GlpBio

PARP

PARP(多聚ADP核糖聚合酶)

Poly (ADP-ribose) polymerases (PARPs) is a large family of proteins with a conserved catalytic domain that catalyze an immediate DNA-damage-dependent post-translational modification of histones and other nuclear proteins leading to the survival of injured proliferating cells. So far, a total number of 18 human PARP proteins encoded by different genes have been identified, including PARP-1 to PARP-4, PARP-5a, PARP-5b, PARP-5c and PARP-6 to PARP-16. The general structural of PARP proteins has been revealed through the extensive study of the founding family member PARP-1, which is characterized by the presence of four functional domains, including a DNA-binding domain, a caspase-cleaved domain, an automodification domain and a catalytic domain.

PARP 相关产品(118)

  • GC19505 structure
    GC19505RK-287107
    CAS: 2171386-10-8
    纯度: >99.50%

    A TNKS1/2 inhibitor

  • GC19542 structure
    GC19542GeA-69
    CAS: 2143475-98-1
    纯度: >99.50%

    GeA-69 是一种多聚腺苷二磷酸核糖聚合酶 14 (PARP14) 的选择性变构抑制剂，靶向大结构域 2 (MD2)，Kd 值为 2.1 µM。 GeA-69 参与 DNA 损伤修复机制并阻止 PARP14 MD2 募集到激光诱导的 DNA 损伤部位。

  • GC32793 structure
    GC32793Rucaparib Camsylate
    CAS: 1859053-21-6
    纯度: >99.50%

    A PARP1 inhibitor

  • GC33223 structure
    GC33223BRCA1-IN-1
    CAS: 1622262-74-1

    BRCA1-IN-1是一种新型的小分子BRCA1抑制剂，IC50和Ki分别为0.53μM和0.71μM。

  • GC33358 structure
    GC33358WD2000-012547
    CAS: 283172-68-9

    WD2000-012547是一种选择性的PARP-1抑制剂，pKi为8.221。

  • GC34071 structure
    GC34071Pamiparib (BGB-290)
    CAS: 1446261-44-4
    纯度: >99.50%

    Pamiparib (BGB-290)是一种强效口服的聚腺苷二磷酸核糖聚合酶（PARP）抑制剂，对PARP-1和PARP-2的IC 50 值分别为1.3nM和0.9nM。

  • GC34120 structure
    GC34120Niraparib R-enantiomer (MK 4827 (R-enantiomer))
    CAS: 1038915-58-0
    纯度: >99.50%

    Niraparib R-enantiomer (MK-4827 R-enantiomer) 是一种出色的 PARP1 抑制剂，IC50 为 2.4 nM。

  • GC34195 structure
    GC34195K-756
    CAS: 130017-40-2
    纯度: >99.00%

    K-756是一种直接的选择性tankyrase(TNKS)抑制剂，抑制TNKS1和TNKS2的ADP-核糖基化活性，IC50分别为31和36nM。

  • GC35150 structure
    GC351505,7,4'-Trimethoxyflavone
    CAS: 5631-70-9
    纯度: >99.50%

    4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.

  • GC35547 structure
    GC35547BR102375
    CAS: 2366255-59-4

    BR102375 是一种用于治疗 2 型糖尿病的 non-TZD (噻唑烷二酮类) PPAR γ 完全激动剂， 其 EC50 值和 Amax比率值分别为 0.28 μM 和 98%。

  • GC35550 structure
    GC35550BRCA1-IN-2
    CAS: 1622262-55-8
    纯度: >98.00%

    BRCA1-IN-2 (compound 15) 是具有细胞渗透性的 BRCA1 蛋白-蛋白相互作用 (PPI) 的抑制剂，IC50 值 0.31 μM，Kd 值为 0.3 μM， BRCA1-IN-2 通过阻断 BRCA1 (BRCT)2/ 蛋白质相互作用而具有抗肿瘤活性。

  • GC36751 structure
    GC36751NMS-P515
    CAS: 1262395-13-0

    NMS-P515 是有效的、口服有效的、立体定向的PARP-1 的抑制剂，Kd 值为16 nM，IC50 值为 27 nM (Hela 细胞中)。有抗肿瘤活性。

  • GC36855 structure
    GC36855Paris saponin VII
    CAS: 68124-04-9
    纯度: >98.00% / >98.50%

    Chonglou Saponin VII (Dioscinin, Polyphyllin-VII, Paris saponin-VII), a kind of steroidal saponins from Chonglou (Rhizoma Paridis Chonglou), inhibits EMT and reduces the invasion of ovarian cancer cells via the GSK-3β/β-catenin signaling pathway.

  • GC37728 structure
    GC37728Talazoparib tosylate
    CAS: 1373431-65-2
    纯度: >99.50%

    Talazoparib tosylate（BMN 673ts）是一种有效的具有口服活性的PARP1/2抑制剂，是Talazoparib的甲苯磺酸盐形式。Talazoparib抑制PARP1的IC 50 值为0.57nM。

  • GC37735 structure
    GC37735Tankyrase-IN-2
    CAS: 1588870-36-3
    纯度: >99.50%

    A TNKS1/2 inhibitor

  • GC39302 structure
    GC39302PARP14 inhibitor H10
    CAS: 2084811-68-5
    纯度: >98.00%

    PARP14 inhibitor H10 (化合物 H10) 是针对 PARP14 的选择性抑制剂 (IC50=490 nM)，是其他 PARP 的抑制剂 (约为 PARP1 的 24 倍)。PARP14 抑制剂 H10 诱导 caspase-3/7 介导的细胞凋亡 (apoptosis)。

  • GC40468 structure
    GC404681,5-Isoquinolinediol
    CAS: 5154-02-9
    纯度: >99.00%

    An inhibitor of poly(ADP-ribose) polymerases

  • GC45772 structure
    GC457726(5H)-Phenanthridinone
    CAS: 1015-89-0
    纯度: >98.00%

    An inhibitor of PARP1 and 2

  • GC45808 structure
    GC45808OUL35
    CAS: 6336-34-1
    纯度: >99.00%

    An inhibitor of PARP10

  • GC46900 structure
    GC46900AZ9482
    CAS: 1825345-33-2
    纯度: >98.00%

    A PARP inhibitor

  • GC47055 structure
    GC47055CAY10749
    CAS: 2337386-47-5
    纯度: >98.00%

    A dual inhibitor of PARP and PI3K

  • GC47056 structure
    GC47056CAY10753
    纯度: >98.00%

    A TNKS2 inhibitor

  • GC47693 structure
    GC47693m-Methoxybenzamide
    CAS: 5813-86-5
    纯度: >98.00%

    A PARP inhibitor

  • GC50506 structure
    GC50506Fluorescein-NAD+

    荧光素-NAD+ 是放射性标记的 NAD 的替代品，也是 ADP 核糖基化的底物。