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DNA Damage /
PARP

PARP

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TC-E 5001

Catalog No. A11454
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TNKS 抑制剂

TC-E 5001是双重tankyrase（TNKS）抑制剂（TNKS1和TNKS2的Kd值分别为79和28 nM，TNKS2的IC50 = 33 nM），在PARP1和PARP2上没有活性（IC50> 19 uM）。抑制Wnt信号并稳定Axin2水平。了解更多

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Pamiparib

Catalog No. A17073
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PARP 抑制剂

Pamiparib也称为BGB-290，是一种高效的，选择性的PARP抑制剂，具有良好的药物代谢和药代动力学特性。了解更多

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AIM-100

Catalog No. A14986
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Ack1 (TNK2) 抑制剂

AIM-100是Ack1的小分子抑制剂，IC50为24 nM。了解更多

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XMD8-87

Catalog No. A17134
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TNK2 抑制剂

XMD8-87是酪氨酸激酶非受体2（TNK2）抑制剂，IC50值为1.9μM。了解更多

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WIKI4

Catalog No. A14283
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Tankyrase 抑制剂

WIKI4是一种新型的Tankyrase抑制剂，对TNKS2的IC50为15 nM。了解更多

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- 最新产品
XMD16-5

Catalog No. A17130
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TNK2 抑制剂

XMD16-5是酪氨酸激酶非受体2（TNK2）抑制剂。了解更多

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Rucaparib (Camsylate)

Catalog No. A18013
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PARP 抑制剂

Rucaparib Camsylate is an inhibitor of PARP with a Ki of 1.4 nM for PARP1, and also shows binding affinity to eight other PARP domains. 了解更多

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NMS-P515

Catalog No. A18449
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PARP-1 抑制剂

NMS-P515 is a potent inhibitor of PARP-1 both in biochemical (Kd: 0.016 μM) and cellular (IC50: 0.027 μM) assays. 了解更多

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PARP14 inhibitor H10

Catalog No. A18616
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PARP14 抑制剂

PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (??24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis. 了解更多

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Niraparib tosylate

Catalog No. A16618
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PARP1/PARP2 inhibitor

Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. 了解更多

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- Laurie B Schenkel, .et al. A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants, Cell Chem Biol, 2021, Mar 2;S2451-9456(21)00095-7 PMID: 33705687
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Niraparib hydrochloride

Catalog No. A18018
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PARP1 and PARP2 inhibitor

Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. 了解更多

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E7449

Catalog No. A21553
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PARP1/PARP2 inhibitor

E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ?50 and ?50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD+ as substrate. 了解更多

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Niraparib R-enantiomer

Catalog No. A21880
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PARP1 inhibitor

Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM. 了解更多

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Veliparib dihydrochloride

Catalog No. A21356
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PARP inhibitor

Veliparib dihydrochloride is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively. 了解更多

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NMS-P118

Catalog No. A20994
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PARP-1 Inhibitor

NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy. 了解更多

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AZ6102

Catalog No. A15873
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TNKS1/2 抑制剂

AZ6102是有效的TNKS1/2抑制剂，对其他PARP家族酶具有100倍的选择性，对DLD-1细胞中Wnt途径的抑制作用的IC50为5 nM。了解更多

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MN-64

Catalog No. A15927
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TNKS 抑制剂

MN-64是Tankyrase 1和2的有效和选择性抑制剂（IC50分别为6和72 nM）。了解更多

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NVP-TNKS656

Catalog No. A15786
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TNKS2 抑制剂

NVP-TNKS656是一种高效，选择性和活性的TNKS2抑制剂，IC50为6 nM。对PARP1和PARP2的选择性> 300倍。了解更多

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G007-LK

Catalog No. A15528
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TNKS 抑制剂

G007-LK对坦科聚合酶1和2具有很高的选择性，生化IC50值分别为46 nM和25 nM，细胞IC50值为50 nM，并具有出色的小鼠药代动力学特征，了解更多

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- Dominic B. Bernkopf, .et al. An aggregon in conductin/axin2 regulates Wnt/β-catenin signaling and holds potential for cancer therapy, Nat Commun, 2019, 10:4251 PMID: 31534175
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BGP-15

Catalog No. A16344
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PARP 抑制剂

BGP-15是一种PARP抑制剂，可以预防小鼠的心力衰竭和心房颤动。了解更多

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ABT-888 (Veliparib)

Catalog No. A10026
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PARP 抑制剂

ABT-888 (Veliparib)是一种潜在的抗癌药物，可作为PARP抑制剂。了解更多

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- Subhajit Chatterjee, .et al. PARP inhibitor Veliparib (ABT-888) enhances the anti-angiogenic potentiality of Curcumin through deregulation of NECTIN-4 in oral cancer: Role of nitric oxide (NO), Cell Signal, 2021, Apr;80:109902 PMID: 33373686
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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BSI-201 (Iniparib)

Catalog No. A10164
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PARP 抑制剂

BSI-201 (Iniparib)是一种有效的PARP-1抑制剂，已被证明可以穿越血脑屏障。了解更多

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- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
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AG-014699 (Rucaparib)

Catalog No. A10045
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PARP 抑制剂

AG-014699 (Rucaparib)是一种PARP抑制剂，可抑制聚（ADP-核糖）聚合酶（PARP，后者是DNA修复中的关键酶。无细胞试验中作用于PARP1的Ki为1.4 nM，对其余8个PARP位点也有结合亲和力。了解更多

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- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
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AG14361

Catalog No. A10046
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PARP 抑制剂

AG14361是一种有效的PARP抑制剂，可在MMR（错配修复）有效/不足的细胞中增强替莫唑胺（TMZ）的细胞毒性。了解更多

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- Vimal Pandey, .et al. Roscovitine effectively enhances antitumor activity of temozolomide in vitro and in vivo mediated by increased autophagy and Caspase-3 dependent apoptosis, Scientific Reports, 2019, 9, Article number: 5012
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3-Aminobenzamide

Catalog No. A10475
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PARP 抑制剂

3-Aminobenzamide是一种新型PARP抑制剂，已知它通过抑制DNA损伤的修复使细胞在体外对辐射敏感。了解更多

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- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
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A-966492

Catalog No. A10019
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PARP1 抑制剂

A-966492在全细胞试验中显示出对K（i）为1 nM，EC（50）为1 nM的聚（ADP-核糖）聚合酶-1（PARP-1）酶的高效力。了解更多

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MK-4827 (Niraparib)

Catalog No. A11026
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PARP 抑制剂

MK-4827 (Niraparib)是一种新型有效的口服生物可利用的PARP-1和PARP-2抑制剂。了解更多

Product Citations (5)

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- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Ann-Katrin Hopp, .et al. Mitochondrial NAD+ Controls Nuclear ARTD1-Induced ADP-Ribosylation, Molecular cell, 2021, Jan 21; 81(2): 340?C354 PMID: 33450210
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
- Khalid Hilmi, .et al. CTCF facilitates DNA double-strand break repair by enhancing homologous recombination repair, Sci Adv, 2017, May; 3(5): e1601898 PMID: 28560323
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BMN673

Catalog No. A11243
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PARP 抑制剂

BMN-673是核酶聚（ADP-核糖）聚合酶（PARP）的口服生物利用抑制剂，无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂，但不抑制PARG，对PTEN突变型高度敏感。具有潜在的抗肿瘤活性。了解更多

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- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
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PJ 34 hydrochloride

Catalog No. A12665
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PARP 抑制剂

PJ 34 hydrochloride是聚（ADP-核糖）聚合酶（PARP）（EC50 = 20 nM）的有效抑制剂。了解更多

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- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
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UPF 1069

Catalog No. A12750
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PARP2 抑制剂

UPF 1069是一种选择性聚（ADP-核糖）聚合酶（PARP）2抑制剂（PARP-2和PARP-1的IC50值分别为0.3和8.0μM）。了解更多

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AZD-2461

Catalog No. A12393
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PARP 抑制剂

AZD2461是新型有效的PARP抑制剂，对P-糖蛋白的亲和力较低。了解更多

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JW 55

Catalog No. A13731
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TNKS1/2 抑制剂

JW 55是端锚聚合酶1和2（TNKS1/2）的PARP域的抑制剂。了解更多

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Rucaparib

Catalog No. A14182
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PARP-1 抑制剂

Rucaparib是纯化的全长人PARP-1的有效抑制剂，对LoVo和SW620细胞中的细胞PARP具有更高的抑制作用。了解更多

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- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
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ME0328

Catalog No. A14309
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PARP3 抑制剂

ME0328是一种有效的选择性PARP抑制剂，对PARP3的IC50为0.89μM，选择性是PARP1的7倍。了解更多

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Benzamide

Catalog No. A14371
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PARP-1 抑制剂

Benzamide是苯甲酸的酰胺衍生物，是聚（ADP-核糖）聚合酶-1（PARP-1）的抑制剂。了解更多

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BMN-673 8R,9S

Catalog No. A15024
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PARP 抑制剂

BMN-673 8R,9S 是BMN-673的（8R，9S）对映异构体。BMN 673是一种新型PARP抑制剂，IC50为0.58 nM。了解更多

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PJ34

Catalog No. A15215
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PARP 抑制剂

PJ34是新型有效的PARP-1/2特异性抑制剂，EC50为20 nM。了解更多

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- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
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4-HQN

Catalog No. A15370
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PARP 抑制剂

4-HQN已显示抑制PARP（聚（ADP-核糖）合成酶），该酶催化NAD+的ADP-核糖部分与各种蛋白质的共价结合。了解更多

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BYK 204165

Catalog No. A15371
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PARP-1 抑制剂

BYK204165是一种可渗透细胞的异喹啉二酮化合物，可有效并选择性地抑制聚（ADP-核糖）聚合酶1（PARP1）。了解更多

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BYK 49187

Catalog No. A15372
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PARP-1/PARP-2 抑制剂

BYK 49187，PARP-1和PARP-2抑制剂（无细胞重组PARP-1和鼠PARP-2的pIC50值分别为8.36和7.50）。了解更多

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DR 2313

Catalog No. A15373
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PARP 抑制剂

DR 2313是一种水溶性嘧啶酮化合物，起PARP（聚（ADP-核糖）聚合酶）抑制剂的作用。了解更多

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EB 47

Catalog No. A15374
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PARP1 抑制剂

EB 47是PARP1的有效抑制剂，IC50为45 nM。了解更多

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NU 1025

Catalog No. A15375
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PARP 抑制剂

NU 1025是一种有效的聚（ADP-核糖）聚合酶（PARP）抑制剂，可增强L1210细胞中一系列机制多样的抗癌药的细胞毒性。了解更多

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