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(120)

  • 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。

  • GC62105 structure
    GC62105Senaparib
    CAS: 1401682-78-7
    纯度: >99.00%

    Senaparib (IMP4297) 是强效的、选择性的、口服有效的 PARP1/2 抑制剂。Senaparib (IMP4297) 在动物模型中表现强效的抗肿瘤活性。

  • GC62121 structure
    GC62121Fluzoparib
    CAS: 1358715-18-0
    纯度: >98.00%

    Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity.

  • GC62129 structure
    GC62129Venadaparib
    CAS: 1681017-83-3
    纯度: >98.00%

    Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells.

  • GC62154 structure
    GC62154N-Descyclopropanecarbaldehyde Olaparib
    CAS: 763111-47-3
    纯度: >99.00%

    N-Descyclopropanecarbaldehyde Olaparib 是含有 DOTA 的奥拉帕尼的类似物。Descyclopropanecarbaldehyde Olaparib 是一种 CRBN 配体，可用于合成新型靶向 EGFR 和 PARP 的双靶点 PROTAC，DP-C-4。N-Descyclopropanecarbaldehyde Olaparib 可以用 F-18 或荧光团进行放射性标记用于正电子发射断层扫描 (PET) 或几种类型的肿瘤的光学成像。

  • GC62252 structure
    GC62252Mefuparib hydrochloride
    CAS: 1449746-00-2
    纯度: >98.00%

    Mefuparib hydrochloride (MPH) 是一种具有口服活性的，底物竞争性和选择性的 PARP1/2 抑制剂，IC50 分别为 3.2 nM 和 1.9 nM。Mefuparib hydrochloride 诱导细胞凋亡 (apoptosis)，并在体内外具有显着的抗癌活性。

  • GC62275 structure
    GC62275PARP1-IN-5 dihydrochloride
    CAS: 2823308-89-8

    PARP1-IN-5 dihydrochloride 是一种低毒、具有口服活性、有效的和有选择性的 PARP-1 抑制剂(IC50 =14.7 nM)。PARP1-IN-5 dihydrochloride 可用于癌症研究。

  • GC62310 structure
    GC62310AZD5305
    CAS: 2589531-76-8
    纯度: >99.50%

    AZD5305高选择性PARP1抑制剂，通过精准靶向PARP1破坏肿瘤细胞的DNA损伤修复机制，从而诱导癌细胞死亡，AZD5305对PARP1（IC 50 =3nM）的选择性比PARP2（IC 50 =1400nM）高约500倍。