SKLB-23bb

Catalog No.S8743

SKLB-23bb Chemical Structure

Molecular Weight(MW): 396.44

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.

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Biological Activity

Description SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.
Targets
HDAC6 [1]
(Cell-based assay)
<100 nM
In vitro

SKLB-23bb shows cytotoxic effects against a panel of solid and hematologic tumor cell lines at the low submicromolar level. In contrast to the reported HDAC6-selective inhibitors, SKLB-23bb is more efficient against solid tumor cells. SKLB-23bb selectively inhibits cellular HDAC6, but the antitumor activity of SKLB-23bb is independent of HDAC6. SKLB-23bb could bind to the colchicine site in β-tubulin and act as a microtubule polymerization inhibitor. It blocks tumor cell cycle at G2-M phase and triggers cellular apoptosis[1].

In vivo

In solid tumor xenografts, oral administration of SKLB-23bb efficiently inhibits tumor growth. SKLB-23bb has good pharmacokinetic profiles and is orally bioavailable[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HCT116 and A2780S cells
  • Concentrations: 200 nM
  • Incubation Time: 3, 6, 12 and 24 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: HCT116, A2780S, and MCF-7 xenografts established on Balb/c nude mice
  • Formulation: --
  • Dosages: 3, 6, 12.5, 25 and 50 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (199.27 mM)
Ethanol 79 mg/mL (199.27 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 396.44
Formula

C21H24N4O4

CAS No. 1815580-06-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID