Free shipping on all orders over $ 500

Niltubacin

Cat. No. M1738
Niltubacin Structure
Synonym:

MAZ-1391

Size Price Availability Quantity
1mg USD 180 In stock
5mg USD 320 In stock
Bulk Inquiry?

Quality Control
Biological Activity

Niltubacin, as an inactive derivative of Tubacinis, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. Histone deacetylase 6 (HDAC6) is structurally and functionally unique among the 11 human zinc-dependent histone deacetylases. HDAC6-selective inhibitor tubacin significantly enhances cell death induced by the topoisomerase II inhibitors etoposide and doxorubicin and the pan-HDAC inhibitor SAHA (vorinostat) in transformed cells (LNCaP, MCF-7), an effect not observed in normal cells. The inactive analogue of tubacin, nil-tubacin, does not sensitize transformed cells to these anticancer agents.

Protocol
Cell Experiment
Cell lines Raji cells
Preparation method Cell adhesion assay Prior to SDF-1α (100 ng/ml) stimulation, Raji cells were treated with DMSO, NaB (1 μM), or tubacin (1 μM) for 3 hours. Then cells were plated into a 96-well plate which were precoated with Fibronectin (50 ng/ml) to allow cell adherence for 30 minutes. Subsequently cells were washed with PBS three times to remove the non-adherent cells, and adherent cells were measured by CellTiter-Glo luminescent cell viability assay kit.
Concentrations 1μM
Incubation time 3h
Animal Experiment
Animal models PLD animal model 3-week-old PCK rats
Formulation saline
Dosages 30 mg/kg body
Administration intraperitoneally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 706.85
Formula C41H42N2O7S
CAS Number
Purity >99%
Solubility DMSO ≥5 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source J Cell Biochem (2017). Figure 5. Niltubacin (Abmole Bioscience Inc.)
Method Clonogenic survival assay
Cell Lines FEMX-I cell line
Concentrations 200 µm
Incubation Time 24 h
Results This effect was specific for tubacin, as TSA, niltubacin and ACY-1215 did not inhibit the formation of cell aggregates. Similar effects were observed in Caco-2 cell line (Supplementary Fig. S5).
Rating
Source J Cell Biochem (2017). Figure 2. Niltubacin (Abmole Bioscience Inc.)
Method Cell Aggregation Assay
Cell Lines FEMX-I cell line
Concentrations
Incubation Time 24 h
Results The effect was specific, as the inactive analog of tubacin, niltubacin, at the same concentration did not increase CD133, CD9, or b-actin levels (Fig. 2c).
Rating
Source Mol. Cell. Biol. (2016). Figure 9. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX)
Method BK-SS mice
Cell Lines
Concentrations 0.5mg/kg i.p.
Incubation Time 5 or 10 or 30 days
Results These drug regimens showed a time dependent reduction of PlGF (Fig. 9C) and ET-1 (Fig. 9D) in plasma, compared to Niltubacin. The 30 day drug treatment effectively reduced plasma levels of PlGF by ~60% (p <0.001, Fig. 9C) and plasma levels of ET-1 by ~60% (p<0.001, Fig. 9D).
Rating
Source Mol. Cell. Biol. (2016). Figure 7. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX)
Method FAIRE-qPCR
Cell Lines HMEC-1 cells
Concentrations 5 µM
Incubation Time 30 min
Results Taken together, these data showed PlGF induced chromatin condensation to repress DNM3os transcription, while Tubacin prevented the repressive effect following PlGF signaling.
Rating
Source Mol. Cell. Biol. (2016). Figure 6. Tubacin and Niltubacin for animal studies were obtained from AbMole Bioscience Inc. (Houston, TX)
Method qRT-PCR and reporter luciferase activity
Cell Lines HMEC-1 cells
Concentrations 5 µM
Incubation Time 30 min
Results We concluded that HDAC6 required functional ATF3 binding sites in the DNM3os promoter and any antagonism of PlGF effects by Tubacin was not due to a general effect on transcription of the endogenous DNM3os gene or the wt DNM3os reporter construct.
Rating
Product Citations
References

Selective inhibition of histone deacetylase 6 (HDAC6) induces DNA damage and sensitizes transformed cells to anticancer agents.
Namdar et al. Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):20003-8. PMID: 21037108.

Histone deacetylase 6 interacts with the microtubule-associated protein tau.
Ding et al. J Neurochem. 2008 Sep;106(5):2119-30. PMID: 18636984.

Related HDAC Products
Chidamide

Chidamide is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.

TMP195

TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.

WT161

WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.

EDO-S101

EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.

Citarinostat

Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Niltubacin, MAZ-1391 supplier, HDAC, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.