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PDD 00017273 

Cat. No.: HY-108360 Purity: >98.0%
Handling Instructions

PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM.

For research use only. We do not sell to patients.

PDD 00017273 Chemical Structure

PDD 00017273 Chemical Structure

CAS No. : 1945950-21-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 215 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 340 In-stock
Estimated Time of Arrival: December 31
25 mg USD 690 Get quote
50 mg   Get quote  
100 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a KD of 1.45 nM.

IC50 & Target

IC50: 26 nM (PARG)[1]
KD: 1.45 nM (PARG)[1]

In Vitro

PDD 00017273 is a potent inhibitor of PARG, with an IC50 of 26 nM, and a KD of 1.45 nM. PDD 00017273 (10 μM) does not inhibit five common Cytochrome P450 enzymes. PDD 00017273 (30 μM) modestly increasess phosphorylated H2AX (γH2AX) intensity, PDD 00017273 also decreases in NAD/H through PARG inhibition after DNA damage. 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[1]. PDD 00017273 (0.3 μM) inhibits degradation of PAR polymers in MCF7 cells. PDD 00017273 (0.3 μM) also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1 depleted cells. PDD 00017273 stalls replication forks and induces DNA damage that requires homologous recombination (HR) for repair[2].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9432 mL 9.7159 mL 19.4318 mL
5 mM 0.3886 mL 1.9432 mL 3.8864 mL
10 mM 0.1943 mL 0.9716 mL 1.9432 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Briefly, PARG in vitro assays are conducted in a total volume of 15 μL in a standard 384-well format. A total of 5 μL of human full length PARG used at a final reaction concentration of 65 pM, is added to 5 μL of Bt-NAD ribosylated PARP1 substrate at a final reaction concentration of 4.8 nM in assay buffer (50 mM Tris pH 7.4, 0.1 mg/mL BSA, 3 mM EDTA, 0.4 mM EGTA, 1 mM DTT, 0.01% Tween 20, 50 mM KCl). The reaction is incubated at RT for 10 min, and then 5 μL of detection reagent is added. Detection reagent consists of 42 nM mAb anti-6HIS XL665 and 2.25 nM streptavidin europium cryptate, both at 3× working stock concentrations (final concentrations of 14 nM and 0.75 nM, respectively), in detection buffer (50 mM Tris pH 7.4, 0.1 mg/mL BSA and 100 mM KF). Following incubation at RT for 60 min in the dark, TR-FRET signal is measured at λEx 340 nm and λEm 665 nm and λEm 620 nm using a PHERAstar FS plate reader. The ratio is calculated as [Em665/EM620] × 104 for each well and used to calculate percent inhibition for test compounds[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

HeLa cells are seeded in 30 μL of media at 1 × 104 cells/mL in Greiner 384-well plates. A total of 16-24 h later, cells are treated with inhibitors (8 pt dose response, 0.01-30 μM, triplicates) or vehicle (DMSO) control. The outer wells are left undosed to account for edge effects. After 72 h, 50 μL of 3.7% formaldehyde/PBS is added to each well, and cells are fixed for 20 min. Cells are then rinsed twice with PBS and stained for 1 h with Hoechst 33342/PBS (1:2000) in the dark. After two further rinses with PBS, images are captured and nuclei counted on a CellInsight. The maximum number of fields are captured from each triplicate well, which approximated to at least 1000 nuclei in vehicle-dosed wells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

514.62

Formula

C₂₃H₂₆N₆O₄S₂

CAS No.

1945950-21-9

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
PDD 00017273
Cat. No.:
HY-108360
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PDD 00017273

Cat. No.: HY-108360