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
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%。
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。
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。
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。
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
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
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
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
GC17052 MK-4827 Racemate selective inhibitor of PARP1/PARP2
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
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
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
GC10690 BYK 204165
PARP Inhibitor XIV
A selective inhibitor of PARP1
GC16474 4-HQN
4-羟基喹唑啉
A heterocyclic building block
GC17783 Veliparib dihydrochloride
维利帕尼二盐酸盐; ABT-888 dihydrochloride
An orally bioavailable inhibitor of PARP1 and PARP2
GC10995 PJ34
PJ-34;PJ 34
An inhibitor of poly (ADP-ribose) polymerases
GC17802 MK-4827
尼拉帕尼; MK-4827
An orally bioavailable PARP1/2 inhibitor
GC10920 BMN-673 8R,9S
他拉唑帕利 (8R,9S); (8R,9S)-BMN-673; (8R,9S)-LT-673
BMN-673 8R,9S ((8R,9S)-BMN-673) 是 Talazoparib 的对映异构体。 BMN-673 8R,9S 是一种 PARP1 抑制剂，IC50 为 144 nM。
GC17965 AZD2461
4-[4-氟-3-[(4-甲氧基哌啶-1-基)羰基]苄基]酞嗪-1(2H)-酮
A PARP inhibitor
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
GC12496 INO-1001
3-氨基苯甲酰胺,3-aminobenzamide
A PARP inhibitor
GC12390 A-966492 A PARP1 and PARP2 inhibitor
GC10145 PJ34 hydrochloride
PJ 34 Hydrochloride
An inhibitor of poly (ADP-ribose) polymerases
GC16318 AG-14361 A PARP1 inhibitor
GC15353 Iniparib (BSI-201)
3-硝基-4-碘苯甲酰胺,BSI201,BSI 201
A PARP1 inhibitor
GC15955 Rucaparib (AG–014699,PF–01367338) phosphate
瑞卡帕布磷酸盐; AG-014699 phosphate; PF-01367338 phosphate
A PARP1 inhibitor
GC17580 Olaparib (AZD2281, Ku-0059436)
奥拉帕尼; AZD2281; KU0059436
Olaparib (AZD2281, Ku-0059436) 是一种有效的选择性 PARP 抑制剂，特异性靶向 PARP1 和 PARP2（IC 50 分别 = 5 nM 和 1 nM）。
GC15932 BMN 673
他拉唑帕利; BMN-673; LT-673
A PARP inhibitor