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DNA Damage

DNA Damage

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PARP-2-IN-1

Catalog No. A20240
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PARP-2 inhibitor

PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM. 了解更多

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INO-1001

Catalog No. A20680
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PARP inhibitor

INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. 了解更多

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BSI-201 (Iniparib)

Catalog No. A10164
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PARP 抑制剂

BSI-201 (Iniparib)是一种有效的PARP-1抑制剂，已被证明可以穿越血脑屏障。了解更多

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- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
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AG-014699 (Rucaparib)

Catalog No. A10045
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PARP 抑制剂

AG-014699 (Rucaparib)是一种PARP抑制剂，可抑制聚（ADP-核糖）聚合酶（PARP，后者是DNA修复中的关键酶。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。了解更多

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- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
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3-Aminobenzamide

Catalog No. A10475
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PARP 抑制剂

3-Aminobenzamide是一种新型PARP抑制剂，已知它通过抑制DNA损伤的修复使细胞在体外对辐射敏感。了解更多

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- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
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BMN673

Catalog No. A11243
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PARP 抑制剂

BMN-673是核酶聚（ADP-核糖）聚合酶（PARP）的口服生物利用抑制剂，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。具有潜在的抗肿瘤活性。了解更多

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- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
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PJ34

Catalog No. A15215
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PARP 抑制剂

PJ34是新型有效的PARP-1/2特异性抑制剂，EC50为20 nM。了解更多

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- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
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G007-LK

Catalog No. A15528
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TNKS 抑制剂

G007-LK对坦科聚合酶1和2具有很高的选择性，生化IC50值分别为46 nM和25 nM，细胞IC50值为50 nM，并具有出色的小鼠药代动力学特征，了解更多

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- Dominic B. Bernkopf, .et al. An aggregon in conductin/axin2 regulates Wnt/β-catenin signaling and holds potential for cancer therapy, Nat Commun, 2019, 10:4251 PMID: 31534175
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Rucaparib

Catalog No. A14182
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PARP-1 抑制剂

Rucaparib是纯化的全长人PARP-1的有效抑制剂，对LoVo和SW620细胞中的细胞PARP具有更高的抑制作用。了解更多

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- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
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AG14361

Catalog No. A10046
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PARP 抑制剂

AG14361是一种有效的PARP抑制剂，可在MMR（错配修复）有效/不足的细胞中增强替莫唑胺（TMZ）的细胞毒性。了解更多

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- Vimal Pandey, .et al. Roscovitine effectively enhances antitumor activity of temozolomide in vitro and in vivo mediated by increased autophagy and Caspase-3 dependent apoptosis, Scientific Reports, 2019, 9, Article number: 5012
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PJ 34 hydrochloride

Catalog No. A12665
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PARP 抑制剂

PJ 34 hydrochloride是聚（ADP-核糖）聚合酶（PARP）（EC50 = 20 nM）的有效抑制剂。了解更多

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- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
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MK-4827 (Niraparib)

Catalog No. A11026
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PARP 抑制剂

MK-4827 (Niraparib)是一种新型有效的口服生物可利用的PARP-1和PARP-2抑制剂。了解更多

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- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Ann-Katrin Hopp, .et al. Mitochondrial NAD+ Controls Nuclear ARTD1-Induced ADP-Ribosylation, Molecular cell, 2021, Jan 21; 81(2): 340?C354 PMID: 33450210
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- Tahira Baloch, .et al. Sequential therapeutic targeting of ovarian Cancer harboring dysfunctional BRCA1, BMC Cancer, 2019, Jan 10;19(1):44 PMID: 30630446
- Khalid Hilmi, .et al. CTCF facilitates DNA double-strand break repair by enhancing homologous recombination repair, Sci Adv, 2017, May; 3(5): e1601898 PMID: 28560323
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. Structurally unique PARP-1 inhibitors for the treatment of prostate cancer, Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. Development and evaluation of poly adenosine 5'-diphosphate-ribose polymerase 1 immobilization-based receptor chromatography, J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. Development and Validation of Bioanalytical Method for Estimation of Niraparib in Rat Plasma Using High Performance LC-MS/MS And Its Application to Pharmacokinetic Study, Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. Phenotypic Switching of Atherosclerotic Smooth Muscle Cells is Regulated by Activated PARP1-Dependent TET1 Expression, J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. Forced Self-Modification Assays as a Strategy to Screen MonoPARP Enzymes, SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. Biguanides in combination with olaparib limits tumorigenesis of drug-resistant ovarian cancer cells through inhibition of Snail, Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. PARP inhibitor Olaparib Enhances the Apoptotic Potentiality of Curcumin by Increasing the DNA Damage in Oral Cancer Cells through Inhibition of BER Cascade, Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation, Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. NADP+ is an endogenous PARP inhibitor in DNA damage response and tumor suppression, Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. IGFBP-3 interacts with NONO and SFPQ in PARP-dependent DNA damage repair in triple-negative breast cancer, Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II, Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. Inhibition of PI3K-AKT-mTOR pathway sensitizes endometrial cancer cell lines to PARP inhibitors, BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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CUDC-101

Catalog No. A10246
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HDAC 抑制剂

CUDC-101是一种抑制多种靶标的新型化合物，旨在抑制HDAC，EGFR和Her2。了解更多

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ITF2357 (Givinostat)

Catalog No. A10488
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HDAC 抑制剂

ITF2357 (Givinostat)是一种HDACS抑制剂，具有潜在的抗炎、抗血管生成和抗肿瘤活性。了解更多

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Droxinostat

Catalog No. A10337
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HDAC 抑制剂

Droxinostat是HDAC3，HDAC6和HDAC8的选择性抑制剂，显示出可比较的HDAC6和HDAC8抑制作用，IC50分别为2.47和1.46μmol/ L。了解更多

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PCI-24781 (Abexinostat)

Catalog No. A10700
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HDAC 抑制剂

PCI-24781 (Abexinostat)是一种广谱苯基异羟肟酸HDAC抑制剂。了解更多

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Tubastatin A HCl

Catalog No. A11042
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HDAC6 抑制剂

Tubastatin A HCl是一种有效的选择性HDAC6抑制剂，在无细胞试验中IC50为15 nM。它对除HDAC8（57倍）以外的所有其他同工酶（1000倍）具有选择性。了解更多

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- Isin Cakir, .et al. Histone deacetylase 6 inhibition restores leptin sensitivity and reduces obesity, Nat Metab, 2022, Jan;4(1):44-59 PMID: 35039672
- Isin Cakir, .et al. Sulforaphane reduces obesity by reversing leptin resistance, Elife, 2022, Mar 24 PMID: 35323110
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Pyroxamide (NSC 696085)

Catalog No. A10764
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HDAC 抑制剂

Pyroxamide (NSC 696085)是亲和纯化的HDAC1的有效抑制剂，可导致乙酰化核心组蛋白在用该试剂培养的MEL细胞中积累。了解更多

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PCI-34051

Catalog No. A11152
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HDAC 抑制剂

PCI-34051是一种有效的特异性组蛋白脱乙酰基酶8（HDAC8）抑制剂，其选择性是其他HDAC亚型的200倍以上。了解更多

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Parthenolide ((-)-Parthenolide)

Catalog No. A10698
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Parthenolide ((-)-Parthenolide), Nuclear Factor-κB抑制剂，可特异性地耗尽HDAC1蛋白，而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。了解更多

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Tubacin

Catalog No. A10954
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HDAC6 抑制剂

Tubacin (tubulin acetylation inducer)是一种高效且选择性强，可逆，可透过细胞的HDAC6抑制剂，IC50为4 nM。了解更多

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LAQ824 (NVP-LAQ824, Dacinostat)

Catalog No. A10516
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HDAC 抑制剂

LAQ824 (NVP-LAQ824)是一种有效的新型组蛋白去乙酰化酶抑制剂，具有显著的抗多发性骨髓瘤活性。了解更多

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- De-Run Chen, .et al. Engineered nanogels simultaneously implement HDAC inhibition and chemotherapy to boost antitumor immunity via pyroptosis, Appl Mater Today, 2022, 26: 101363
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ACY-1215 (Rocilinostat)

Catalog No. A11940
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HDAC6 抑制剂

ACY-1215 (Rocilinostat)是一种选择性HDAC6抑制剂，从而通过Hsp90的超乙酰化作用破坏Hsp90蛋白伴侣系统，并防止随后的总蛋白降解。了解更多

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CI994 (Tacedinaline)

Catalog No. A11964
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HDAC 抑制剂

CI994 (Tacedinaline)是一种组蛋白脱乙酰基酶（HDAC）抑制剂，可在活细胞中诱导组蛋白超乙酰化。了解更多

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Apicidin

Catalog No. A12745
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HDAC 抑制剂

Apicidin是一种有效的组蛋白脱乙酰基酶（HDAC）抑制剂，具有潜在的抗癌活性。了解更多

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RGFP966

Catalog No. A13218
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HDAC3 抑制剂

RGFP966是一种HDAC3抑制剂，IC50为0.08μM，与其他HDAC相比，具有> 200倍的选择性。了解更多

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BRD9757

Catalog No. A12911
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HDAC6 抑制剂

BRD9757是一种高效且选择性的HDAC6抑制剂，对HDAC6的IC50为30 nM。了解更多

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Resminostat

Catalog No. A12556
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HDAC 抑制剂

Resminostat，也称为RAS2410，是一种有效的I和II类组蛋白脱乙酰基酶（HDAC）抑制剂。它结合并抑制HDAC，从而导致高度乙酰化的组蛋白的积累。选择性的抑制HDAC1/3/6，IC50为42.5 nM/50.1 nM/71.8 nM，作用于HDAC8效果弱，IC50为877 nM。了解更多

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Scriptaid

Catalog No. A12722
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HDAC 抑制剂

Scriptaid是一种HDAC抑制剂（组蛋白脱乙酰基酶）。了解更多

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Nexturastat A

Catalog No. A14032
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HDAC6 抑制剂

Nexturastat A是一种芳基脲衍生物，可作为组蛋白脱乙酰基酶6（HDAC6）的有效且高度选择性的抑制剂（IC50 = 5.02+/-0.60 nM）。了解更多

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HPOB

Catalog No. A14197
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HDAC6 抑制剂

HPOB是组蛋白去乙酰化酶6(HDAC6；IC50 = 56 nM)。了解更多

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Splitomicin

Catalog No. A14221
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NAD(+)-dependent histone deacetylase Sir2p 抑制剂

Splitomicin是一种选择性的NAD(+)-依赖性组蛋白脱乙酰基酶Sir2p抑制剂，IC50为60 uM，在基于细胞的测定中显示出更高的活性。了解更多

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Tasquinimod

Catalog No. A12616
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HDAC4 抑制剂

Tasquinimod是一种变构抑制HDAC4信号传导的口服活性抗血管生成剂。了解更多

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Santacruzamate A

Catalog No. A14236
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HDAC 抑制剂

Santacruzamate A (CAY10683)是一种有效的选择性HDAC抑制剂，对HDAC2的IC50为119 pM，选择性是其他HDAC的3600倍以上。了解更多

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LMK-235

Catalog No. A14341
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HDAC4/5 抑制剂

LMK-235是选择性组蛋白脱乙酰基酶(HDAC) 4和HDAC5抑制剂。了解更多

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ST7612AA1

Catalog No. A14418
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HDAC 抑制剂

ST7612AA1是新型的有效HDAC抑制剂，具有潜在的抗癌活性。了解更多

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Domatinostat (4SC-202)

Catalog No. A14354
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HDAC 抑制剂

4SC-202是生物利用的苯甲酰胺和人I类组蛋白脱乙酰基酶（HDACs）同工酶1、2和3的抑制剂，具有潜在的抗肿瘤活性。了解更多

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TMP 195

Catalog No. A14326
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HDAC 抑制剂

TMP195是最有效和选择性的IIa类HDAC抑制剂。了解更多

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BRD73954

Catalog No. A15489
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HDAC 抑制剂

BRD73954是一种小分子抑制剂，可有效抑制HDAC6和HDAC8（IC50分别为36和120 nM）。了解更多

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UF010

Catalog No. A15781
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HADC 抑制剂

UF010是一种有效的选择性HADC抑制剂，对于HDAC 3、2、1和8分别具有IC50?0.06 uM，0.1 uM，0.5 uM和1.5 uM。它的选择性是其他HDAC的6倍以上。了解更多

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HDAC inhibitor

Catalog No. A13405
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HDAC 抑制剂

N/A 了解更多

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CAY10603

Catalog No. A16431
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HDAC6 抑制剂

CAY10603是一种有效的选择性HDAC6抑制剂，IC50为2 pM，选择性是其他HDAC的200倍以上。了解更多

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SR-4370

Catalog No. A16899
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HDAC 抑制剂

SR-4370是HDAC抑制剂。SR-4370对HDAC1，HDAC2和HDAC3的IC50值分别为0.5 uM，0.1 uM和0.06 uM。了解更多

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HDAC8-IN-1

Catalog No. A17091
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HDAC8 抑制剂

HDAC8-IN-1是一种HDAC8抑制剂，在癌细胞系中的IC50为27.2 nM。了解更多

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Tinostamustine (EDO-S101)

Catalog No. A18342
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HDAC inhibitor

EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively. 了解更多

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SKLB-23bb

Catalog No. A18339
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HDAC6 inhibitor

SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively. 了解更多

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Valproic acid

Catalog No. A17323
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HDAC inhibitor

Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. 了解更多

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- Dan Zhao, .et al. From crypts to enteroids: establishment and characterization of avian intestinal organoids, Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
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Tucidinostat (Chidamide)

Catalog No. A17861
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HDAC inhibitor

Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9. 了解更多

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CM-675

Catalog No. A18741
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PDE5/HDAC-1 inhibitor

CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer??s disease. 了解更多

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