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[CAS NO. 1945950-21-9] PDD 00017273
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-108360 |
| Brand: | MCE |
| CAS: | 1945950-21-9 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 514.62 |
| Molecular Formula | C23H26N6O4S2 |
| 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 |
5 Publications Citing Use of MCE
Summary
PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase ( PARG ), with an IC 50 of 26 nM, and a K D of 1.45 nM [1] [2] .
In Vitro
PDD 00017273 is a potent inhibitor of PARG, with an IC 50 of 26 nM, and a K D 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 48.58 mM ; ultrasonic and warming and heat to 60°C)
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 |
References
- [1] James DI, et al. First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to AZD2281. ACS Chem Biol. 2016 Nov 18;11(11):3179-3190. Epub 2016 Oct 12.
- [2] Gravells P, et al. Specific killing of DNA damage-response deficient cells with inhibitors of poly(ADP-ribose) glycohydrolase. DNA Repair (Amst). 2017 Apr;52:81-91.
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