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.

Products for PARP

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Cat.No. 产品名称 Information
GC62105 Senaparib

IMP4297
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。
GC67962 Simmiparib Simmiparib 是一种高效且具有口服活性的 PARP1 和 PARP2 抑制剂，IC50 分别为 1.75 nM 和 0.22 nM。Simmiparib 对 PARP1/2 的抑制作用强于其母体化合物 Olaparib 。在同源重组修复 (HR) 缺陷细胞中，Simmiparib 诱导 DNA 双链断裂 (DSB) 积累和 G2/M 阻滞，从而诱导细胞凋亡 (apoptosis)。Simmiparib 在细胞和裸鼠移植瘤模型中都表现出显著的抗癌活性。
GC69907 SK-575 SK-575 是一种高效、特异的蛋白水解靶向嵌合体 (PROTAC) 的 PARP1 降解剂，其 IC50 为2.30 nM。SK-575 能有效抑制携带 BRCA1/2 突变的癌细胞的生长。
GC37728 Talazoparib tosylate

BMN 673ts
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IC₅₀值为0.57nM。
GC15041 Tankyrase Inhibitors (TNKS) 22

TNKS 22;TNKS22;TNKS-22
Tankyrase inhibitor
GC11548 Tankyrase Inhibitors (TNKS) 49

TNKS 49;TNKS49;TNKS-49
Tankyrase inhibitor
GC37735 Tankyrase-IN-2 A TNKS1/2 inhibitor
GC71552 TNKS-2-IN-1 TNKS-2-IN-1（化合物13g）是TNKS-2抑制剂。
GC73633 TNKS-2-IN-2 TNKS-2-IN-2是一种有效的选择性TNKS2抑制剂，IC50为22 nM。
GC73760 Trilexium

TRX-E-009-1
Trilexium (TRX-E-009-1)是与TRX-E-002-1结构相关的第三代苯并吡喃。
GC14509 UPF 1069

5-(2-氧代-2-苯基乙氧基)-1(2H)-异喹啉酮,UPF-1069,UPF1069
A selective PARP2 inhibitors
GC17783 Veliparib dihydrochloride

维利帕尼二盐酸盐; ABT-888 dihydrochloride
An orally bioavailable inhibitor of PARP1 and PARP2
GC62129 Venadaparib

IDX-1197
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.
GC73136 VPC-70063 VPC-70063是一种强效的Myc-Max抑制剂，抑制Myc-Max转录活性的IC50值为8.9μM。
GC33358 WD2000-012547 WD2000-012547是一种选择性的PARP-1抑制剂，pKi为8.221。
GC11674 WIKI4

Tankyrase 1/2 Inhibitor V
A potent TNKS1/2 inhibitor
GC12781 XAV-939

3,5,7,8-四氢-2-[4-(三氟甲基)苯基]-4H-噻喃并[4,3-D]嘧啶-4-酮
XAV-939 选择性抑制 β-连环蛋白介导的转录。
GC91435 YCH1899 YCH1899是一种聚(ADP-核糖)聚合酶1(PARP1)和PARP2的抑制剂(IC50s = 1)，它选择性地作用于PARP1和PARP2，而不影响PARP3、-4、-5A、-5B、-6、-7、-10和-12 (IC50s = 1 -14.1 nM)。