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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GC40468
1,5-Isoquinolinediol
1,5-二羟基异喹啉,NSC 65585
An inhibitor of poly(ADP-ribose) polymerases -
GC62781
2-Methylquinazolin-4-ol
2-甲基-4(3H)-喹唑酮
2-Methylquinazolin-4-ol 是一种高效、竞争性的 poly(ADP-ribose) synthetase 抑制剂,其 Ki 值为 1.1 μM。2-Methylquinazolin-4-ol 是哺乳动物天冬氨酸氨基转移酶 (ATCase) 抑制剂,其 IC50 值为 0.20 mM。 -
GC62805
4’-Methoxychalcone
4'-甲氧基查尔酮
4'-Methoxychalcone, found in citrus, is chalcone derivative that has shown diverse pharmacological properties, including anti-tumor and anti-inflammatory activities. 4'-Methoxychalcone significantly enhanced adipocyte differentiation, in part, by its potent effects on PPARγ activation and by its reverse effect on TNF-α. -
GC16474
4-HQN
4-羟基喹唑啉
A heterocyclic building block -
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. -
GN10629
5,7-dihydroxychromone
5,7-二羟基色酮
A flavone decomposition product with diverse biological activities -
GC68161
5-AIQ
5-Aminoisoquinolin-1-one
5-AIQ (5-Aminoisoquinolin-1-one) 是一种水溶性的 PARP-1 抑制剂。5-AIQ 是多种药物中的一个重要官能团。5-AIQ 减少肝脏缺血再灌注相关的组织损伤,可用于肝脏缺血再灌注相关治疗条件的研究。 -
GC45772
6(5H)-Phenanthridinone
6(5H)-菲啶酮
An inhibitor of PARP1 and 2 -
GC12390
A-966492
A PARP1 and PARP2 inhibitor
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GC12422
ABT-888 (Veliparib)
维利帕尼; ABT-888
ABT-888 (Veliparib) (ABT-888) 是一种有效的 PARP 抑制剂,抑制 PARP1 和 PARP2,Kis 分别为 5.2 和 2.9 nM。
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GC16318
AG-14361
A PARP1 inhibitor
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GC73642
ALK-IN-26
ALK-IN-26是ALK抑制剂,对ALK酪氨酸激酶的IC50值为7.0 μM。
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GC70420
Amelparib
Amelparib是PARP-1的强效、口服活性和水溶性抑制剂。
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GC70421
Amelparib hydrochloride
Amelparib hydrochloride是PARP-1的强效、口服活性和水溶性抑制剂。
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GC65899
AZ3391
AZ3391 是一种有效的 PARP 抑制剂。AZ3391 是一种喹喔啉衍生物。PARP 酶家族在许多细胞过程中发挥重要作用,例如复制、重组、染色质重塑和 DNA 损伤修复。AZ3391具有研究中枢神经系统组织中发生的疾病和病症的潜力,例如大脑和脊髓 (信息摘自专利 WO2021260092A1,化合物 23)。
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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 -
GC46900
AZ9482
A PARP inhibitor
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GC73919
AZD-9574-acid
PPAR-1抑制剂AZD-9574-acid (70D)可用于合成PROTAC (CAS 2923686-70-6)。
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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 -
GC62310
AZD5305
AZD5305
AZD5305 is a highly selective and potent inhibitor of PARP1 with an IC50 of 3 nM in wild-type A549 lung cancer cells. AZD5305 shows no or minimal growth inhibitory effects in other cells (IC50s >10μM). -
GC73130
Basroparib
STP1002
Basroparib是一种具有抗肿瘤活性的强效聚ADP核糖聚合酶(PARP)抑制剂。 -
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 -
GC15932
BMN 673
他拉唑帕利; BMN-673; LT-673
A PARP 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。 -
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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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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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。
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GC10690
BYK 204165
PARP Inhibitor XIV
A selective inhibitor of PARP1 -
GC14434
BYK 49187
Potent PARP-1/PARP-2 inhibitor
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GC47055
CAY10749
A dual inhibitor of PARP and PI3K
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GC47056
CAY10753
A TNKS2 inhibitor
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GC68940
DB008
DB008 是一种有效的选择性 PARP16 抑制剂,IC50 值为 0.27 μM,含有丙烯酰胺亲电试剂。DB008 具有膜渗透性,可选择性标记 PARP16。
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GN10040
Dehydrocorydaline
脱氢紫堇碱; 13-Methylpalmatine
Dehydrocorydaline是从延胡索中分离得到的一种季铵生物碱。 -
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 -
GC64209
E7016
GPI 21016
E7016 (GPI 21016) 是一种口服有效的 PARP 抑制剂。E7016 可以通过抑制 DNA 修复来增强肿瘤细胞在体内外的放射敏感性。E7016 用作一种潜在的抗肿瘤剂。 -
GC18172
E7449
E7449; 2X-121
An inhibitor of PARP1, PARP2, and TNKS1/2 -
GC12991
EB 47
A PARP1 and TNKS2 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。
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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. -
GC10456
Fucosterol
岩皂甾醇,24-ethylidene Cholesterol
A natural phytosterol with diverse biological activities -
GC13541
G007-LK
Tankyrase 1/2 Inhibitor VI
A TNKS1/2 inhibitor -
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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GC15353
Iniparib (BSI-201)
3-硝基-4-碘苯甲酰胺,BSI201,BSI 201
A PARP1 inhibitor -
GC12496
INO-1001
3-氨基苯甲酰胺,3-aminobenzamide
A PARP inhibitor -
GC12869
JW 55
Tankyrase 1/2 Inhibitor IV
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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GC65907
KSQ-4279
USP1-IN-1
KSQ-4279 (USP1-IN-1, Formula I) 是USP1 和 PARP 的抑制剂。 -
GC47693
m-Methoxybenzamide
3-甲氧基苯甲酰胺,3-MBA
A PARP inhibitor -
GC13419
ME0328
A selective PARP3 inhibitor
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GC62252
Mefuparib hydrochloride
MPH
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。