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PDD 00017273

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Chemical Structure| 1945950-21-9 同义名 : -
CAS号 : 1945950-21-9
货号 : A631748
分子式 : C23H26N6O4S2
纯度 : 95%
分子量 : 514.62
MDL号 : MFCD30536372
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 25 mg/mL(48.58 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 PDD 00017273 is a potent inhibitor of PARG with an IC50 value of 26 nM and a Kd value of 1.45 nM[1][2].PDD 00017273 (10 μM) does not inhibit the five common cytochrome P450 enzymes. PDD 00017273 at a concentration of 30 μM moderately increases the intensity of γH2AX, and also reduces NAD/H2AX by inhibiting PARG after DNA damage. PDD 00017273 inhibits ZR-75-1 cells carrying the BRCA1 and BRCA2 wild-types, but is weakly active against MDA-MB-436 cells carrying the 5396 + 1G>A mutant BRCA1[1].At a concentration of 0.3 μM, PDD 00017273 inhibited the degradation of PAR polymers in MCF7 cells, and also reduced the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1 depleted cells. PDD 00017273 blocks replication forks and induces DNA damage that requires homologous recombination (HR) to repair[2].
实验方案
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

参考文献

[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.