PARP
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
PARP产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1060 |
Olaparib (AZD2281, Ku-0059436)Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。 |
CYREN does not regulate repair of replication-induced DSBs. Representative images of chromosomes.
|
|
| S1004 |
Veliparib (ABT-888)Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂，无细胞试验中Ki分别为5.2 nM和2.9 nM，对SIRT2没有活性。Phase 3。 |
Chromosomal single-strand break repair rates in the indicated RPE-1 cell lines following treatment with 50 μM H2O2 in the presence/absence of 10 μM of the PARP inhibitor (PARPi) Veliparib, as measured by alkaline comet assay. Data are the mean tail moment of 100 cells per sample per experiment and are the average (-/+SEM) of three independent experiments. Two-way ANOVA analysis between relevant genotypes is presented (ns= not significant, **= p<0.01, ***= p<0.001).
|
|
| S1098 |
Rucaparib (AG-014699,PF-01367338) phosphateRucaparib (AG-014699,PF-01367338)是一种PARP抑制剂，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。Phase 3。 |
Representative images for RAD51 and γH2AX foci formation, surrogate DSB markers, in stable shK-H or shSCR 231 cells after rucaparib or vehicle (0.01% DMSO) treatment for 24 hours. DAPI-stained cell nuclei. Scale bars, 10 μm.
|
|
| S1087 |
Iniparib (BSI-201)Iniparib (BSI-201)是一种PARP1抑制剂，在三阴性乳腺癌(TNBC)中具有作用效果。Phase 3。 |
Immunoblot analysis of
PARylation after treatment with various PARP
inhibitors.The asterisk indicates
a nonspecific band.
|
|
| S7048 |
Talazoparib (BMN 673)Talazoparib (BMN 673)是一种新型的PARP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。Phase 3。 |
DNA damage persists on withdrawal of PARPi in RNASEH2AKO cells. Wild-type and RNASEH2AKO HeLa cells were treated with talazoparib and released into fresh medium for the indicated times before being processed for γ-H2AX immunofluorescence and propidium iodide (PI) staining. The γ-H2AX immunofluorescence (pseudocolor plots) and cell cycle (histograms) FACS profiles shown are representative of three biologically independent experiments.
|
|
| S9360New |
4-Hydroxyquinazoline |
||
| S8592New |
Pamiparib (BGB-290)Pamiparib (BGB-290)是有效的PARP1和PARP2选择性抑制剂，IC50分别为0.83和0.11 nM。相较于其他PARP酶，它对PARP1和PARP2具有高选择性。 |
||
| S2178 |
AG-14361AG14361是一种有效的PARP1抑制剂，无细胞试验中Ki为<5 nM。它比benzamides至少有效1000倍。 |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| S1132 |
INO-1001 (3-Aminobenzamide)INO-1001是一种有效的PARP抑制剂，作用于CHO细胞的IC50为<50 nM，在再灌注期间，是一种因氧化诱导而发生的心肌功能障碍的调节剂。Phase 2 |
Propofol inhibited the increase of PARP-1׳s expression and activity. Mice (n=6) were injected intraperitoneally with propofol, INO-1001 (a PARP-1 inhibitor) or equal volume of normal saline (NS), and then were trained with objects. Naïve animals were injected with normal saline and trained without objects (the same as habituation). 30 min after acquisition trial, the hippocampal tissues were harvested for determining PARP-1 (A and B) and PAR (C and D) expression by Western blot. Histogram represented the relative level normalized to naïve. *P<0.05, **P<0.01.
|
|
| S2197 |
A-966492A-966492是一种新型有效的PARP1和PARP2抑制剂，Ki分别为1 nM和1.5 nM。 |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| S7300 |
PJ34 HClPJ34 HCl 是PJ34的盐酸盐形式，是一种PARP抑制剂，EC50为20 nM，同等有效作用于PARP1/2。 |
LN229 GBM cells were treated with PJ34 (20 µM), TRAIL (200 ng/ml) or the combination of both and analyzed for the expression of DR5, caspase-9 (CP9) and cleaved caspase-3 (cCP3). The vertical line on the immunoblot indicates that the first and second samples were noncontiguous, but run on the same gel simultaneously with the other samples.
|
|
| S2741 |
Niraparib (MK-4827)Niraparib (MK4827)是一种口服有效的选择性PARP-1和PARP-2抑制剂，可在有BRCA和PTEN功能缺陷的临床肿瘤模型中引起合成致死性。 |
Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W780 cells.
|
|
| S8038 |
UPF 1069UPF 1069是一种选择性PARP2抑制剂，IC50为0.3 μM，比作用于PARP1选择性高27倍左右。 |
||
| S7029 |
AZD2461AZD2461是一种新型PARP抑制剂，作用于Pgp比Olaparib亲和力低。Phase 1。 |
(b) Hoechst-positive cell quantification of caspase and PARP inhibitors and their effect on ARPE-19 cells undergoing UOS in the presence and absence of NPD1 (lower panel). Bars represent data averages of three repeats (technical replicas) of three independent experiments (biological replicas). *P<0.05
|
|
| S7438 |
ME0328ME0328 是一种强效的选择性的PARP抑制剂，IC50为0.89 μM，其作用于PARP3的选择性比作用于PARP1的选择性高约七倍。 |
Colony survival assay in wild-type A549 cells treated with vehicle, 3.0 μM ME0328 or 500 nM KU58948 and pyridostatin.
|
|
| S8370 |
BGP-15 2HClBGP-15是具有PARP抑制活性的烟酸胺肟衍生物。BGP-15被发现能够在缺血再灌注损伤后起到保护作用。 |
||
| S7625 |
Niraparib (MK-4827) tosylateNiraparib (MK-4827) tosylate是PARP1/PARP2的选择性抑制剂，IC50分别为3.8 nM和2.1 nM。 |
Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. *P<0.05, **P<0.01
|
|
| S7730 |
NU1025NU1025 是一种有效的 PARP 抑制剂，IC50 为 400 nM。 |
||
| S7239 |
G007-LKG007-LK是一种有效的选择性tankyrase抑制剂，对TNKS1/2的IC50分别为46 nM 和 25 nM。 |
Western blot analysis of SH3BP2 in WT BMMs after culture for 2 days in the presence of IWR-1 (2 μM), G007-LK (0.1 μM), or ICG001 (2 μM). |
|
| S7238 |
NVP-TNKS656NVP-TNKS656是一种高度有效的，选择性的，口服具有活性的tankyrase抑制剂，对 TNKS2 的IC50为6 nM，选择性比作用于PARP1和PARP2高300多倍。 |
||
| S8419 |
E7449E7449是一种具有生物口服活性的、能够通过血脑屏障的PARP1/2双效小分子化合物抑制剂，同样还能抑制PARP5a/5b（即TNKS1/2）。对PARP1和PARP2的IC50分别为1 nM和1.2 nM。 |
||
| S8363 |
NMS-P118NMS-P118是一种有效的、具有口服活性、高度选择性的PARP-1抑制剂，具有良好的药物吸收和药物动力学特性，对PARP1的选择性比对PARP2高150倍（Kd 0.009 μM vs 1.39 μM） |
||
| S4715 |
BenzamideBenzamide, PARP的抑制剂，IC50为3.3 μM。它是苯甲酸的一种衍生物。 |
||
| S4710 |
PicolinamidePicolinamide在大鼠胰岛细胞核中，是一种强效的PARP抑制剂。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1060 |
Olaparib (AZD2281, Ku-0059436)Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。 |
CYREN does not regulate repair of replication-induced DSBs. Representative images of chromosomes.
|
|
| S1004 |
Veliparib (ABT-888)Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂，无细胞试验中Ki分别为5.2 nM和2.9 nM，对SIRT2没有活性。Phase 3。 |
Chromosomal single-strand break repair rates in the indicated RPE-1 cell lines following treatment with 50 μM H2O2 in the presence/absence of 10 μM of the PARP inhibitor (PARPi) Veliparib, as measured by alkaline comet assay. Data are the mean tail moment of 100 cells per sample per experiment and are the average (-/+SEM) of three independent experiments. Two-way ANOVA analysis between relevant genotypes is presented (ns= not significant, **= p<0.01, ***= p<0.001).
|
|
| S1098 |
Rucaparib (AG-014699,PF-01367338) phosphateRucaparib (AG-014699,PF-01367338)是一种PARP抑制剂，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。Phase 3。 |
Representative images for RAD51 and γH2AX foci formation, surrogate DSB markers, in stable shK-H or shSCR 231 cells after rucaparib or vehicle (0.01% DMSO) treatment for 24 hours. DAPI-stained cell nuclei. Scale bars, 10 μm.
|
|
| S1087 |
Iniparib (BSI-201)Iniparib (BSI-201)是一种PARP1抑制剂，在三阴性乳腺癌(TNBC)中具有作用效果。Phase 3。 |
Immunoblot analysis of
PARylation after treatment with various PARP
inhibitors.The asterisk indicates
a nonspecific band.
|
|
| S7048 |
Talazoparib (BMN 673)Talazoparib (BMN 673)是一种新型的PARP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。Phase 3。 |
DNA damage persists on withdrawal of PARPi in RNASEH2AKO cells. Wild-type and RNASEH2AKO HeLa cells were treated with talazoparib and released into fresh medium for the indicated times before being processed for γ-H2AX immunofluorescence and propidium iodide (PI) staining. The γ-H2AX immunofluorescence (pseudocolor plots) and cell cycle (histograms) FACS profiles shown are representative of three biologically independent experiments.
|
|
| S9360New |
4-Hydroxyquinazoline |
||
| S8592New |
Pamiparib (BGB-290)Pamiparib (BGB-290)是有效的PARP1和PARP2选择性抑制剂，IC50分别为0.83和0.11 nM。相较于其他PARP酶，它对PARP1和PARP2具有高选择性。 |
||
| S2178 |
AG-14361AG14361是一种有效的PARP1抑制剂，无细胞试验中Ki为<5 nM。它比benzamides至少有效1000倍。 |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| S1132 |
INO-1001 (3-Aminobenzamide)INO-1001是一种有效的PARP抑制剂，作用于CHO细胞的IC50为<50 nM，在再灌注期间，是一种因氧化诱导而发生的心肌功能障碍的调节剂。Phase 2 |
Propofol inhibited the increase of PARP-1׳s expression and activity. Mice (n=6) were injected intraperitoneally with propofol, INO-1001 (a PARP-1 inhibitor) or equal volume of normal saline (NS), and then were trained with objects. Naïve animals were injected with normal saline and trained without objects (the same as habituation). 30 min after acquisition trial, the hippocampal tissues were harvested for determining PARP-1 (A and B) and PAR (C and D) expression by Western blot. Histogram represented the relative level normalized to naïve. *P<0.05, **P<0.01.
|
|
| S2197 |
A-966492A-966492是一种新型有效的PARP1和PARP2抑制剂，Ki分别为1 nM和1.5 nM。 |
Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band. |
|
| S7300 |
PJ34 HClPJ34 HCl 是PJ34的盐酸盐形式，是一种PARP抑制剂，EC50为20 nM，同等有效作用于PARP1/2。 |
LN229 GBM cells were treated with PJ34 (20 µM), TRAIL (200 ng/ml) or the combination of both and analyzed for the expression of DR5, caspase-9 (CP9) and cleaved caspase-3 (cCP3). The vertical line on the immunoblot indicates that the first and second samples were noncontiguous, but run on the same gel simultaneously with the other samples.
|
|
| S2741 |
Niraparib (MK-4827)Niraparib (MK4827)是一种口服有效的选择性PARP-1和PARP-2抑制剂，可在有BRCA和PTEN功能缺陷的临床肿瘤模型中引起合成致死性。 |
Western Blot data testing protein expression after treatment with Olaparib, Niraparib, and Talazoparib on Brca1-deficient cell line in W780 cells.
|
|
| S8038 |
UPF 1069UPF 1069是一种选择性PARP2抑制剂，IC50为0.3 μM，比作用于PARP1选择性高27倍左右。 |
||
| S7029 |
AZD2461AZD2461是一种新型PARP抑制剂，作用于Pgp比Olaparib亲和力低。Phase 1。 |
(b) Hoechst-positive cell quantification of caspase and PARP inhibitors and their effect on ARPE-19 cells undergoing UOS in the presence and absence of NPD1 (lower panel). Bars represent data averages of three repeats (technical replicas) of three independent experiments (biological replicas). *P<0.05
|
|
| S7438 |
ME0328ME0328 是一种强效的选择性的PARP抑制剂，IC50为0.89 μM，其作用于PARP3的选择性比作用于PARP1的选择性高约七倍。 |
Colony survival assay in wild-type A549 cells treated with vehicle, 3.0 μM ME0328 or 500 nM KU58948 and pyridostatin.
|
|
| S8370 |
BGP-15 2HClBGP-15是具有PARP抑制活性的烟酸胺肟衍生物。BGP-15被发现能够在缺血再灌注损伤后起到保护作用。 |
||
| S7625 |
Niraparib (MK-4827) tosylateNiraparib (MK-4827) tosylate是PARP1/PARP2的选择性抑制剂，IC50分别为3.8 nM和2.1 nM。 |
Berberine activates PARP1 in ovarian cancer cells. PAR synthesis is detected by immunofluorescence staining in A2780 and HO8910 treated with different concentration of berberine alone or in combination with niraparib (10 μM) for 48 h. Top: representative examples of immunofluorescence staining of PAR. Scale bar, 20 μm. Bottom: quantification of PAR level in A2780 and HO8910. Immunofluorescence intensities were quantified by ImageJ. *P<0.05, **P<0.01
|
|
| S7730 |
NU1025NU1025 是一种有效的 PARP 抑制剂，IC50 为 400 nM。 |
||
| S7239 |
G007-LKG007-LK是一种有效的选择性tankyrase抑制剂，对TNKS1/2的IC50分别为46 nM 和 25 nM。 |
Western blot analysis of SH3BP2 in WT BMMs after culture for 2 days in the presence of IWR-1 (2 μM), G007-LK (0.1 μM), or ICG001 (2 μM). |
|
| S7238 |
NVP-TNKS656NVP-TNKS656是一种高度有效的，选择性的，口服具有活性的tankyrase抑制剂，对 TNKS2 的IC50为6 nM，选择性比作用于PARP1和PARP2高300多倍。 |
||
| S8419 |
E7449E7449是一种具有生物口服活性的、能够通过血脑屏障的PARP1/2双效小分子化合物抑制剂，同样还能抑制PARP5a/5b（即TNKS1/2）。对PARP1和PARP2的IC50分别为1 nM和1.2 nM。 |
||
| S8363 |
NMS-P118NMS-P118是一种有效的、具有口服活性、高度选择性的PARP-1抑制剂，具有良好的药物吸收和药物动力学特性，对PARP1的选择性比对PARP2高150倍（Kd 0.009 μM vs 1.39 μM） |
||
| S4715 |
BenzamideBenzamide, PARP的抑制剂，IC50为3.3 μM。它是苯甲酸的一种衍生物。 |
||
| S4710 |
PicolinamidePicolinamide在大鼠胰岛细胞核中，是一种强效的PARP抑制剂。 |
