TCS HDAC6 20b

TCS HDAC6 20b

Catalog Number:
L002369256APE
Mfr. No.:
APE-A4500
Price:
$514
  • Size:
    10mg
    Quantity:
    Add to Cart:
      • Overview
        • Please contact us at for specific academic pricing.

          Background

          TCS HDAC6 20b is a potent and selective inhibitor of histone deacetylase 6 (HADC6) [1].
          Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription. Mutation of HADC6 is associated with Alzheimer's disease.
          In HCT116 cells, TCS HDAC6 20b increased ɑ-tubulin acetylation in a dose-dependent way without a significant increase in acetylated histone H4, which indicated that TCS HDAC6 20b selectively inhibit HDAC6 [1]. Treatment human colon cancer HCT116 cells with TCS HDAC6 20b (5 μM) and paclitaxel (PTX) (0.03 μM) inhibited cells growth by approximately 50%, which suggested that TCS HDAC6 20b has potential as drug candidates when used with PTX. In estrogen receptor ɑ (ERɑ) -positive breast cancer MCF-7 cells, treatment with 17β-estradiol (E2) (1 nM) increased cell growth by 40%, which was significantly blocked by TCS HDAC6 20b [2].

          [1]. Suzuki T, Kouketsu A, Itoh Y, et al. Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. J Med Chem, 2006, 49(16): 4809-4812.
          [2]. Itoh Y, Suzuki T, Kouketsu A, et al. Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. J Med Chem, 2007, 50(22): 5425-5438.

      • Properties
        • Alternative Name
          S-((S)-7-((3R,5R,7R)-adamantan-1-ylamino)-6-((tert-butoxycarbonyl)amino)-7-oxoheptyl) 2-methylpropanethioate
          CAS Number
          956154-63-5
          Molecular Formula
          C26H44N2O4S
          Molecular Weight
          480.7
          Appearance
          White Oily foam
          Purity
          Purity ≥95.00%
          Solubility
          Soluble in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187

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