Home DNA Damage/DNA Repair HDAC inhibitor Nexturastat A

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Nexturastat A HDAC inhibitor

Cat.No.S7473

Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.
Nexturastat A HDAC inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 341.4

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Quality Control

Batch: S747301 DMSO]68 mg/mL]false]Ethanol]2 mg/mL]false]Water]Insoluble]false Purity: 99.65%
99.65

Chemical Information, Storage & Stability

Molecular Weight 341.4 Formula

C19 H23 N3 O3

 Storage (From the date of receipt)
CAS No. 1403783-31-2 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCCCN(CC1=CC=C(C=C1)C(=O)NO)C(=O)NC2=CC=CC=C2

Solubility

In vitro
Batch:

DMSO : 68 mg/mL (199.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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
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Mechanism of Action

Features
Urea-based HDAC6-selective inhibitor.
Targets/IC50/Ki
HDAC6 [1]
(Cell-free assay)
5 nM
In vitro
In B16 murine melanoma cells, Nexturastat A leads to a dose-dependent increase of acetyl α-tubulin levels without a concomitant elevation of histone H3 acetylation. Moreover, this compound potently inhibits the growth of B16 melanoma cells with GI50 of 14.3 μM. [1]
Kinase Assay
HDAC inhibition assays
HDAC inhibition assays are performed by Reaction Biology Corp. using isolated human, recombinant full2length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide,RHKKAc, derived from residues 379-382 of p53 is used as substrate. The reaction buffer is made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds are delivered in DMSO and delivered to enzyme mixture with preincubation of 5-10 min followed by substrate addition and incubation for 2 h at 30°C. Trichostatin A and developer are added to quench the reaction and generate fluorescence, respectively. Dose-response curves are generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. IC50 values are then generated from the resulting plots, and the values expressed are the average of duplicate trials ± standard deviation.
References

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