Nexturastat A

HDAC6 inhibitor,highly potent and selective CAS# 1403783-31-2

Nexturastat A

Catalog No. BCC5345----Order now to get a substantial discount!

Product Name & Size Price Stock
Nexturastat A: 5mg $403 In Stock
Nexturastat A: 10mg Please Inquire In Stock
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Chemical structure

Nexturastat A

3D structure

Chemical Properties of Nexturastat A

Cas No. 1403783-31-2 SDF Download SDF
PubChem ID 71462653 Appearance Powder
Formula C19 H23 N3 O3 M.Wt 341.4
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 56 mg/mL (164.03 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-[[butyl(phenylcarbamoyl)amino]methyl]-N-hydroxybenzamide
SMILES CCCCN(CC1=CC=C(C=C1)C(=O)NO)C(=O)NC2=CC=CC=C2
Standard InChIKey JZWXMCPARMXZQV-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H23N3O3/c1-2-3-13-22(19(24)20-17-7-5-4-6-8-17)14-15-9-11-16(12-10-15)18(23)21-25/h4-12,25H,2-3,13-14H2,1H3,(H,20,24)(H,21,23)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Nexturastat A

DescriptionNexturastat A is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 value of 5 nM.
TargetsHDAC6    
IC505 nM     

Nexturastat A Dilution Calculator

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Nexturastat A Molarity Calculator

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Preparing Stock Solutions of Nexturastat A

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9291 mL 14.6456 mL 29.2912 mL 58.5823 mL 73.2279 mL
5 mM 0.5858 mL 2.9291 mL 5.8582 mL 11.7165 mL 14.6456 mL
10 mM 0.2929 mL 1.4646 mL 2.9291 mL 5.8582 mL 7.3228 mL
50 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.1716 mL 1.4646 mL
100 mM 0.0293 mL 0.1465 mL 0.2929 mL 0.5858 mL 0.7323 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Nexturastat A

Nexturastat A is a selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 value of 5.2 nM [1].

Nexturastat A is a HDAC inhibitor. It was developed by structural modification of aryl urea HDACIs. The inhibitory activity of Nexturastat A is most potent against HDAC6 with IC50 value of 5.2 nM. Besides that, Nexturastat A also shows inhibition of other HDACs with IC50 values of 3.02, 6.92, 6.68, 9.39, 11.7, 4.46, 0.954, 6.72, 7.57 and 5.14 μM for HDAC1, 2, 3, 4, 5, 7, 8, 9, 10 and 11, respectively. Nexturastat A has been shown to suppress cell proliferation and promote apoptosis in B16 murine melanoma cells [1, 2].

References:
[1] Kalin J H, Bergman J A. Development and therapeutic implications of selective histone deacetylase 6 inhibitors. Journal of medicinal chemistry, 2013, 56(16): 6297-6313.
[2] Zhang L, Han Y, Jiang Q, et al. Trend of Histone Deacetylase Inhibitors in Cancer Therapy: Isoform Selectivity or Multitargeted Strategy. Medicinal research reviews, 2014.

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References on Nexturastat A

The selective HDAC6 inhibitor Nexturastat A induces apoptosis, overcomes drug resistance and inhibits tumor growth in multiple myeloma.[Pubmed:30782785]

Biosci Rep. 2019 Mar 22;39(3). pii: BSR20181916.

Multiple myeloma (MM) is a hematological malignancy of plasma cells that produce a monoclonal immunoglobulin protein. Despite significant advances in the treatment of MM, challenges such as resistance to therapy remain. Currently, inhibition of histone deacetylases (HDACs) is emerging as a potential method for treating cancers. Numerous HDAC inhibitors are being studied for the use in monotherapy or in conjunction with other agents for MM. In the present study, we investigated the anti-myeloma effect of Nexturastat A (NexA), a novel selective HDAC6 inhibitor. We found that NexA impaired MM cells viability in a dose- and time-dependent manner. NexA also provoked a cell cycle arrest at the G1 phase in MM cells. Furthermore, NexA promoted apoptosis of MM cells via transcriptional activation of the p21 promoter, which may through its ability to up-regulate the H3Ac and H4Ac levels. Additionally, NexA could overcome bortezomib (BTZ) resistance in MM cells, and NexA in combination with BTZ had stronger efficacy. We also confirmed that NexA inhibited tumor growth in murine xenograft models of MM. These interesting findings provided the rationale for the future advancement of this novel HDAC6 inhibitor as a potential therapeutic anti-myeloma agent.

Description

Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.

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