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  • PDD 00017273
  • 货号: abs821384
    CAS号: 1945950-21-9
    分子式: C23H26N6O4S2
    分子量: 514.62
    产品说明书
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    货号-规格 货期 价格 数量
    abs821384-5mg 4周 ¥4032.00
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    abs821384-25mg 4周 ¥14742.00
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    大包装询价
    产品描述
    描述
    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.
    纯度
    98%
    储存/保存方法
    store at -20℃ for one year(Powder)
    生物活性
    In vitro(体外研究)
    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. 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.
    In vivo(体内研究)
    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. 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.
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