JNJ-26481585

JNJ-26481585

Catalog Number:
L002369003APE
Mfr. No.:
APE-A4090
Price:
$280
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          JNJ-26481585 is a novel histone deacetylase (HDAC) inhibitor that exerts a strong potency towards class I HDAC (including HDAC1, HDAC2 and HDAC3), with values of inhibition constant IC50 of 0.11, 0.33 and 4.8 nmol/L respectively, leading to strong anti-proliferative activities (IC50 ranging from 3.1 to 246 nmol/L) against a broad range of cancer cell lines including lung, breast, colon, prostate, brain and overian cancer cell lines. Recent study results have shown that JNJ-26481585 strongly induce the HDAC1-suppressed p21waf1,cip1 promoter in vivo, histone H3 acetylation in tumor tissue and apoptosis in human colon cancer cell lines (both APC wild-type and mutant) in vitro.

      • Properties
        • Alternative Name
          JNJ26481585; N-hydroxy-2-(4-((((1-methyl-1H-indol-3-yl)methyl)amino)methyl)piperidin-1-yl)pyrimidine-5-carboxamide
          CAS Number
          875320-29-9
          Molecular Formula
          C21H26N6O2
          Molecular Weight
          394.47
          Purity
          98.96%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Sauradip Chaudhuri, Martha Fowler, et al. "β-Cyclodextrin-Poly (β-Amino Ester) Nanoparticles Are a Generalizable Strategy for High Loading and Sustained Release of HDAC Inhibitors." ChemRxiv. Mar 27.2020
          2. Zhou H, Mondal A, et al. "Time-Dependent Effects of POT1 Knockdown on Proliferation, Tumorigenicity, and HDACi Response of SK-OV3 Ovarian Cancer Cells." Biomed Res Int. 2018 Feb 6;2018:7184253. PMID:29546066
          3. Householder KT, DiPerna DM, et al. "pH driven precipitation of quisinostat onto PLA-PEG nanoparticles enables treatment of intracranial glioblastoma." Colloids Surf B Biointerfaces. 2018 Feb 24;166:37-44. PMID:29533842

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