SKLB-23bb

Catalog No.S8743

For research use only.

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.

SKLB-23bb Chemical Structure

CAS No. 1815580-06-3

Purity & Quality Control

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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].

Assay
Methods Test Index PMID
Western blot Ac-α-tubulin / Ac-H3 ; p-H3 ; PARP / CF-PARP / Caspase 3 / CF-caspase 3 / Caspase 9 / CF-Caspase 9 29610282
Immunofluorescence α-tubulin 29610282
Growth inhibition assay Cell viability 29610282
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 (from reference)

Cell Research:

[1]

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

    --

Animal Research:

[1]

  • Animal Models: HCT116, A2780S, and MCF-7 xenografts established on Balb/c nude mice
  • Dosages: 3, 6, 12.5, 25 and 50 mg/kg
  • Administration: oral

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 396.44
Formula

C21H24N4O4

CAS No. 1815580-06-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC2=CC=CC=C2C(=N1)N(C)C3=CC(=C(C=C3)OC)OCCCC(=O)NO

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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

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