S0519 |
BYK204165
|
BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
-
Sci Transl Med, 2021, 13(592)eabc7211
|
|
S0732 |
GeA-69
|
GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM. |
|
|
S0913 |
4',5,7-Trimethoxyflavone
|
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. |
|
|
S1004 |
Veliparib (ABT-888)
|
Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3. |
-
Cell, 2022, 185(11):1943-1959.e21
-
Cell, 2022, 185(1):169-183.e19
-
Mol Cell, 2022, S1097-2765(22)00085-5
|
|
S1060 |
Olaparib (AZD2281)
|
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. |
-
Cell, 2022, 185(1):169-183.e19
-
Cancer Cell, 2022, S1535-6108(21)00662-0
-
Nat Cell Biol, 2022, 24(1):51-61
|
|
S1087 |
Iniparib (BSI-201)
|
Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
-
Front Oncol, 2021, 11:773186
-
Nat Commun, 2021, 12(1):736
-
PLoS Pathog, 2020, 21;16(4):e1008474
|
|
S1098 |
Rucaparib (AG-014699) phosphate
|
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. |
-
Mol Cell, 2022, S1097-2765(22)00394-X
-
Cancer Lett, 2022, 530:29-44
-
Mol Cancer Ther, 2022, molcanther.0798.2021
|
|
S1132 |
3-Aminobenzamide
|
3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way. |
-
Cell Death Discov, 2021, 7(1):181
-
Acta Pharm Sin B, 2019, 9(4):782-793
-
J Cell Biochem, 2017, 118(11):3943-3952
|
|
S1180 |
XAV-939
|
XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. |
-
Cancer Discov, 2022, candisc.0680.2021
-
Cell Res, 2022, 10.1038/s41422-022-00668-0
-
Nat Commun, 2022, 13(1):2548
|
|
S2178 |
AG-14361
|
AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
-
Cell Stem Cell, 2022, S1934-5909(22)00010-8
-
J Neurochem, 2022, 10.1111/jnc.15606
-
Front Cell Dev Biol, 2021, 9:621906
|
|
S2197 |
A-966492
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
-
Front Immunol, 2021, 12:712021
-
bioRxiv, 2021, 10.1101/2020.10.18.333070
-
Nat Commun, 2021, 12(1):736
|
|
S2741 |
Niraparib (MK-4827)
|
Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3. |
-
Nucleic Acids Res, 2022, 50(7):3958-3973
-
Mol Cancer Ther, 2022, molcanther.0604.2021
-
Sci Transl Med, 2021, 13(592)eabc7211
|
|
S4710 |
Picolinamide
|
Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
|
|
S4715 |
Benzamide
|
Benzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM. |
-
Int J Mol Sci, 2019, 20(21)
-
Mol Pharmacol, 2019, 96(4):419-429
-
Acta Neuropathol Commun, 2014, 2:57
|
|
S4948 |
Rucaparib
|
Rucaparib (Rubraca, AG014699, PF01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
-
Mol Cancer Ther, 2022, 21(4):647-657
-
Int J Mol Sci, 2022, 23(10)5770
-
Cancer Lett, 2021, S0304-3835(21)00571-1
|
|
S5195 |
Rucaparib Camsylate
|
Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
-
Int J Mol Sci, 2022, 23(10)5770
-
J Exp Clin Cancer Res, 2021, 40(1):276
-
Cell Death Dis, 2021, 12(6):546
|
|
S6739 |
MN 64
|
MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. |
|
|
S6745 |
JW55
|
JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
-
Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
-
Oncotarget, 2021, 12(7):674-685
|
|
S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
|
|
S7029 |
AZD2461
|
AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1. |
-
Cell Chem Biol, 2021, S2451-9456(21)00058-1
-
Nat Commun, 2021, 12(1):736
-
Dev Cell, 2020, 53(2):240-252.e7
|
|
S7048 |
Talazoparib (BMN 673)
|
Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. |
-
Cell, 2022, 185(1):169-183.e19
-
Mol Cell, 2022, S1097-2765(22)00394-X
-
Mol Cell, 2022, 82(10):1924-1939.e10
|
|
S7238 |
NVP-TNKS656
|
NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
|
-
Med Sci Monit, 2018, 24: 5914–5924
-
Med Sci Monit, 2018, 24:5914-5924
|
|
S7239 |
G007-LK
|
G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
|
-
J Clin Med, 2020, 30;9(4)
-
Cancer Discov, 2020, 6 pii: CD-19-1242
-
J Cell Sci, 2020, 14;jcs245811
|
|
S7300 |
PJ34 HCl
|
PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
-
Cell Rep, 2022, 39(6):110792
-
J Neurochem, 2022, 10.1111/jnc.15606
-
Nat Commun, 2021, 12(1):6362
|
|
S7438 |
ME0328
|
ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
-
Mol Cancer Ther, 2018, 17(10):2206-2216
-
SLAS Discov, 2018, 23(6):545-553
-
Breast Cancer Res Treat, 2018, 172(1):23-32
|
|
S7490 |
WIKI4
|
WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
|
-
Sci Rep, 2022, 12(1):7
-
Carcinogenesis, 2020, 41(7):993-1004
-
Nat Commun, 2019, 10(1):4363
|
|
S7625 |
Niraparib (MK-4827) tosylate
|
Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
-
Sci Transl Med, 2021, 13(592)eabc7211
-
Sci Adv, 2021, 7(21)eabf0197
-
Proc Natl Acad Sci U S A, 2021, 118(40)e2109252118
|
|
S7730 |
NU1025
|
NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
|
-
J Clin Med, 2020, 30;9(4)
-
Med Sci Monit, 2019, 25:2886-2895
|
|
S8038 |
UPF 1069
|
UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
-
Cell Death Differ, 2021, 10.1038/s41418-020-00733-4
-
J Clin Med, 2020, 30;9(4)
-
Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
|
|
S8363 |
NMS-P118
|
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
-
bioRxiv, 2021, 10.1101/2020.10.18.333070
-
J Clin Med, 2020, 30;9(4)
-
Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
|
|
S8370 |
BGP-15 2HCl
|
BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
|
|
S8419 |
Stenoparib (E7449)
|
Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
-
bioRxiv, 2021, 10.1101/2020.10.18.333070
-
J Clin Med, 2020, 30;9(4)
|
|
S8592 |
Pamiparib (BGB-290)
|
Pamiparib (BGB-290) is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
-
Neuro Oncol, 2021, 23(6):920-931
-
Cell Rep, 2021, 36(4):109429
-
Front Immunol, 2021, 12:712021
|
|
S8876 |
RK-287107
|
RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. |
|
|
S8992 |
RBN012759
|
RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response. |
|
|
S8993 |
Atamparib (RBN-2397)
|
Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment. |
|
|
S9360 |
4-Hydroxyquinazoline
|
4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM. |
|
|
S9712 |
Fluzoparib (SHR-3162)
|
Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity. |
|
|
S9875New |
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). |
|
|
S9893New |
Venadaparib(IDX-1197)
|
Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. |
|
|
S2271 |
Berberine chloride (NSC 646666)
|
Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
-
J Biomol Struct Dyn, 2022, 1-11
-
Front Pharmacol, 2021, 12:632201
-
Molecules, 2021, 26(5)1210
|
|
S5967 |
Berberine chloride hydrate
|
Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
-
Front Pharmacol, 2021, 12:632201
|
|
S6882 |
HI-TOPK-032
|
HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells. |
|
|
S0519 |
BYK204165
|
BYK204165 is a potent and selective inhibitor of the poly(ADP-ribose) polymerase (PARP). BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with pIC50 of 7.35 and pKi of 7.05 and murine PARP-2 (mPARP-2) with pIC50 of 5.38, respectively. |
- Sci Transl Med, 2021, 13(592)eabc7211
|
|
S0732 |
GeA-69
|
GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM. |
|
|
S0913 |
4',5,7-Trimethoxyflavone
|
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. |
|
|
S1004 |
Veliparib (ABT-888)
|
Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. Phase 3. |
- Cell, 2022, 185(11):1943-1959.e21
- Cell, 2022, 185(1):169-183.e19
- Mol Cell, 2022, S1097-2765(22)00085-5
|
|
S1060 |
Olaparib (AZD2281)
|
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. |
- Cell, 2022, 185(1):169-183.e19
- Cancer Cell, 2022, S1535-6108(21)00662-0
- Nat Cell Biol, 2022, 24(1):51-61
|
|
S1087 |
Iniparib (BSI-201)
|
Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
- Front Oncol, 2021, 11:773186
- Nat Commun, 2021, 12(1):736
- PLoS Pathog, 2020, 21;16(4):e1008474
|
|
S1098 |
Rucaparib (AG-014699) phosphate
|
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3. |
- Mol Cell, 2022, S1097-2765(22)00394-X
- Cancer Lett, 2022, 530:29-44
- Mol Cancer Ther, 2022, molcanther.0798.2021
|
|
S1132 |
3-Aminobenzamide
|
3-Aminobenzamide (3-ABA , 3-Amino Benzamide, 3-AB) is a potent inhibitor of Poly(ADP-ribose)polymerase (PARP) and inhibits cell apoptosis after SCI (Spinal Cord Injury) in caspase-independent way. |
- Cell Death Discov, 2021, 7(1):181
- Acta Pharm Sin B, 2019, 9(4):782-793
- J Cell Biochem, 2017, 118(11):3943-3952
|
|
S1180 |
XAV-939
|
XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β. |
- Cancer Discov, 2022, candisc.0680.2021
- Cell Res, 2022, 10.1038/s41422-022-00668-0
- Nat Commun, 2022, 13(1):2548
|
|
S2178 |
AG-14361
|
AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides. |
- Cell Stem Cell, 2022, S1934-5909(22)00010-8
- J Neurochem, 2022, 10.1111/jnc.15606
- Front Cell Dev Biol, 2021, 9:621906
|
|
S2197 |
A-966492
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
- Front Immunol, 2021, 12:712021
- bioRxiv, 2021, 10.1101/2020.10.18.333070
- Nat Commun, 2021, 12(1):736
|
|
S2741 |
Niraparib (MK-4827)
|
Niraparib (MK-4827) is a selective inhibitor of PARP1/2 with IC50 of 3.8 nM/2.1 nM, with great activity in cancer cells with mutant BRCA-1 and BRCA-2. It is >330-fold selective against PARP3, V-PARP and Tank1. Niraparib can form PARP–DNA complexes resulting in DNA damage, apoptosis, and cell death. Phase 3. |
- Nucleic Acids Res, 2022, 50(7):3958-3973
- Mol Cancer Ther, 2022, molcanther.0604.2021
- Sci Transl Med, 2021, 13(592)eabc7211
|
|
S4710 |
Picolinamide
|
Picolinamide (2-Pyridinecarboxamide, Picolinoylamide, 2-Carbamoylpyridine) is found to be a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells. |
|
|
S4715 |
Benzamide
|
Benzamide, a derivative of benzoic acid, is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM. |
- Int J Mol Sci, 2019, 20(21)
- Mol Pharmacol, 2019, 96(4):419-429
- Acta Neuropathol Commun, 2014, 2:57
|
|
S4948 |
Rucaparib
|
Rucaparib (Rubraca, AG014699, PF01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
- Mol Cancer Ther, 2022, 21(4):647-657
- Int J Mol Sci, 2022, 23(10)5770
- Cancer Lett, 2021, S0304-3835(21)00571-1
|
|
S5195 |
Rucaparib Camsylate
|
Rucaparib (Rubraca, AG014699, PF01367338) Camsylate is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. |
- Int J Mol Sci, 2022, 23(10)5770
- J Exp Clin Cancer Res, 2021, 40(1):276
- Cell Death Dis, 2021, 12(6):546
|
|
S6739 |
MN 64
|
MN-64 is a potent inhibitor of TNKS1 and TNKS2 with IC50 value of 6 and 72 nM, respectively. |
|
|
S6745 |
JW55
|
JW55 is a potent and selective inhibitor of the canonical Wnt pathway that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
- Chin J Integr Med, 2021, 10.1007/s11655-021-3282-0
- Oncotarget, 2021, 12(7):674-685
|
|
S6899 |
Licochalcone D
|
Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage. |
|
|
S7029 |
AZD2461
|
AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1. |
- Cell Chem Biol, 2021, S2451-9456(21)00058-1
- Nat Commun, 2021, 12(1):736
- Dev Cell, 2020, 53(2):240-252.e7
|
|
S7048 |
Talazoparib (BMN 673)
|
Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. |
- Cell, 2022, 185(1):169-183.e19
- Mol Cell, 2022, S1097-2765(22)00394-X
- Mol Cell, 2022, 82(10):1924-1939.e10
|
|
S7238 |
NVP-TNKS656
|
NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
|
- Med Sci Monit, 2018, 24: 5914–5924
- Med Sci Monit, 2018, 24:5914-5924
|
|
S7239 |
G007-LK
|
G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
|
- J Clin Med, 2020, 30;9(4)
- Cancer Discov, 2020, 6 pii: CD-19-1242
- J Cell Sci, 2020, 14;jcs245811
|
|
S7300 |
PJ34 HCl
|
PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2. |
- Cell Rep, 2022, 39(6):110792
- J Neurochem, 2022, 10.1111/jnc.15606
- Nat Commun, 2021, 12(1):6362
|
|
S7438 |
ME0328
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ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1. |
- Mol Cancer Ther, 2018, 17(10):2206-2216
- SLAS Discov, 2018, 23(6):545-553
- Breast Cancer Res Treat, 2018, 172(1):23-32
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S7490 |
WIKI4
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WIKI4 is a novel Tankyrase inhibitor with IC50 of 15 nM for TNKS2, and leads to inhibition of Wnt/beta-catenin signaling.
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- Sci Rep, 2022, 12(1):7
- Carcinogenesis, 2020, 41(7):993-1004
- Nat Commun, 2019, 10(1):4363
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S7625 |
Niraparib (MK-4827) tosylate
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Niraparib tosylate (MK-4827, ZEJULA) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM. Niraparib increases formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. |
- Sci Transl Med, 2021, 13(592)eabc7211
- Sci Adv, 2021, 7(21)eabf0197
- Proc Natl Acad Sci U S A, 2021, 118(40)e2109252118
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S7730 |
NU1025
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NU1025 (NSC 696807) is a potent PARP inhibitor with IC50 of 400 nM.
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- J Clin Med, 2020, 30;9(4)
- Med Sci Monit, 2019, 25:2886-2895
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S8038 |
UPF 1069
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UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1. |
- Cell Death Differ, 2021, 10.1038/s41418-020-00733-4
- J Clin Med, 2020, 30;9(4)
- Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
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S8363 |
NMS-P118
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NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively). |
- bioRxiv, 2021, 10.1101/2020.10.18.333070
- J Clin Med, 2020, 30;9(4)
- Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007
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S8370 |
BGP-15 2HCl
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BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury. |
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S8419 |
Stenoparib (E7449)
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Stenoparib (E7449, 2X-121, MGI25036) is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 and also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively. |
- bioRxiv, 2021, 10.1101/2020.10.18.333070
- J Clin Med, 2020, 30;9(4)
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S8592 |
Pamiparib (BGB-290)
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Pamiparib (BGB-290) is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. |
- Neuro Oncol, 2021, 23(6):920-931
- Cell Rep, 2021, 36(4):109429
- Front Immunol, 2021, 12:712021
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S8876 |
RK-287107
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RK-287107 is a novel, potent and selective tankyrase inhibitor with antitumor activity. RK-287107 inhibits tankyrase-1 and tankyrase-2 in vitro with IC50 of 14.3 nM and 10.6 nM. |
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S8992 |
RBN012759
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RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response. |
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S8993 |
Atamparib (RBN-2397)
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Atamparib (RBN-2397) is a potent, selective and orally active NAD+ competitive inhibitor PARP7 with IC50 of <3 nM and Kd of <0.001 μM. RBN-2397 has the potential for the research of tumor treatment. |
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S9360 |
4-Hydroxyquinazoline
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4-Hydroxyquinazoline (Quinazolin-4-ol, 4-Quinazolinol) is a PARP inhibitor with a high potency for PARP-1 with IC50 of 9.5 μM. |
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S9712 |
Fluzoparib (SHR-3162)
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Fluzoparib (SHR3162, HS10160) is a potent Poly (ADP-ribose) polymerase (PARP) inhibitor that shows anti-tumor activity. |
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S9875New |
AZD5305
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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). |
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S9893New |
Venadaparib(IDX-1197)
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Venadaparib (IDX-1197), a potent PARP1/2 inhibitor with IC50 values of 1.4 nM and 1.0 nM respectively, prevents the repair of DNA single-strand breaks (SSB) and promotes the conversion of SSB to double-stranded breaks (DSB), which ultimately leads to synthetic lethality in cancer cells. |
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