Activators & Inhibitors

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.

HC Toxin is a reversible, cell-permeable inhibitor of HDACs. It is a cyclic tetrapeptide first isolated from C. carbonum, a maize pathogen. It up-regulates the expression of 15-lipoxygenase-1 in colorectal cancer cells and has been shown to induce fetal hemoglobin in human primary erythroid cells.

Suberohydroxamic acid (SBHA) is a competitive HDAC inhibitor. SBHA has been shown to cause cell differentiation, cell cycle arrest, and apoptosis.

LY171883 is a PDE inhibitor and a selective, potent inhibitor of the leukotriene D4 receptor. Also, LY171883 binds to the PPAR nuclear receptor at 50-100 ?M and induces adipogenesis in cultured NIH3T3 fibroblasts.

IBMX, also known as 1-Methyl-3-Isobutylxanthine and Isobutylmethylxanthine, is a widely-used inhibitor of cAMP and cGMP PDEs. It has been shown that the increase in cellular cAMP and cGMP levels, resulting from the inhibition of PDEs by IBMX, activates cyclicnucleotide-regulated protein kinases. IBMX does not inhibit PDE8A, PDE8B, or PDE9.