Histone H2AX Inhibitors
Chemical inhibitors of Histone H2AX play a crucial role in modulating the protein's function in response to DNA damage. KU-55933, CP-466722, and Mirin are compounds that target the activation pathways of Histone H2AX. KU-55933 and CP-466722 directly inhibit ATM kinase, an enzyme that phosphorylates Histone H2AX as part of the cellular response to DNA strand breaks. By blocking ATM kinase activity, these inhibitors prevent the phosphorylation of Histone H2AX, thereby hindering its role in signaling and coordinating DNA repair processes. Mirin, on the other hand, indirectly affects Histone H2AX by targeting the Mre11-Rad50-Nbs1 complex, which is essential for the activation of ATM kinase. By inhibiting this complex, Mirin disrupts the upstream signaling that leads to Histone H2AX phosphorylation.
Similarly, VE-821 and CGK733 inhibit ATR kinase, another enzyme capable of modifying Histone H2AX in response to DNA damage, particularly during replication stress. These inhibitors preclude the phosphorylation of Histone H2AX by ATR kinase, impacting the protein's involvement in the DNA damage response. DNA-PKcs, which also phosphorylates Histone H2AX, is targeted by NU7441 and NU7026, both of which inhibit DNA-PK activity and consequently the phosphorylation of Histone H2AX that is critical for DNA repair via non-homologous end joining. Wortmannin and LY294002 are broader PI3K inhibitors that, at higher concentrations, can inhibit ATM and DNA-PKcs, leading to a reduction in Histone H2AX phosphorylation. Additionally, Caffeine at high concentrations can inhibit both ATM and ATR kinases, impacting Histone H2AX activation. Lastly, Chk2 Inhibitor II and SCH900776 interrupt the signaling cascades involving Chk2 and CHK1 kinases, respectively, both of which can phosphorylate Histone H2AX, thus affecting the protein's function in the context of DNA damage signaling.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
ATM Kinase Inhibitor | 587871-26-9 | sc-202963 | 2 mg | $110.00 | 28 | |
KU-55933 is an ATM kinase inhibitor. ATM kinase is responsible for phosphorylating Histone H2AX at serine 139. By inhibiting ATM kinase, KU-55933 prevents the phosphorylation of Histone H2AX, thereby inhibiting its activation in DNA damage response. | ||||||
VE 821 | 1232410-49-9 | sc-475878 | 10 mg | $360.00 | ||
VE-821 is an ATR kinase inhibitor. ATR kinase, like ATM, can also phosphorylate Histone H2AX as part of the DNA damage response. VE-821 inhibits ATR kinase activity, which in turn inhibits the phosphorylation and thus the function of Histone H2AX. | ||||||
MRN-ATM Pathway Inhibitor, Mirin | 299953-00-7 | sc-203144 | 10 mg | $141.00 | 4 | |
Mirin is an inhibitor of the Mre11-Rad50-Nbs1 (MRN) complex, which is involved in the activation of ATM kinase. By inhibiting this complex, Mirin indirectly inhibits the phosphorylation of Histone H2AX by preventing ATM kinase activation. | ||||||
NU 7441 | 503468-95-9 | sc-208107 | 5 mg | $357.00 | 10 | |
NU7441 is a DNA-PKcs inhibitor. DNA-PKcs is involved in the non-homologous end joining pathway of DNA repair and can phosphorylate Histone H2AX. Inhibiting DNA-PKcs with NU7441 prevents this phosphorylation, inhibiting Histone H2AX function. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin is a PI3K inhibitor that also inhibits DNA-PKcs and ATM kinases at higher concentrations. By inhibiting these kinases, Wortmannin prevents the phosphorylation of Histone H2AX, thereby inhibiting its role in DNA repair processes. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is another PI3K inhibitor that, similar to Wortmannin, can inhibit ATM and DNA-PKcs, leading to the inhibition of Histone H2AX phosphorylation and thereby its function in DNA 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 is known to inhibit ATM and ATR kinases at high concentrations. Through this inhibition, caffeine can prevent the phosphorylation of Histone H2AX, thus inhibiting its function in the cellular response to DNA damage. | ||||||
ATM/ATR Kinase Inhibitor Inhibitor | 905973-89-9 | sc-202964 | 5 mg | $106.00 | 8 | |
CGK733 is an inhibitor of both ATM and ATR kinases. By inhibiting these kinases, CGK733 prevents the activation of Histone H2AX through phosphorylation, thus inhibiting its function in the DNA damage response. | ||||||
DNA-PK Inhibitor II | 154447-35-5 | sc-202143 sc-202143A | 10 mg 50 mg | $155.00 $660.00 | 6 | |
NU7026 is a DNA-PK inhibitor. Inhibiting DNA-PK with NU7026 leads to reduced phosphorylation of Histone H2AX, thereby inhibiting its function in DNA repair. | ||||||
BML-277 | 516480-79-8 | sc-200700 sc-200700A | 10 mg 50 mg | $132.00 $492.00 | 2 | |
Chk2 Inhibitor II targets Chk2 kinase, which is involved in DNA damage signaling and can phosphorylate Histone H2AX. Inhibition of Chk2 can thus lead to decreased Histone H2AX function in DNA damage repair pathways. | ||||||