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PARP1 Human Pre-designed siRNA Set A contains three designed siRNAs for PARP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Parp1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Parp1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
PARP1-IN-11 (compound 49) is a potent PARP1 inhibitor with IC50 value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 [1].
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells [1].
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) [1].
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity [1].
PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations [1].
PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) [1].
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer [1].
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer [1].
PARP1-IN-16 (compound 12a) is a potent PARP1 inhibitor, with an IC50 of 1.89 nM. PARP1-IN-16 can arrest the cell cycle in S phase and induce apoptosis in HCT-116 cells [1].
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells [1].
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 [1].
PARP-1-IN-4 is a PARP-1 inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC50 value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma [1].
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis[1].
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM [1].
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice [1].
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) [1].
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer [1].
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis[1].
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model [1].
PARP-1-IN-13 (Compound 19c) is a PARP-1 inhibitor (IC50: 26 nM). PARP-1-IN-13 inhibits DNA single-strand breakage repair and aggravates DNA double-strand breakage. PARP-1-IN-13 promotes the apoptosis of cancer cells through the mitochondrial apoptosis pathway [1].
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis [1].
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor [1].
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[1].
PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities [1].
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator [1] .
PARPi-FL is a small molecule and fluorescent inhibitor of PARP1. PARPi-FL is a highly selective probe and can be used as an imaging agent to detect glioblastomas in vivo [1].
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice was 75.4% [1].
iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1[1].
SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to PARP1, with an IC50 of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM [1].
BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1(hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1[1].
Amelparib is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50 =18.5 nmol/L) and cellular PAR formation (IC50 =10.7 nmol/L) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke [1].
Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride inhibits PARP-1 activity (IC50 = 18.5 nM) and cellular PAR formation (IC50 = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke [1].
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD + breast cancer and advanced solid malignancies research [1].
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity [1].
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Stenoparib (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.
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity [1].
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 [1].
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research [1].
MD6a is a melatonin derivative with inhibitroy activity towards PARP-1, which maintains proteins hemostasis and improves mitochondrial function through TOR/HSF-1 signaling. MD6a a neuroprotective effect [1].
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors [1].
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors [1].
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research [1].
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy [1].
CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects [1] .
Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models [1].
Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins [1] .
DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance [1].
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts [1].
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells [1].
DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection [1].
CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560) [1].
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. 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[1].
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach [1]. Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo [1] .
PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity [1].
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo [1] .
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations [1].
NH2-PEG7 is a PROTAC linker, which refers to the PEG composition. NH2-PEG7 can be used in the synthesis of the PROTAC PARP1 degrader iRucaparib-AP6 [1].
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair [1] .
5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver [1] .
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research [1].
PARP/HDAC-IN-1 (compound B102) is a potent dual inhibitor of PARP and HDAC. PARP/HDAC-IN-1 inhibits PARP1, PARP2 and HDAC1 with IC50s of 19.01, 2.13, 1690 nM, respectively [1].
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. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity [1] .
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
DPQ hydrochloride (6, 7-dimethoxy-2 -(1-piperazinyl)-4-quinazolinamine hydrochloride) is a PARP1 inhibitor, with IC50 value of 40 nM. DPQ hydrochloride has anti-inflammatory and antiviral activity. DPQ hydrochloride is used to study acute lung injury [1] .
Thalidomide-NH-PEG7 is a synthesized E3 ligase ligand-linker conjugate for ADC. Thalidomide-NH-PEG7 can be connected to the ligand for protein by a linker to form PROTAC iRucaparib-AP6, a highly specific PARP1 degrader [1].
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12[1].
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity [1] .
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. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity [1] .
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity [1] .
ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1ARTD1/PARP1 with IC50s of 2.0 μM, and 9.7 μM, respectively [1].
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor [1] .
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model [1].
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research [1] .
AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.
MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity [1].
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1(ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively [1].
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase [1].
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM [1]. (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase [1].
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats [1].
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model [1].
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases [1].
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia [1].
Amino-PEG3-C2-Azido is a PEG-based PROTAC linker can be used in the synthesis of the PARP1 degrader iRucaparib-TP3 (HY-130645) [1]. Amino-PEG3-C2-Azido is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
EB-47 dihydrochloride, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD + and extends from the nicotinamide to the adenosine subsite [1].
EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD + and extends from the nicotinamide to the adenosine subsite [1].
PARP7-IN-16 (compound 36) is a potent, selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer [1].
NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP .
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .
Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research [1].
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity [1] .
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity [1].
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity [1].
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more [1].
NTPO trisodium is a DNA damage inducer, causing genomic DNA damage and fragmentation, activating ATR-mediated cell cycle checkpoints. The DNA damaging effects of NTPO trisodium are abrogated by base excision repair (BER) but not nucleotide excision repair (NER) [1].
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 [1].
Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins [1] .
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia [1].
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
The PARP1 protein is a polyADP-ribosyltransferase that crucially mediates polyADP-ribosylation (PARsylation) in DNA repair, including base excision and double-strand breaks. By interacting with factors such as HPF1 and NMNAT1, the specificity of PARP1 extends to various amino acids. PARP Protein, Human (sf9, His) is the recombinant human-derived PARP protein, expressed by Sf9 insect cells , with C-His labeled tag. The total length of PARP Protein, Human (sf9, His) is 1014 a.a., with molecular weight of 100-110 kDa.
PARP, a poly-ADP-ribosyltransferase, catalyzes poly-ADP-ribosylation, crucial for DNA repair. This protein irreversibly binds to DNA breaks, disrupting repair processes and triggering DNA damage-induced apoptosis. PARP Protein, Mouse (sf9, His) is the recombinant mouse-derived PARP protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of PARP Protein, Mouse (sf9, His) is 1014 a.a., with molecular weight of ~75 kDa.
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. 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[1].
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
Cleaved-PARP1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 113 kDa, targeting to Cleaved-PARP1. It can be used for WB assays with tag free, in the background of Human.
PARP1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 113 kDa, targeting to PARP. It can be used for WB,ICC/IF,IHC-P,FC assays with tag free, in the background of Human, Mouse.
PARP1 Antibody (YA245) is a non-conjugated and Rabbit origined monoclonal antibody about 113 kDa, targeting to PARP1. It can be used for WB,IHC-F,IHC-P,ICC/IF assays with tag free, in the background of Human, Mouse, Rat.
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1?degrader based on Rucaparib by using the PROTAC approach [1]. Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Amino-PEG3-C2-Azido is a PEG-based PROTAC linker can be used in the synthesis of the PARP1 degrader iRucaparib-TP3 (HY-130645) [1]. Amino-PEG3-C2-Azido is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells [1].
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM [1]. (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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