Histone H2A.X Activators
Histone H2A.X is a crucial component of chromatin, functioning primarily in the cellular response to DNA damage. Upon encountering DNA double-strand breaks (DSBs), H2A.X becomes phosphorylated at serine 139 to form γ-H2A.X, marking the site of DNA damage and initiating the DNA repair process. This phosphorylation event triggers a cascade of cellular events, leading to the recruitment of DNA repair proteins to the site of damage. γ-H2A.X acts as a scaffold for the assembly of repair complexes, facilitating both homologous recombination and non-homologous end joining repair pathways. Additionally, γ-H2A.X plays a vital role in signaling pathways that induce cell cycle arrest, allowing time for DNA repair mechanisms to operate effectively. By halting the cell cycle, γ-H2A.X prevents the propagation of damaged DNA and reduces the risk of genomic instability and tumorigenesis.
Activation of Histone H2A.X is primarily driven by the DNA damage response pathway. Various factors, including genotoxic stressors such as ionizing radiation, UV light, and chemical agents, induce DNA damage and trigger the activation of kinases such as ATM (ataxia telangiectasia mutated) and ATR (ataxia telangiectasia and Rad3-related protein). These kinases phosphorylate H2A.X at the site of DNA damage, leading to the formation of γ-H2A.X. Additionally, chromatin remodeling complexes and histone-modifying enzymes can influence the accessibility of H2A.X for phosphorylation, further regulating its activation. The activation of H2A.X serves as a critical step in the cellular response to DNA damage, ensuring efficient repair and maintenance of genomic integrity.
SEE ALSO...
Items 1 to 10 of 11 total
Display:
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
A-485 | 1889279-16-6 | sc-507493 | 5 mg | $275.00 | ||
A-485 is a potent and selective inhibitor of the histone deacetylase 7 (HDAC7) enzyme. HDAC7 is known to negatively regulate H2A.X phosphorylation. By inhibiting HDAC7, A-485 promotes an environment conducive to increased H2A.X phosphorylation, a crucial step in the cellular response to DNA damage. | ||||||
DNA-PK Inhibitor II | 154447-35-5 | sc-202143 sc-202143A | 10 mg 50 mg | $155.00 $660.00 | 6 | |
DNA-PK Inhibitor II is a specific DNA-dependent protein kinase (DNA-PK) inhibitor. DNA-PK is implicated in the phosphorylation of H2A.X in response to DNA double-strand breaks. By inhibiting DNA-PK, this compound disrupts the signaling pathway leading to H2A.X phosphorylation, indirectly affecting the activation of H2A.X in DNA repair processes. | ||||||
BAY 87-2243 | 1227158-85-1 | sc-507483 | 5 mg | $100.00 | ||
BAY 87-2243 is a selective inhibitor of the hypoxia-inducible factor (HIF) pathway, specifically targeting HIF-1α. H2A.X activation is influenced by cellular responses to hypoxia, and by inhibiting HIF-1α, BAY 87-2243 disrupts the signaling cascade leading to H2A.X phosphorylation, providing an indirect means of modulating H2A.X activation. | ||||||
Cisplatin | 15663-27-1 | sc-200896 sc-200896A | 100 mg 500 mg | $76.00 $216.00 | 101 | |
Cisplatin is a platinum-based chemotherapeutic agent that induces DNA damage, including the formation of DNA adducts. The cellular response to this damage involves the phosphorylation of H2A.X. Cisplatin's mechanism of action indirectly activates H2A.X by inducing DNA lesions, triggering the ataxia-telangiectasia mutated (ATM) kinase pathway and subsequent H2A.X phosphorylation in the DNA damage response. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a potent and selective inhibitor of p38 mitogen-activated protein kinase (MAPK), a kinase involved in stress response pathways. H2A.X activation is influenced by stress-induced signaling cascades. Inhibiting p38 MAPK with SB203580 disrupts the stress response pathway, leading to altered H2A.X phosphorylation and modulation of its activation in cellular stress conditions. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is a phosphoinositide 3-kinase (PI3K) inhibitor, affecting the PI3K/Akt signaling pathway. This pathway plays a role in regulating H2A.X phosphorylation. By inhibiting PI3K, Wortmannin disrupts this pathway, influencing the activation of H2A.X in response to DNA damage and oxidative stress. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $32.00 $170.00 $385.00 | 63 | |
Etoposide is a topoisomerase II inhibitor used in chemotherapy. It induces DNA double-strand breaks, leading to the activation of H2A.X as part of the cellular response to DNA damage. Etoposide's mechanism involves the generation of DNA lesions, triggering the ataxia-telangiectasia mutated (ATM) kinase pathway and subsequent H2A.X phosphorylation in the DNA damage response. | ||||||
Trichostatin A | 58880-19-6 | sc-3511 sc-3511A sc-3511B sc-3511C sc-3511D | 1 mg 5 mg 10 mg 25 mg 50 mg | $149.00 $470.00 $620.00 $1199.00 $2090.00 | 33 | |
Trichostatin A is a potent inhibitor of histone deacetylases (HDACs). HDACs are involved in chromatin remodeling and gene expression. H2A.X activation is influenced by the acetylation status of histones. Trichostatin A, by inhibiting HDACs, modulates the acetylation of histones, indirectly affecting the activation of H2A.X and its involvement in DNA damage repair and chromatin dynamics. | ||||||
Camptothecin | 7689-03-4 | sc-200871 sc-200871A sc-200871B | 50 mg 250 mg 100 mg | $57.00 $182.00 $92.00 | 21 | |
Camptothecin is a topoisomerase I inhibitor that induces DNA damage. This leads to the activation of H2A.X, as part of the cellular response to DNA strand breaks. Camptothecin's mechanism involves the formation of topoisomerase I-DNA cleavage complexes, triggering the ataxia-telangiectasia mutated (ATM) kinase pathway and subsequent H2A.X phosphorylation in the DNA damage response. | ||||||
AZD7762 | 860352-01-8 | sc-364423 | 2 mg | $107.00 | ||
AZD7762 is a selective inhibitor of checkpoint kinases 1 and 2 (Chk1/2). Chk1/2 are key regulators of cell cycle checkpoints in response to DNA damage. By inhibiting Chk1/2, AZD7762 disrupts the cell cycle checkpoints and indirectly affects H2A.X activation by altering the dynamics of DNA damage response pathways and cell cycle progression. | ||||||