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SKLB-23bb HDAC inhibitor

Name: SKLB-23bb
Brand: Selleck Chemicals
SKU: S8743
Availability: InStock
Rating: 5 (1 reviews)

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.

Chemical Structure

Molecular Weight: 396.44

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Quality Control

Batch: Purity: 99.72%

99.72

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Inhibitors	ITF-2357 (Givinostat) Hydrochloride Monohydrate Fimepinostat (CUDC-907) Trichostatin A (TSA) Entinostat (MS-275) RGFP966 Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A Hydrochloride Tubastatin A Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

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
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

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	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=NC2=CC=CC=C2C(=N1)N(C)C3=CC(=C(C=C3)OC)OCCCC(=O)NO

Mechanism of Action

Targets/IC₅₀/Ki	HDAC6 (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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/29610282/

Applications

Methods	Biomarkers	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