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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 | Rucaparib | 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 hydrochloride | 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 | Niraparib | 1038915-60-4 | MK-4827 is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively. |
| CSN17415 | Niraparib hydrochloride | 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 | E7449 | 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 | AZD5305 | 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(3H)-Quinazolinone | 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 | 2-(4-(tert-Butyl)phenyl)quinazolin-4(1H)-one | 59455-93-5 |
