All AbMole products are for research use only, cannot be used for human consumption.
JNJ-26481585 (Quisinostat) is an oral histone deacetylase (HDAC) inhibitor with IC50 values of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. JNJ-26481585 fully inhibited the growth of C170HM2 colorectal liver metastases, whereas again 5-fluorouracil/Leucovorin showed modest activity. JNJ-26481585 exhibits broad spectrum antiproliferative activity in solid and hematologic cancer cell lines, such as all lung, breast, colon, prostate, brain, and ovarian tumor cell lines, with IC50 ranging from 3.1-246 nM, which is more potent than vorinostat, R306465, panobinostat, CRA-24781, or mocetinostat in various human cancer cell lines tested. Once daily oral administration of JNJ-26481585 induced continuous histone H3 acetylation. JNJ-26481585 is currently in a phase II clinical trial for the treatment of previously treated cutaneous T-cell lymphoma.
 |
Source | Oncotarget (2015). Figure 2. JNJ-26481585 |
| Method | colony formation assay | |
| Cell Lines | RMS cells | |
| Concentrations | 7.5 nM | |
| Incubation Time | 23 h | |
| Results | Notably, the combination of JNJ-26481585 and Doxorubicin significantly reduced colony formation of RMS cells compared to treatment with either agent alone |
| Cell Experiment | |
|---|---|
| Cell lines | colo-205, HT-29, HCT-116, H460, H1229, DU145, and A2780 cell lines |
| Preparation method | Cell proliferation and apoptosis assays. All cell lines were obtained from American Type Culture Collection and cultured according to instructions. The effect of HDAC inhibitors on cell proliferation was measured using an MTT as described (12). Proliferation of non–small cell lung carcinoma (NSCLC) cell lines was assessed using an Alamar Blue–based assay as described (12). For proliferation of hematologic cell lines, cells were incubated for 72 h and the cytotoxic activity was evaluated by MTS assay. Data are presented as mean IC50 or IC40 ± SD of at least three independent experiments. For apoptosis assays, human tumor cells were incubated for 24, 48, and 96 h with JNJ-26481585 at the indicated concentrations. Cells were stained for Annexin V and 7-AAD, according to the manufacturer's instructions and analyzed (Guava PCA-96 Nexin kit, Guava Technologies). The number of apoptotic and necrotic cells was expressed as a percentage of the total number of cells present in the well. Total cell number was expressed as a percentage of control, and the percentage of apoptotic/necrotic cells present in the absence of compound was subtracted from all values. All results shown are an average of three independent experiments (± SD). |
| Concentrations | 3, 10, 30, 100 and 300 nM |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | NMRI nude mice bearing colorectal cancer HCT-116 xenografts |
| Formulation | 20% hydroxypropyl-β-cyclodextrin (final pH 8.7) |
| Dosages | 10 mg/kg once daily for 14 days |
| Administration | i.p. |
| Molecular Weight | 394.47 |
| Formula | C21H26N6O2 |
| CAS Number | 875320-29-9 |
| Solubility (25°C) | DMSO 49 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
|---|
| Belinostat
Belinostat (PXD101) is a novel HDAC inhibitor with an IC50 of 27 nM. |
| CUDC-101
CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. |
| Givinostat hydrochloride monohydrate
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor. The IC50 values for maize HDAC preparations HD2, HD-1B and HD-1A are 10, 7.5 and 16 nM respectively. |
| Niltubacin
Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. |
| Tubacin
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
