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Chemical Structure| 1945950-21-9 Chemical Structure| 1945950-21-9

Structure of PDD 00017273
CAS No.: 1945950-21-9

Chemical Structure| 1945950-21-9

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PDD00017273 is a potent and selective inhibitor of Poly(ADP-ribose) glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM. It catalyses hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, reversing the effects of poly(ADP-ribose) polymerases (PARPs). PDD 00017273 suppresses the ZR-75-1 cells carring BRCA1 and BRCA2 wild type, and exhibits less potent activities against MDA-MB-436 cells carry the 5396 + 1G>A mutation in BRCA1. It is used for specific killing of cells defective in certain homologous recombination (HR) proteins such as breast cancer gene 1/2 (BRCA1/2).

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Product Details of PDD 00017273

CAS No. :1945950-21-9
Formula : C23H26N6O4S2
M.W : 514.62
SMILES Code : O=S(C1=CC2=C(N(CC3=CC(C)=NN3C)C(N(CC4=CN=C(C)S4)C2=O)=O)C=C1)(NC5(C)CC5)=O
MDL No. :MFCD30536372

Safety of PDD 00017273

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
UMSCC6 cells 1 µM 16 h PDD00017273 significantly reduced the survival of UMSCC6 cells following high-LET proton irradiation, indicating that PARG plays a crucial role in the repair of complex DNA damage induced by high-LET protons. PMC10874437
FaDu cells 1 µM 16 h PDD00017273 significantly reduced the survival of FaDu cells following high-LET proton irradiation, indicating that PARG plays a crucial role in the repair of complex DNA damage induced by high-LET protons. PMC10874437
HeLa cells 1 µM 16 h PDD00017273 significantly reduced the survival of HeLa cells following high-LET proton irradiation, indicating that PARG plays a crucial role in the repair of complex DNA damage induced by high-LET protons. PMC10874437
HeLa cells 3 μM 6 h PDD promotes MZ1-induced degradation of BRD4 PMC11220168
HCT116 cells 3 μM 6 h PDD promotes MZ1-induced degradation of BRD4 PMC11220168
MDA-MB-231 0.3 μM 16 h PDD00017273 also showed sensitization to ionizing radiation in MDA-MB-231 cells. PMC5765821
Pancreatic cancer cells 1 µM 24 h To evaluate the effect of PDD00017273 on ZZW-115-induced cell death, it was found that PDD00017273 enhanced the cell death effect PMC9307593
MC3T3-E1 cells 1 µM 28 days PDD00017273 significantly enhanced ALP activity and promoted mineralization at day 28. PMC9103302
MC3T3-E1 cells 1 µM 24 h PDD00017273 significantly increased intracellular PAR levels, indicating inhibition of PARG enzymatic activity. PMC9103302
MCF-7 0.3 μM 16 h PDD00017273 was used to inhibit PARG activity, leading to the accumulation and persistence of PAR, thereby increasing sensitivity to ionizing radiation. PMC5765821

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.72mL

1.94mL

0.97mL

19.43mL

3.89mL

1.94mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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