Home Epigenetics HDAC inhibitor SKLB-23bb

research use only

SKLB-23bb HDAC inhibitor

Cat.No.S8743

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 HDAC inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 396.44

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 396.44 Formula

C21H24N4O4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1815580-06-3 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=NC2=CC=CC=C2C(=N1)N(C)C3=CC(=C(C=C3)OC)OCCCC(=O)NO

Solubility

In vitro
Batch:

DMSO : 79 mg/mL (199.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 79 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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, this compound is more efficient against solid tumor cells. It selectively inhibits cellular HDAC6, but the antitumor activity of this chemical is independent of HDAC6. It could bind to the colchicine site in β-tubulin and act as a microtubule polymerization inhibitor. This compound 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. This compound has good pharmacokinetic profiles and is orally bioavailable[1].
References

Applications

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 S8743-WB1 29610282
Immunofluorescence α-tubulin S8743-IF1 29610282
Growth inhibition assay Cell viability S8743-viability1 29610282

Tech Support

Handling Instructions

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

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map