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TCS HDAC6 20b

Catalog No.GC12019

An HDAC6 inhibitor

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TCS HDAC6 20b Chemical Structure

Cas No.: 956154-63-5

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1mg
$44.00
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5mg
$205.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

TCS HDAC6 20b is a potent and selective inhibitor of histone deacetylase 6 (HADC6) [1].

Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription. Mutation of HADC6 is associated with Alzheimer's disease.

In HCT116 cells, TCS HDAC6 20b increased ɑ-tubulin acetylation in a dose-dependent way without a significant increase in acetylated histone H4, which indicated that TCS HDAC6 20b selectively inhibit HDAC6 [1]. Treatment human colon cancer HCT116 cells with TCS HDAC6 20b (5 μM) and paclitaxel (PTX) (0.03 μM) inhibited cells growth by approximately 50%, which suggested that TCS HDAC6 20b has potential as drug candidates when used with PTX. In estrogen receptor ɑ (ERɑ) -positive breast cancer MCF-7 cells, treatment with 17β-estradiol (E2) (1 nM) increased cell growth by 40%, which was significantly blocked by TCS HDAC6 20b [2].

References:
[1].  Suzuki T, Kouketsu A, Itoh Y, et al. Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate. J Med Chem, 2006, 49(16): 4809-4812.
[2].  Itoh Y, Suzuki T, Kouketsu A, et al. Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. J Med Chem, 2007, 50(22): 5425-5438.

Chemical Properties

Cas No. 956154-63-5 SDF
Chemical Name S-((S)-7-((3R,5R,7R)-adamantan-1-ylamino)-6-((tert-butoxycarbonyl)amino)-7-oxoheptyl) 2-methylpropanethioate
Canonical SMILES CC(C(SCCCCC[C@H](NC(OC(C)(C)C)=O)C(NC1(C[C@H](C2)C3)C[C@H]3C[C@H]2C1)=O)=O)C
Formula C26H44N2O4S M.Wt 480.7
Solubility DMSO: 20 mg/ml,Ethanol: 20 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.0803 mL 10.4015 mL 20.803 mL
5 mM 0.4161 mL 2.0803 mL 4.1606 mL
10 mM 0.208 mL 1.0401 mL 2.0803 mL
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