Activators & Inhibitors

RGFP966 is specific for HDAC3, with an IC50 of 0.08 µM and no effective inhibition of any other HDAC at concentrations up to 15 µM.

Rocilinostat, also known as ACY-1215, is a selective HDAC6 inhibitor with IC50 of 5 nM. It is over 10-fold more selective for HDAC6 than HDAC1, 2, 3 (class I HDACs) with slight activity against HDAC8, and minimal activity against HDAC4, 5, 7, 9, 11, SIRT1, and SIRT2.

Rocilinostat, also known as ACY-1215, is a selective HDAC6 inhibitor with IC50 of 5 nM. It is over 10-fold more selective for HDAC6 than HDAC1, 2, 3 (class I HDACs) with slight activity against HDAC8, and minimal activity against HDAC4, 5, 7, 9, 11, SIRT1, and SIRT2.

Rocilinostat, also known as ACY-1215, is a selective HDAC6 inhibitor with IC50 of 5 nM. It is over 10-fold more selective for HDAC6 than HDAC1, 2, 3 (class I HDACs) with slight activity against HDAC8, and minimal activity against HDAC4, 5, 7, 9, 11, SIRT1, and SIRT2.

Roflumilast is an orally active, selective inhibitor of phophodiesterase-4 (PDE-4) with IC50 value of 0.11 nM . Roflumilast displays anti-inflammatory and immunomodulatory in vitro.

Roflumilast is an orally active, selective inhibitor of phophodiesterase-4 (PDE-4) with IC50 value of 0.11 nM . Roflumilast displays anti-inflammatory and immunomodulatory in vitro.

Roflumilast is an orally active, selective inhibitor of phophodiesterase-4 (PDE-4) with IC50 value of 0.11 nM . Roflumilast displays anti-inflammatory and immunomodulatory in vitro.

Romidepsin, also known as FK228 or depsipeptide, is a potent and selective inhibitor of HDAC1 and HDAC2 , which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.

Romidepsin, also known as FK228 or depsipeptide, is a potent and selective inhibitor of HDAC1 and HDAC2 , which are associated with the regulation of re-expression of silenced tumor suppressor genes. It was the first HDAC inhibitor to manifest anti-tumor activity and originally isolated from a rod-shaped Gram-negative bacterium, Chromobacterium violaceum, found in a Japanese soil sample. Romidepsin exhibits a stronger inhibition towards HDAC1 and HDAC2 enzymes (class I), removing acetyl groups from the lysine residues of N-terminal histone tails and maintaining a more open and transcriptionally active chromatin state, than HDAC4 and HDAC6 enzymes (class II). Besides HDAC inhibition, romidepsin is also able to induce cell cycle arrest, cellular differentiation, apoptosis and alteration of gene expression in adult malignancies.