C)S4)C2=O)=O)C=C1)(NC5(C)CC5)=O

Molecular Formula

C23H25N5O4S3

Molecular Weight

531.67

References & Citations

[1]Nie L, et al. DePARylation is critical for S phase progression and cell survival. Elife. 2024 Apr 5;12:RP89303.|[2]Bohdan Waszkowycz, et al. Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly (ADP-ribose) Glycohydrolase (PARG) : Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides. J Med Chem. 2018 Dec 13;61 (23) :10767-10792.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

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