Home Epigenetics HDAC inhibitor SKLB-23bb For research use only.

SKLB-23bb

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

SKLB-23bb Chemical Structure

CAS: 1815580-06-3

Purity & Quality Control

Batch: Purity: 99.72%
99.72

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Signaling Pathway

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HDAC Signaling Pathway

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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
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].
Cell Research Cell lines HCT116 and A2780S cells
Concentrations 200 nM
Incubation Time 3, 6, 12 and 24 h
Method

--
Experimental Result Images Methods Biomarkers Images 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 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].
Animal Research 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

Chemical Information & Solubility

Molecular Weight 396.44 Formula

C21H24N4O4
CAS No. 1815580-06-3 SDF --
Smiles CC1=NC2=CC=CC=C2C(=N1)N(C)C3=CC(=C(C=C3)OC)OCCCC(=O)NO
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 79 mg/mL ( (199.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble


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In vivo
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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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