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PARP

PARP

货号 产品名 CAS号 信息
CSN13593 XAV-939   284028-89-3 XAV-939 is a selective Wnt pathway β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 values of 11 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively.
CSN15823 WIKI4 838818-26-1 WIKI4 is a potent inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM) and inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM).
CSN17138 UPF 1069 1048371-03-4 UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM, which is ~27-fold selective against PARP1.
CSN26456 Talazoparib tosylate 1373431-65-2 Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib.
CSN50651 Senaparib 1401682-78-7 Senaparib, also known as IMP4297, is s a novel highly potent and selective oral PARP1/2 inhibitor with strong antitumor activity in preclinical studies. Senaparib demonstrated encouraging clinical benefit and a favorable tolerability profile in patients with advanced solid tumour.
CSN13901 Rucaparib phosphate 459868-92-9 Rucaparib phosphate is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains.
CSN13914 8-Fluoro-2-(4-((methylamino)methyl)phenyl)-4,5-dihydro-1H-azepino[5,4,3-cd]indol-6(3H)-one 283173-50-2 Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1, also showing binding affinity to eight other PARP domains.
CSN26731 Rucaparib monocamsylate 1859053-21-6 Rucaparib camsylate is a potent, orally available inhibitor of poly ADP-ribose polymerase (PARP) 1 and 2.
CSN23902 RK-287107 2171386-10-8 RK-287107 is a novel tankyrase-specific inhibitor with IC50 values of 14.3 nM and 10.6 nM for tankyrase-1 and tankyrase-2, respectively.
CSN27617 RBN012759 2360851-29-0 RBN012759 is a selective inhibitor of PARP14 with IC50 of <3 nM.
CSN27229 RBN-2397   2381037-82-5 RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors .
CSN17163 PJ34 344458-19-1 PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.
CSN13594 PJ34 HCl 344458-15-7 PJ34 HCl is a potent specific inhibitor of PARP-l/2 with IC50 of 110 nM and 86 nM.
CSN32499 PARPi-FL 1380359-84-1 PARPi-FL is a fluorescent PARP imaging agent.
CSN23081 Rucaparib camsylate 1327258-57-0 PARP inhibitor
CSN13750 NVP-TNKS656 1419949-20-4 NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, showing > 300 fold selectivity against PARP1 and PARP2.
CSN27556 Nudifloramide 701-44-0 Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro.
CSN19131 Niraparib metabolite M1 1476777-06-6 Niraparib metabolite M1 is a metabolite of niraparib, which acts as a poly (ADP-Ribose) polymerase (PARP) inhibitor.
CSN51360 Niraparib tosylate hydrate 1613220-15-7 Niraparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity.
CSN16905 MN-64 92831-11-3 MN-64 is an inhibitor of tankyrases, showed 6 nM potency against tankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.
CSN17416 Niraparib tosylate 1038915-73-9 MK-4827 tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM and with great activity in cancer cells with mutant BRCA-1 and BRCA-2 and > 330-fold selective against PARP3, V-PARP and Tank1.
CSN21302 Niraparib (R-enantiomer) 1038915-58-0 MK-4827 R-enantiomer is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
CSN13146 (S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide 1038915-60-4 MK-4827 is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively.
CSN17415 Niraparib HCl 1038915-64-8 MK-4827 HCl is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM, showing great activity in cancer cells with mutant BRCA-1 and BRCA-2, and is > 330-fold selective against PARP3, V-PARP and Tank1.
CSN19194 ME0328 1445251-22-8 ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
CSN19692 Lt-626 1207456-03-8 LT-626 functions as an effective radiosensitizer during fractionated radiation treatment, leading to significant decrease in tumor burden and doubling the median survival.
CSN16009 JW 55 664993-53-7 JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
CSN26730 INO-1001 501364-82-5 INO-1001 is an isoindolinone derivative and potent inhibitor of the nuclear enzyme poly (ADP-ribose) polymerase (PARP) with chemosensitization and radiosensitization properties. INO-1001 inhibits PARP, which may result in inhibition of tumor cell DNA repair mechanisms and, so, tumor cell resistance to chemotherapy and radiation therapy. PARP enzymes are activated by DNA breaks and have been implicated in the repair of DNA single-strand breaks (SSB). NOTE: as of 7/29/2016, many vendors are selling INO-1001 with wrong structure (3-aminobenzamide, CAS# 3544-24-9)
CSN17047 3-Aminobenzamide 3544-24-9 INO-1001 is a potent inhibitor of PARP with IC50 of < 50 nM in CHO cells and a mediator of oxidant-induced myocyte dysfunction during reperfusion.
CSN24184 GeA-69 2143475-98-1 GeA-69 is a selective PARP14 inhibitor with Kd value of 2.1 µM, targeting on macrodomain 2.
CSN17770 G007-LK 1380672-07-0 G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
CSN17497 Stenoparib 1140964-99-3 E7449 is an orally bioavailable, potent, small molecule inhibitor of PARP1 and PARP2 and enhances the efficacy of radiotherapy and chemotherapy and has potent single agent anticancer activity in BRCA-deficient tumors.
CSN25274 BYK204165 1104546-89-5 BYK204165 is a potent and selective poly(ADP-ribose) polymerase (PARP)-1 inhibitor (pIC50 values are 5.38 and 7.35 for PARP-2 and PARP-1 respectively).
CSN15885 Talazoparib 1207456-01-6 BMN-673 is a PARP1/2 inhibitor with IC50 of 0.57 nM for PARP1.
CSN16087 (8R,9S)-Talazoparib 1207456-00-5 BMN-673 8R,9S is an enantiomer of BMN-673, which is a PARP1/2 inhibitor with IC50 of 0.57 nM for PARP1.
CSN21993 Pamiparib 1446261-44-4 BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM.
CSN16496 AZD-2461 1174043-16-3 AZD2461 is a PARP inhibitor, which has the potential to avoid the olaparib resistence mediated by Pgp.
CSN32732 Saruparib 2589531-76-8 AZD-5305 is a potent and highly selective PARP1 inhibitor. AZD5305 dosed at 0.1mg/kg QD or higher for 35 days delivered about 90% regression in the BRCA1m triple-negative breast cancer (TNBC) xenograft model MDA-MB-436.
CSN27722 AZ9482   1825345-33-2 AZ9482 is a PARP inhibitor with IC50 values of 1, 1, 46, 640, 9, and 160nM for PARP1, -2, -3, -6, TNKS1/PARP5a, and TNKS2, respectively.
CSN17985 AZ6102 1645286-75-4 AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.
CSN18861 AZ1366 1645286-58-3 AZ1366 inhibits tankyrase as a cotreatment strategy with EGFR inhibition in an identifiable subset of EGFR-driven NSCLC.
CSN26555 PROTAC PARP1 degrader 2369022-68-2 at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
CSN17188 AG14361 328543-09-5 AG14361 is a potent inhibitor of PARP1 with Ki of < 5 nM.
CSN16464 A-966492 934162-61-5 A-966492 is a potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
CSN22652 4-Hydroxyquinazoline 491-36-1 4-HQN is a PARP inhibitor with IC50 of 9.5 μM.
CSN23547 3-Methoxybenzamide 5813-86-5 3-Methoxybenzamide is a competitive poly(ADP-ribose) synthetase inhibitor with Ki value < 2 μM and also inhibits ADP-ribosyltransferase (ADPRT).
CSN33195 4-Aminonaphthalimide 1742-95-6
CSN42991 K-756 130017-40-2
CSN106889 TNKS-IN-1 59455-93-5
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