Resminostat (4SC-201) is a novel, orally bioavailable histone deacetylase (HDAC) inhibitor for the treatment of cancers. Resminostat inhibited proliferation and induced G0/G1 cell cycle arrest in 3 out of 4 MM cell lines accompanied with decreased levels of cyclin D1, cdc25a, Cdk4 and pRb as well as upregulation of p21 at 1 micromol/l. Resminostat (4SC-201) induces hyperacetylation of histone H4 in MM cells. Low micromolar concentrations of resminostat (RAS2410) abrogated cell growth and strongly induced apoptosis (IC50=2.5-3 micromol/l in 3 out of 4 MM cell lines) in MM cell lines as well as primary MM cells. Resminostat decreased phosphorylation of 4E-BP1 and p70S6k indicating an interference with Akt pathway signalling. Resminostat treatment resulted in increased protein levels of Bim and Bax and decreased levels of Bcl-xL.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
The novel inhibitor of histone deacetylase resminostat (RAS2410) inhibits proliferation and induces apoptosis in multiple myeloma (MM) cells.
Mandl-Weber S, et al. Br J Haematol. 2010 May;149(4):518-28. PMID: 20201941.
|Related HDAC Products|
Valproic acid is an HDAC inhibitor with IC50 in the range of 0.5~2 mM.
Chidamide is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.