53BP1 Activators
The chemical class of 53BP1 activators encompasses a diverse range of compounds that influence 53BP1 activity through distinct mechanisms. These activators can be broadly categorized into DNA damage-inducing agents, cell cycle regulators, and inhibitors of key signaling proteins involved in the DNA damage response.DNA damage-inducing agents such as Methyl Methanesulfonate (MMS), Bleomycin, Etoposide, Cisplatin, and Camptothecin directly cause DNA lesions, leading to the recruitment and activation of 53BP1 at sites of damage. These compounds represent a class of genotoxic agents that trigger the cellular machinery involved in DNA repair, with 53BP1 playing a crucial role in orchestrating repair processes.
Cell cycle regulators like Palbociclib and Olaparib indirectly activate 53BP1 by influencing cell cycle dynamics and DNA repair pathways. Palbociclib induces cell cycle arrest by inhibiting CDK4/6, promoting DNA damage accumulation and subsequent 53BP1 activation. Olaparib, on the other hand, disrupts PARP-mediated DNA repair, leading to synthetic lethality and increased reliance on alternative repair pathways involving 53BP1. Inhibitors of key signaling proteins such as NU7026, NSC 207895, AZ20, A-196, and ATM Kinase Inhibitor (KU-55933) modulate 53BP1 activity by targeting specific components of the DNA damage response pathway. These compounds disrupt key kinases or histone methyltransferases, affecting the signaling cascade and leading to the activation of 53BP1 as part of an alternative response mechanism.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
DNA-PK Inhibitor II | 154447-35-5 | sc-202143 sc-202143A | 10 mg 50 mg | $155.00 $660.00 | 6 | |
DNA-PK Inhibitor II (NU7026) is a selective DNA-PK inhibitor that indirectly influences 53BP1 activation. By inhibiting DNA-PK activity, NU7026 disrupts the non-homologous end joining (NHEJ) pathway, leading to increased reliance on 53BP1-mediated repair mechanisms. This compound alters the balance between homologous recombination and NHEJ, indirectly activating 53BP1 by promoting its recruitment to DNA damage sites and facilitating its role in DNA repair processes. | ||||||
Methyl methanesulfonate | 66-27-3 | sc-250376 sc-250376A | 5 g 25 g | $56.00 $133.00 | 2 | |
Methyl Methanesulfonate (MMS) is an alkylating agent that induces DNA damage, triggering the activation of DNA repair pathways, including those involving 53BP1. MMS causes DNA alkylation, leading to the formation of DNA lesions. In response to this genotoxic stress, 53BP1 is recruited to damaged DNA sites, initiating repair processes. | ||||||
NSC-207895 | 58131-57-0 | sc-364550 sc-364550A | 5 mg 10 mg | $354.00 $666.00 | ||
NSC 207895, also known as MI-63, is a small molecule inhibitor of MDM2, a negative regulator of p53. By inhibiting MDM2, NSC 207895 stabilizes p53 and enhances its transcriptional activity. The activation of p53, in turn, influences downstream effectors, including 53BP1, which plays a role in DNA damage response pathways. The indirect activation of 53BP1 by NSC 207895 is linked to the stabilization and activation of p53. | ||||||
Bleomycin | 11056-06-7 | sc-507293 | 5 mg | $275.00 | 5 | |
Bleomycin is an anti-tumor antibiotic that induces DNA strand breaks, leading to DNA damage. The genotoxic effects of bleomycin activate DNA repair mechanisms, including the involvement of 53BP1 in response to double-strand breaks. The indirect activation of 53BP1 by bleomycin is mediated through its ability to induce DNA damage, resulting in the recruitment of 53BP1 to damaged DNA sites. | ||||||
Palbociclib | 571190-30-2 | sc-507366 | 50 mg | $321.00 | ||
PD 0332991 is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), leading to cell cycle arrest. The indirect activation of 53BP1 by palbociclib is associated with its impact on cell cycle dynamics. By inhibiting CDK4/6, palbociclib disrupts the cell cycle progression, promoting DNA damage accumulation and activating DNA repair pathways. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $51.00 $231.00 $523.00 | 63 | |
Etoposide is a topoisomerase II inhibitor that induces DNA damage, particularly DNA double-strand breaks. The genotoxic effects of etoposide activate DNA repair pathways, including the involvement of 53BP1 in the repair of double-strand breaks. The indirect activation of 53BP1 by etoposide is mediated through its ability to induce DNA damage, resulting in the recruitment of 53BP1 to damaged DNA sites. | ||||||
Cisplatin | 15663-27-1 | sc-200896 sc-200896A | 100 mg 500 mg | $138.00 $380.00 | 101 | |
Cisplatin is a platinum-based chemotherapeutic agent that induces DNA damage, particularly DNA cross-links. The genotoxic effects of cisplatin activate DNA repair pathways, including the involvement of 53BP1 in response to DNA lesions. The indirect activation of 53BP1 by cisplatin is mediated through its ability to induce DNA damage, resulting in the recruitment of 53BP1 to damaged DNA sites. | ||||||
Camptothecin | 7689-03-4 | sc-200871 sc-200871A sc-200871B | 50 mg 250 mg 100 mg | $58.00 $186.00 $94.00 | 21 | |
Camptothecin is a topoisomerase I inhibitor that induces DNA damage by causing DNA strand breaks. The genotoxic effects of camptothecin activate DNA repair pathways, including the involvement of 53BP1 in the repair of DNA lesions. The indirect activation of 53BP1 by camptothecin is mediated through its ability to induce DNA damage, resulting in the recruitment of 53BP1 to damaged DNA sites. | ||||||
AZ20 | 1233339-22-4 | sc-503186 | 5 mg | $255.00 | 1 | |
AZ20 is a small molecule inhibitor of ATR (ataxia-telangiectasia and Rad3-related protein kinase). By inhibiting ATR, AZ20 disrupts the DNA damage response pathway, leading to the activation of alternative pathways, including those involving 53BP1. The indirect activation of 53BP1 by AZ20 is linked to the perturbation of ATR-dependent signaling, emphasizing the intricate network of kinases and regulators that modulate 53BP1 activity in response to DNA damage. | ||||||
Olaparib | 763113-22-0 | sc-302017 sc-302017A sc-302017B | 250 mg 500 mg 1 g | $210.00 $305.00 $495.00 | 10 | |
Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor that induces synthetic lethality in cells with DNA repair defects. The indirect activation of 53BP1 by olaparib is associated with its impact on the PARP-mediated DNA repair pathway. By inhibiting PARP, olaparib disrupts DNA repair processes, leading to increased reliance on alternative pathways involving 53BP1. | ||||||