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
- Cat.No. 产品名称 Information
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GC62121
Fluzoparib
氟唑帕利; SHR3162; Fuzuloparib
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity. -
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。 -
GC47693
m-Methoxybenzamide
3-甲氧基苯甲酰胺,3-MBA
A PARP inhibitor - GC47056 CAY10753 A TNKS2 inhibitor
- GC47055 CAY10749 A dual inhibitor of PARP and PI3K
- GC46900 AZ9482 A PARP inhibitor
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GC50506
Fluorescein-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。
- GC39302 PARP14 inhibitor H10 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)。
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GC45808
OUL35
NSC39047
An inhibitor of PARP10 -
GC45772
6(5H)-Phenanthridinone
6(5H)-菲啶酮
An inhibitor of PARP1 and 2 - GC37735 Tankyrase-IN-2 A TNKS1/2 inhibitor
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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。 -
GC36855
Paris saponin VII
重楼皂苷 VII; Chonglou Saponin VII
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. - GC36751 NMS-P515 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。
- GC35550 BRCA1-IN-2 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。
- GC35547 BR102375 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%。
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GC35150
5,7,4'-Trimethoxyflavone
5,7,4'-三甲氧基黄酮
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. -
GC40468
1,5-Isoquinolinediol
1,5-二羟基异喹啉,NSC 65585
An inhibitor of poly(ADP-ribose) polymerases - GC19542 GeA-69 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。
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GC10456
Fucosterol
岩皂甾醇,24-ethylidene Cholesterol
A natural phytosterol with diverse biological activities - GC19505 RK-287107 A TNKS1/2 inhibitor
- GC34195 K-756 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。
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GC34120
Niraparib R-enantiomer (MK 4827 (R-enantiomer))
MK 4827 (R-enantiomer)
Niraparib R-enantiomer (MK-4827 R-enantiomer) 是一种出色的 PARP1 抑制剂,IC50 为 2.4 nM。 -
GC34071
Pamiparib (BGB-290)
帕米帕利,BGB-290
A PARP1 and PARP2 inhibitor - GC33358 WD2000-012547 WD2000-012547是一种选择性的PARP-1抑制剂,pKi为8.221。
- GC33223 BRCA1-IN-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。
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GC32793
Rucaparib Camsylate
瑞卡帕布樟脑磺酸盐,AG014699 camsylate; PF-01367338 camsylate
A PARP1 inhibitor -
GC19264
NMS-P118
2-[1-(4,4-二氟环己基)-4-哌啶基]-6-氟-2,3-二氢-3-氧代-1H-异吲哚-4-甲酰胺
A potent and selective PARP1 inhibitor -
GC18172
E7449
E7449; 2X-121
An inhibitor of PARP1, PARP2, and TNKS1/2 -
GC11761
4-amino-1,8-Naphthalimide
4-氨基-1,8-萘二胺,4-Aminonaphthalimide,4-ANI
A PARP inhibitor -
GC16725
AZ6102
REL-2-[4-[6-[(3R,5S)-3,5-二甲基-1-哌嗪基]-4-甲基-3-吡啶基]苯基]-3,7-二氢-7-甲基-4H-吡咯并[2,3-D]嘧啶-4-酮
A TNKS1/2 inhibitor -
GC12844
Benzamide
苯甲酰胺; Benzenecarboxamide; Phenylamide
Benzamide (Benzenecarboxamide) 是一种有效的聚 (ADP-核糖) 聚合酶 (PARP) 抑制剂。 -
GC14251
Picolinamide
2-吡啶甲酰胺,2-Picolinamide
poly (ADP-ribose) synthetase inhibitor -
GC14380
BGP-15
(Z)-N-(2-羟基-3-(哌啶-1-基)丙氧基)烟酰胺双盐酸盐
A PARP inhibitor and insulin sensitizer -
GC17555
NVP-TNKS656
TNKS656
A TNKS2 inhibitor - GC16914 MN 64 A TNKS inhibitor
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GC13541
G007-LK
Tankyrase 1/2 Inhibitor VI
A TNKS1/2 inhibitor -
GC13249
Rucaparib (free base)
瑞卡帕布; AG014699; PF-01367338
A PARP1 inhibitor -
GC11537
MK-4827 tosylate
尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate
An orally bioavailable PARP1/2 inhibitor -
GC12756
MK-4827 hydrochloride
MK-4827 hydrochloride
MK-4827 hydrochloride (MK-4827 hydrochloride) 是一种高效且具有口服生物利用度的 PARP1 和 PARP2 抑制剂,IC50 分别为 3.8 和 2.1 nM。 MK-4827 hydrochloride 抑制 DNA 损伤的修复,激活细胞凋亡并显示出抗肿瘤活性。 - GC13419 ME0328 A selective PARP3 inhibitor
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GC11548
Tankyrase Inhibitors (TNKS) 49
TNKS 49;TNKS49;TNKS-49
Tankyrase inhibitor -
GC15041
Tankyrase Inhibitors (TNKS) 22
TNKS 22;TNKS22;TNKS-22
Tankyrase 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。 -
GC11674
WIKI4
Tankyrase 1/2 Inhibitor V
A potent TNKS1/2 inhibitor -
GC17775
NU 1025
NSC 696807
An inhibitor of PARP -
GC12869
JW 55
Tankyrase 1/2 Inhibitor IV
A TNKS1/2 inhibitor - GC12991 EB 47 A PARP1 and TNKS2 inhibitor
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GC12680
DR 2313
3,5,7,8-四氢-2-甲基-4H-硫代吡喃并[4,3-D]嘧啶-4-酮
A PARP inhibitor - GC14434 BYK 49187 Potent PARP-1/PARP-2 inhibitor