HDAC8
- Known as:
- HDAC8
- Catalog number:
- 000428A
- Product Quantity:
- 250ul
- Category:
- -
- Supplier:
- ABM
- Gene target:
- HDAC8
Related genes to: HDAC8
- Gene:
- HDAC8 NIH gene
- Name:
- histone deacetylase 8
- Previous symbol:
- HDACL1, WTS, MRXS6
- Synonyms:
- RPD3, KDAC8
- Chromosome:
- Xq13.1
- Locus Type:
- gene with protein product
- Date approved:
- 2000-11-28
- Date modifiied:
- 2019-02-19
Related products to: HDAC8
Related articles to: HDAC8
- Phosphatidylinositol 3-kinase (PI3K) and histone deacetylase (HDAC) inhibition is a potential tumor treatment strategy, including for cervical cancer. Herein, a novel series of thienopyrimidine derivatives was rationally designed, synthesized, and biologically evaluated as dual PI3K/HDAC inhibitors targeting cervical cancer. Compound B7 was evaluated for its inhibitory effects across the entire PI3K and HDAC families, and exhibited strong PI3Kα (IC = 25.41 ± 5.23 nM), PI3Kδ (IC = 41.58 ± 4.54 nM), HDAC6 (IC = 29.35 ± 3.41 nM), and moderate HDAC8 inhibition (IC = 157.27 ± 6.18 nM). In cellular assays, B7 suppressed the proliferation of four cervical cancer cell lines (HeLa, SiHa, Ca-Ski, and ME-180) with IC values below 5 μM. And B7 showed moderate selectivity in normal L-O2 and HEK-293T cell viability with IC values around 15 μM. Mechanistically, B7 induced HeLa cell S-phase arrest and apoptosis. Notably, it blocked the PI3K/AKT pathway and upregulated α-tubulin and SMC3 acetylation without altering Ac-H3/H4 levels, consistent with its enzymatic selectivity for HDAC6/8 over Class I HDACs. Molecular dynamics simulations revealed that B7 formed stable binding modes with PI3Kα and HDAC6/8. Although rapid systemic clearance currently limits its in vivo application, the potent cellular efficacy of B7 highlights its utility as a dual PI3K/HDAC lead compound, providing a distinct chemical scaffold for further structural optimization. - Source: PubMed
Publication date: 2026/09/08
Wang WeixuShayilan NaziyilaQi XijinMa Cheng - Insufficient T-cell infiltration is a major barrier to the efficacy of immune checkpoint inhibitors (ICIs) in lung adenocarcinoma (LUAD). We aimed to investigate how the tumor-intrinsic mC methyltransferase NSUN2 shapes the immune landscape of LUAD. - Source: PubMed
Publication date: 2026/09/07
Meng WangyangLu TongDu MingyuanDai XinHan YichaoLi YingyiXu HaiminYang BiaolongWang ZeyuDu HaileiLiao KemanLiu XinnanSun YidanYang CuiDong DongYan YanGuo WeiLi BinLi Hecheng - Ewing sarcoma is an aggressive pediatric cancer for which no targeted therapies have been approved. This disease is driven by EWSR1::ETS family fusions that, like most fusion transcription factors, have proven difficult to target directly. Here, we focus on identifying actionable dependencies within the high-risk STAG2-mutant (STAG2-mut) disease subtype of Ewing sarcoma. In STAG2-mut Ewing sarcoma, STAG1 knockout is synthetically lethal but is not readily druggable. Using the Cancer Dependency Map (DepMap), we identify histone deacetylase 8 (HDAC8) as an enriched vulnerability in this molecular context. CRISPR validation and a newly developed HDAC8 degrader, XY-09-36, confirm this selective dependency and suggest increased reliance on HDAC8-mediated cohesin regulation when STAG2 is lost. These findings establish HDAC8 as a context-dependent, pharmacologically accessible vulnerability and outline a framework for discovering rational targets in tumor subtypes where primary drivers are intrinsically hard to drug. - Source: PubMed
Publication date: 2026/08/26
Olaoye OlasunkanmiXiong YuanRillahan Cory DAdane BiniamDiGiovanni GiuliaRoss Kenneth NAlexe GabrielaHoward BrianaKirmani NadiaNowak Radosław PDonovan Katherine AFischer Eric SStegmaier Kimberly - The impact of fast-food components on epigenetic modifications and their implications for immunotherapy in metastatic breast cancer remain inadequately explored. In this study, we investigated the effects of selected fast-food components monosodium glutamate (MSG), acrylamide (AA), sodium sorbate (SS), and sodium nitrite (NaNO) on the expression of the epigenetic enzymes histone deacetylase 8 (HDAC8) and protein arginine methyltransferase 5 (PRMT5), and their role in suppressing immunotherapeutic responses in MDA-MB-231 triple-negative breast cancer (TNBC) cells. Epigenetic modifications upregulate the expression of immune checkpoint proteins, including the integrin-associated transmembrane protein cluster of differentiation 47 (CD47), which enables metastatic cancer cells to evade immune surveillance by inhibiting macrophage-mediated phagocytosis. These modifications also increase the expression of programmed death-ligand 1 (PD-L1), further promoting immune evasion by inducing T-lymphocyte apoptosis. The key objectives of this study were to determine whether (i) fast-food components (AA, MSG, NaNO, and SS) can directly upregulate the epigenetic enzymes HDAC8 and PRMT5 in MDA-MB-231 cells without prior metabolic activation, and (ii) elevated HDAC8 and PRMT5 expression can induce the overexpression of the immune checkpoint proteins CD47 and PD-L1. Our findings reveal that prolonged exposure to MSG, AA, and SS upregulated the expression of epigenetic enzymes HDAC8 and PRMT5, upregulated oncogenic signaling, and enhanced the stemness-associated features in TNBC cells. These changes are associated with enhanced metastasis and reduced immunotherapeutic effects. Interestingly, our studies revealed that the combined presence of CD47 and HDAC8 inhibitors enhanced macrophage-mediated phagocytosis, thereby enabling immune cells to engulf cancer cells, improved the therapeutic response in TNBC, and promoted anticancer activities. These findings emphasize the importance of personalized dietary strategies for improving the efficacy of cancer immunotherapy and support the integration of specific epigenetic inhibitors with immune checkpoint inhibitors to amplify the therapeutic outcomes. - Source: PubMed
Publication date: 2026/08/10
Mukherjee AsmitaJanah PrithaTripathi ArchanaGayen ParamitaSinha Roy Rituparna - - Source: PubMed
Publication date: 2026/08/27
Papakonstantinou EleniNowak MartaPrince Spasenija SavicSoriano DanielGrize LeticiaFrye Björn ChristianFähndrich SebastianKoelzer Viktor HStolz Daiana