Activators & Inhibitors

RVX-028, also known as RVX-000222, is a potent BET bromodomain inhibitor. It preferentially binds to the second bromodomain on BET proteins. It also stimulates apolipoprotein (APO) AI gene expression, which increases apoA-I and HDL-C in vitro. In vivo, RVX-208 enhances cholesterol efflux via different pathways and significantly increases serum apoA-I and HDL-C in monkeys.

Scriptaid, also known as GCK 1026, is a histone deacetylase inhibitor with optimal concentration of 6-8 µM in a cell based assay. Scriptaid is exhibits lower toxicity than trichostatin A. Scriptaid inhibits tumor growth in vitro and in vivo. It also induces cell cycle arrest in colon cancer cells in culture.

Oxamflatin is a potent inhibitor of histone deacetylases. It has the ability to alter expression of genes involved in cell morphology, motility, apoptosis and cell cycle control, reducing the proliferation of cancer cells.

Chidamide is a histone deacetylase inhibitor which increases Histone H3 acetylation levels in LoVo and HT29 colon cancer cells at low concentrations (4 µM). Chidamide affects the activation of oncogenic signaling kinases by dose-dependently reducing phosphorylated Akt, mTOR, p70S6K, Raf and Erk 1/2 protein expression in colon cancer cells. Chidamide also dose-dependently upregulates p21 protein expression, down-regulates CDK4, and induces cell cycle arrest at the G0/G1 phase.

M344 is a histone deacetylase (HDAC) inhibitor also known as D237 or MS 344. It inhibits human HDACs, and shows a three-fold selectivity for inhibition of HDAC6 over HDAC1. M344 has been found to increase the sensitivity of human squamous carcinoma cells to radiation. It has also been found to promote cell cycle arrest and apoptosis in human ovarian cancer cells and endometrial cancer. M344 can also inhibit maize HDAC.

M-Carboxycinnamic Acid bishydroxamide, or CBHA, is a potent histone deacetylase (HDAC) inhibitor. CBHA has been found to induce apoptosis in nine different neuroblastoma cell lines in culture. It can also completely suppress neuroblastoma tumor growth in SCID mice at 200 mg/kg.

4-iodo-SAHA is a hydrophobic derivative of SAHA, a class I and class II histone deacetylase (HDAC) inhibitor. Similar to SAHA, it demonstrates > 60% inhibition of HDAC1 and HDAC6 activity in a deacetylase activity assay at 1 µM.

HNHA is a cell-permeable inhibitor of histone deacetylase (HDAC) activity. HNHA induces histone hyperacetylation and p21 transcription with inhibition of cell cycle progression in human fibrosarcoma HT1080 cells. In in vivo murine xenographs, HNHA is equally as effective as SAHA in inhibiting tumor growth. HNHA inhibits HUVEC growth and prevents tube formation and migration in response to VEGF. Also HNHA blocks retinal neovascularization and choroidal angiogenesis in mice.

Valproic acid inhibits histone deacetylases (HDACs), in particular Class I HDACs. It is an analog of the natural fatty acid valeric acid. Valproic acid also inhibits GSK3 and depletes cellular inositol-1,4,5-triphosphate. It can have strong effects on stem cell differentiation and self-renewal, and it shows promise in treating cancer and Alzheimer's disease.