Rad50 Inhibitors
The chemical class encompassing Rad50 inhibitors is diverse, containing compounds that indirectly affect Rad50 function by modulating various components of the DNA damage response (DDR) and repair pathways. These inhibitors exert their influence by targeting key enzymes and proteins that are integral to the activation and operation of the DNA repair machinery, in which Rad50 plays a crucial structural and signaling role. The chemicals act on different stages of the DDR, from initial damage detection and signaling to the final steps of repair completion.
The majority of the compounds listed target the enzymatic activities of kinases such as DNA-PK, ATM, and ATR, which are pivotal in the phosphorylation-driven signaling cascades that facilitate the DDR. By inhibiting these kinases, the compounds disrupt the signaling required for the assembly and activation of the MRN complex, subsequently impeding Rad50's function. Additionally, some of the inhibitors work by modulating the stability and activity of the MRN complex directly, such as Mirin, or by influencing the expression of its components, such as Schisandrin B. The ultimate effect of these inhibitory actions is a reduction in Rad50's ability to aid in the repair of DNA breaks, particularly in the processes of homologous recombination and NHEJ, by destabilizing the complex or impairing its recruitment and activation. The precise mechanisms of these inhibitors are a testament to the intricate nature of DDR pathways and highlight the critical role of post-translational modifications such as phosphorylation in regulating protein functions during DNA repair.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
MRN-ATM Pathway Inhibitor, Mirin | 299953-00-7 | sc-203144 | 10 mg | $141.00 | 4 | |
Mirin interferes with the Mre11-Rad50-Nbs1 complex by inhibiting the Mre11 endonuclease activity, which is necessary for the activation of the DNA damage response. Since Rad50 forms a complex with Mre11, its function is indirectly hindered due to the compromised activity of Mre11, leading to ineffective DNA repair and inhibition of Rad50’s role in homologous recombination repair. | ||||||
DNA-PK Inhibitor II | 154447-35-5 | sc-202143 sc-202143A | 10 mg 50 mg | $155.00 $660.00 | 6 | |
DNA-PK Inhibitor II compromises non-homologous end joining (NHEJ), a pathway where Rad50 plays a scaffolding role. By inhibiting DNA-PK, NU7026 prevents the proper assembly of the DNA-PK holoenzyme complex, thus indirectly affecting Rad50’s ability to assist in the bridging and subsequent repair of DNA breaks. | ||||||
NU 7441 | 503468-95-9 | sc-208107 | 5 mg | $357.00 | 10 | |
NU7441, like NU7026, targets DNA-PK, essential for NHEJ. By effectively reducing DNA-PK’s kinase activity, NU7441 disrupts the signaling necessary for the recruitment and action of repair proteins, including Rad50, ultimately impeding the DNA repair process wherein Rad50 is a critical player. | ||||||
ATM Kinase Inhibitor | 587871-26-9 | sc-202963 | 2 mg | $110.00 | 28 | |
ATM Kinase Inhibitor blocks the activity of ATM, a kinase that phosphorylates various substrates involved in the DNA damage response. By inhibiting ATM, KU55933 downregulates the DNA damage signal cascade, which includes the recruitment and activation of the MRN complex. As a result, Rad50’s function in signaling and repair of DNA breaks is indirectly inhibited. | ||||||
KU 60019 | 925701-46-8 | sc-363284 sc-363284A | 10 mg 50 mg | $248.00 $1035.00 | 1 | |
This inhibitor acts on ATM and reduces ATM-mediated signaling in response to DNA damage. By diminishing ATM kinase activity, KU60019 lessens the phosphorylation and activation of downstream targets that are involved in the coordination of DNA repair, thereby indirectly reducing Rad50’s capacity to contribute to DNA damage repair processes. | ||||||
VE 821 | 1232410-49-9 | sc-475878 | 10 mg | $360.00 | ||
VE-821 is an ATR inhibitor that, by inhibiting ATR kinase activity, dampens the homologous recombination repair process. ATR is responsible for the activation of several downstream repair proteins, and its inhibition indirectly hinders Rad50’s function in DNA repair since the complex to which Rad50 belongs is activated and recruited as part of the ATR-mediated DNA damage response. | ||||||
ATM/ATR Kinase Inhibitor Inhibitor | 905973-89-9 | sc-202964 | 5 mg | $106.00 | 8 | |
ATM/ATR Kinase Inhibitor impairs the activation of the DNA damage response, which is critical for the recruitment and proper functioning of the MRN complex that Rad50 is a part of. Thus, the inhibition of ATM and ATR by CGK733 indirectly prevents Rad50 from executing its role in DNA repair. | ||||||
Deoxyschizandrin | 61281-38-7 | sc-278925 | 10 mg | $80.00 | ||
Deoxyschizandrin has been shown to inhibit the expression of Mre11, a component of the MRN complex. By reducing Mre11 levels, Schisandrin B indirectly impedes the MRN complex’s assembly and function, which is crucial for Rad50’s activity in DNA repair and homologous recombination. | ||||||