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DNA repair inhibitors and activators act on enzymes that detect and fix damaged bases and broken strands. A 1993 review estimated that hydrolysis and oxidation damage thousands of DNA bases in every cell each day. In base excision repair, 8-oxoguanine DNA glycosylase 1 (OGG1) excises oxidized guanine, and apurinic/apyrimidinic endonuclease 1 (APE1) then cuts the abasic site. TH10785 is listed as an OGG1 activator, whereas APE1-IN-1 inhibits APE1. DNA repair protein RAD52 homolog (RAD52) became a target after a 2011 study found its loss lethal in cells lacking breast cancer susceptibility protein 2 (BRCA2). D-I03 inhibits RAD52, HAMNO blocks replication protein A (RPA), and CD00509 inhibits tyrosyl-DNA phosphodiesterase 1 (TDP1).
Synonyms: O6-benzyl guanine; O6-BG
KRX-0402 is a small molecule that was specifically designed to block the DNA repair protein, MGMT. MGMT confers resistance to certain alkylating agents, such as temozolomide and BCNU, that are commonly used to treat brain cancer, melanoma and non-Hodgkin–s lymphoma.
Synonyms: NSC111847
HAMNO, also known as NSC-111847, is a potent and selective inhibitor of replication protein A (RPA) interactions with proteins involved in the replication stress response.
CD00509 is a potent inhibitor of the tyrosyl-DNA phosphodiesterase Tdp1, exhibiting an IC50 value of 0.71 μM. By increasing DNA damage, CD00509 promotes apoptosis in MCF-7 breast cancer cells and sensitizes both breast cancer cells and wild-type murine embryonic fibroblasts (MEFs) to Camptothecin (CPT). This compound serves as a valuable tool for investigating therapeutic strategies in breast cancer research and understanding the role of Tdp1 in cellular response to DNA damage.
PCNA-I1 is a selective inhibitor of proliferating cell nuclear antigen (PCNA) that exhibits significant anticancer activity. By stabilizing the PCNA trimer structure (Kd = 0.14-0.41 μM) and impairing its interaction with chromatin, PCNA-I1 effectively induces cell cycle arrest, inhibits DNA replication and repair, and enhances the efficacy of DNA-damaging agents. This compound is particularly useful for research applications targeting prostate cancer, lung cancer, and various other tumors.
APE1-IN-2 is a potent inhibitor of apurinic/apyrimidinic endonuclease 1 (APE1), a key player in the base excision repair (BER) pathway. This compound demonstrates significant anticancer activity by facilitating intracellular accumulation of platinum and triggering DNA damage response mechanisms, leading to apoptosis. APE1-IN-2 is valuable for research applications focused on cancer biology and the modulation of DNA repair processes.
C791-0064 is a selective inhibitor of RAD52, which acts by binding to the protein and disrupting its single-strand annealing activity. This compound is particularly effective in inhibiting the proliferation of cancer cells exhibiting BRCA2 deficiency, leading to increased DNA damage and subsequent apoptosis. C791-0064 serves as a valuable tool for investigating mechanisms associated with BRCA mutation-related cancers, including breast and ovarian cancer.
Anti-osteoporosis agent-1 is a potent inhibitor of replication protein A (RPA), with an IC50 of 18 µM. This compound exhibits significant biological activity in modulating DNA replication and repair processes. Its primary research applications include studies on cellular response to DNA damage and the exploration of therapeutic strategies for osteoporosis-related conditions.
D-I03 is a selective inhibitor of RAD52, exhibiting a Kd of 25.8 μM. This compound effectively disrupts RAD52-dependent single-strand annealing and D-loop formation, with IC50 values of 5 μM and 8 μM, respectively. D-I03 has been shown to suppress the growth of BRCA1- and BRCA2-deficient cell lines and inhibits the formation of damage-induced RAD52 foci without impacting RAD51 foci formation induced by Cisplatin. This reagent is valuable for research exploring DNA repair mechanisms and the role of RAD52 in cancer biology.
TH10785 is an OGG1 (8-oxoguanine glycosylase 1) activator that enhances enzymatic activity by interacting with specific amino acids, phenylalanine-319 and glycine-42. This compound facilitates β, δ-lyase functions, allowing for effective processing of oxidative DNA lesions. TH10785 is valuable for research into diseases associated with DNA damage and the aging process, providing insights into cellular repair mechanisms and potential therapeutic targets.
APE1-IN-1 is a selective inhibitor of apurinic/apyrimidinic (AP) endonuclease 1 (APE1), known for its ability to penetrate the blood-brain barrier. With an IC50 value of 2 μM, this compound enhances the cytotoxic effects of alkylating agents such as Methylmethane sulfonate and Temozolomide in cancer cells. APE1-IN-1 is valuable for research into cancer therapeutics and the roles of DNA repair mechanisms in tumor progression and treatment resistance.
T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that disrupts DNA repair mechanisms, leading to an increased formation of double-strand breaks (DSBs). This compound promotes necroptosis and induces cell cycle arrest in the G1 phase, making it a valuable tool for research focused on cell death and DNA damage response pathways. T2AA can be utilized in studies investigating the effects of inhibited PCNA activity on genomic stability and cellular proliferation.
TDRL-551 is a potent inhibitor of replication protein A (RPA), exhibiting an IC50 of 18 µM. This compound disrupts the interaction between RPA and DNA, thereby enhancing the efficacy of platinum-based chemotherapy agents in cancer treatment. TDRL-551 is particularly relevant for research in cancers like non-small cell lung cancer (NSCLC), providing insights into strategies for overcoming chemoresistance.
UNC9512 is a potent antagonist of the methyl-lysine reader protein 53BP1, which plays a crucial role in the DNA damage response. This compound can be utilized to investigate the functions of 53BP1 in various biological processes, including DNA repair mechanisms, gene editing efficiencies, and tumorigenesis. Its application supports research aimed at understanding the underlying molecular pathways related to genomic stability and cancer development.
6-Hydroxy-DOPA is a selective allosteric inhibitor of the RAD52 single-stranded DNA binding domain. This compound has demonstrated significant inhibition of RAD52 activity, making it a valuable tool for cancer research. Its role in modulating DNA repair processes offers insights into therapeutic strategies targeting RAD52-associated pathways.
UNC-2170 is a selective fragment-like ligand targeting 53BP1, exhibiting an IC50 of 29 µM and a Kd of 22 µM. With over 17-fold selectivity against nine other methyl-lysine reader proteins, UNC-2170 effectively binds to 53BP1, a key player in DNA Damage Repair (DDR) pathways. Its primary application lies in studying the recruitment of 53BP1 to double-strand breaks (DSB), facilitating research in genomic stability and repair mechanisms.
NSC15520 is a selective inhibitor of Replication Protein A (RPA), targeting its N-terminal DNA binding domain (DBD). This compound effectively disrupts the interaction between RPA and key proteins such as p53 and RAD9, thus interfering with critical cellular processes. NSC15520 also prevents the helix destabilization of duplex DNA oligonucleotides, making it a valuable tool for studies in DNA replication, repair, recombination, and damage response signaling pathways.
Synonyms: BMH-23
AR03 is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor, exhibiting an IC50 of 2.1 µM. It selectively targets the Ape1 enzyme with low affinity for double-stranded DNA. This compound enhances the cytotoxic effects of methyl methanesulfonate and temozolomide in SF767 cells, making it a valuable tool for studying DNA damage response and repair mechanisms in cancer research.
PCNA-IN-1 is a selective inhibitor of the PCNA/PIP-box interaction, demonstrating an IC50 greater than 50 μM. This compound is primarily utilized in cancer research, offering potential insights into the mechanisms of cell proliferation and tumor progression. Its ability to disrupt protein interactions makes it a valuable tool for studying the role of PCNA in various malignancies.
APE1-IN-3 is a selective inhibitor of apurinic/apyrimidinic endonuclease 1 (APE1), a crucial enzyme involved in DNA repair and cellular response to oxidative stress. This compound exhibits significant biologic activity in impairing APE1 function, thereby facilitating the understanding of its role in cancer biology. APE1-IN-3 is applicable in research aimed at elucidating the mechanisms of tumorigenesis and exploring potential therapeutic strategies targeting DNA repair pathways in cancer.
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UNC-2170 maleate is a selective inhibitor of the methyl-lysine binding protein 53BP1, with an IC50 value of 29 µM and a Kd of 22 µM. This compound demonstrates a remarkable 17-fold selectivity for 53BP1 compared to nine other methyl-lysine reader proteins. 53BP1 is crucial in DNA Damage Repair (DDR) mechanisms and is recruited to sites of double-strand breaks (DSB), making UNC-2170 maleate a valuable tool for research in DNA repair processes and related cellular pathways.
T2AA hydrochloride is a small molecule inhibitor targeting proliferating cell nuclear antigen (PCNA). It effectively disrupts the interaction between PCNA and PIP-box peptides with an IC50 of approximately 1 μM, as well as inhibiting the binding of PCNA to full-length p21 protein. This compound is valuable for research applications related to cell cycle regulation and cancer biology.
Lucanthone is a selective inhibitor of Apurinic endonuclease-1 (APE-1), targeting its endonuclease activity. This compound exhibits significant anti-tumor properties through its ability to enhance DNA damage sensitivity in cancer cells. Lucanthone has applications in cancer research, particularly in studies focused on DNA repair mechanisms and the therapeutic modulation of cellular responses to DNA-damaging agents.
Lucanthone hydrochloride is an inhibitor of Apurinic endonuclease-1 (APE-1), a key enzyme involved in the base excision repair pathway. This compound demonstrates significant biological activity by facilitating the accumulation of DNA lesions, thereby enhancing cellular sensitivity to DNA-damaging agents. Lucanthone hydrochloride is commonly utilized in research studies focused on DNA repair mechanisms, cancer therapy, and oxidative stress responses.
TDP1 Inhibitor-3 is a selective inhibitor of Tyrosyl-DNA Phosphodiesterase 1 (TDP1), demonstrating an IC50 value of 0.63 μM. This compound exhibits potent activity in preventing TDP1-mediated DNA repair, making it a valuable tool for investigating the role of TDP1 in cellular processes. It is particularly applicable in cancer research and studies focusing on DNA damage response mechanisms.
TDP1 Inhibitor-2 is a selective inhibitor of tyrosyl-DNA phosphodiesterase 1 (TDP1), demonstrating potent inhibition with an IC50 value of 99 nM. Additionally, it exhibits inhibitory effects on SCAN1, presenting an IC50 of 3.5 μM. This compound is valuable for studying DNA repair mechanisms and exploring therapy potential in related neurodegenerative conditions.
