DNA pol θ Inhibitors
DNA polymerase θ (pol θ) inhibitors constitute a versatile array of compounds with distinct mechanisms that intricately modulate the enzyme's involvement in DNA synthesis and repair. Aphidicolin, a tetracyclic diterpenoid, directly inhibits DNA pol θ by binding to its active sites, disrupting polymerase activity and impeding the fidelity of DNA synthesis. Mirin, a small molecule, offers another avenue of direct inhibition by disrupting the interaction between DNA pol θ and DNA ends, impairing DNA synthesis and repair. Furthermore, indirect inhibition of DNA pol θ is achieved through compounds like NU7026, a DNA-dependent protein kinase (DNA-PK) inhibitor. NU7026 disrupts the non-homologous end-joining (NHEJ) pathway, limiting the availability of DNA pol θ during repair processes. RAD51-stimulatory compound RS-1 indirectly modulates DNA pol θ by enhancing homologous recombination (HR), competing with alternative repair pathways. In contrast, RAD51 inhibitor B02 suppresses HR, diverting repair processes away from DNA pol θ.
Thymidine analogs, including AZT, indirectly influence DNA pol θ by inhibiting reverse transcriptases, impacting the availability of DNA substrates. Wortmannin, a phosphoinositide 3-kinase (PI3K) inhibitor, disrupts the PI3K-related kinase (PIKK) signaling pathway, indirectly hampering the activation of DNA repair factors. Caffeine modulates the ATM/ATR pathway, indirectly influencing DNA pol θ through interference with cell cycle checkpoint activation. Furthermore, ATR kinase inhibitors like AZ20 and KU-55933 disrupt the ATR pathway, indirectly modulating DNA pol θ's participation in DNA synthesis and repair. Additionally, ATM kinase inhibitors such as KU-0060648 influence DNA pol θ by disrupting the ATM pathway, limiting the activation of DNA repair factors. CGK 733, a checkpoint kinase 2 (Chk2) inhibitor, indirectly impacts DNA pol θ by disrupting the Chk2 signaling pathway and influencing the enzyme's availability during repair processes. In conclusion, the diverse landscape of DNA pol θ inhibitors showcases their intricate mechanisms, encompassing both direct interference with the polymerase and indirect modulation through pivotal cellular pathways.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Aphidicolin | 38966-21-1 | sc-201535 sc-201535A sc-201535B | 1 mg 5 mg 25 mg | $84.00 $306.00 $1104.00 | 30 | |
Aphidicolin, a tetracyclic diterpenoid, inhibits DNA synthesis by binding to DNA polymerase active sites, preventing DNA pol θ engagement. This direct inhibition hampers polymerase activity and impedes the fidelity of DNA synthesis. | ||||||
MRN-ATM Pathway Inhibitor, Mirin | 299953-00-7 | sc-203144 | 10 mg | $141.00 | 4 | |
Mirin, a small molecule, inhibits DNA pol θ enzymatic activity by disrupting its interaction with DNA ends. This direct inhibition interferes with the polymerase's role in the DNA repair process, leading to impaired DNA synthesis and repair. | ||||||
DNA-PK Inhibitor II | 154447-35-5 | sc-202143 sc-202143A | 10 mg 50 mg | $155.00 $660.00 | 6 | |
NU7026, a DNA-dependent protein kinase (DNA-PK) inhibitor, indirectly inhibits DNA pol θ by disrupting the non-homologous end-joining (NHEJ) pathway. This disruption limits the availability of DNA pol θ during repair processes, indirectly modulating its engagement in DNA synthesis and repair. | ||||||
RAD51 Inhibitor B02 | 1290541-46-6 | sc-507533 | 10 mg | $95.00 | ||
B02, a RAD51 inhibitor, indirectly influences DNA pol θ by suppressing homologous recombination (HR). Reduced HR activity diverts repair processes away from DNA pol θ, indirectly affecting its involvement in DNA synthesis and repair. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin, a phosphoinositide 3-kinase (PI3K) inhibitor, indirectly inhibits DNA pol θ by disrupting the PI3K-related kinase (PIKK) signaling pathway. This interference hampers the activation of DNA repair factors, indirectly modulating the participation of DNA pol θ in DNA synthesis and repair. | ||||||
Caffeine | 58-08-2 | sc-202514 sc-202514A sc-202514B sc-202514C sc-202514D | 50 g 100 g 250 g 1 kg 5 kg | $33.00 $67.00 $97.00 $192.00 $775.00 | 13 | |
Caffeine, an adenosine receptor antagonist, indirectly influences DNA pol θ by modulating the ATM/ATR pathway. This interference with cell cycle checkpoint activation indirectly modulates the availability of DNA pol θ during repair processes, impacting its role in DNA synthesis and repair. | ||||||
AZ20 | 1233339-22-4 | sc-503186 | 5 mg | $255.00 | 1 | |
AZ20, an ATR kinase inhibitor, indirectly inhibits DNA pol θ by disrupting the ataxia-telangiectasia and Rad3-related (ATR) pathway. This interference limits the activation of DNA repair factors, indirectly modulating the participation of DNA pol θ in DNA synthesis and repair. | ||||||
ATM Kinase Inhibitor | 587871-26-9 | sc-202963 | 2 mg | $110.00 | 28 | |
KU-55933, an ATM kinase inhibitor, indirectly inhibits DNA pol θ by disrupting the ataxia-telangiectasia mutated (ATM) pathway. This interference limits the activation of DNA repair factors, indirectly modulating the engagement of DNA pol θ in DNA synthesis and repair. | ||||||
ATM/ATR Kinase Inhibitor Inhibitor | 905973-89-9 | sc-202964 | 5 mg | $106.00 | 8 | |
CGK 733, a checkpoint kinase 2 (Chk2) inhibitor, indirectly inhibits DNA pol θ by disrupting the Chk2 signaling pathway. This interference with cell cycle checkpoints indirectly modulates the availability of DNA pol θ during repair processes, impacting its role in DNA synthesis and repair. | ||||||