ITSA-1 (ITSA1) |
| Catalog No.GC14597 |
ITSA-1 (ITSA1) is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
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Cas No.: 200626-61-5
Sample solution is provided at 25 µL, 10mM.
ITSA-1 (ITSA1) is an HDAC activator through trichostatin A (TSA) suppression.
Trichostatin A (TSA), a streptomyces metabolite, can specifically inhibit mammalian histone deacetylase at a nanomolar concentration causing accumulation of highly acetylated histone molecules in mammalian cells.
In vitro: Previous study reported that in murine embryonic stem cells, TSA treatment for 23 hours inhibited BrdU incorporation compared with the control. TSA-pretreated cells incubated with ITSA1, however, could incorporate BrdU at concentrations where it was inhibited by TSA alone. Moreover, ITSA1 treatment was able to revert the TSA-arrested population to a normal cell cycle distribution. TSA treatment at 300 nM to A549 cells for 2 hours noticeably increased the levels of acetyl-histone H3, whereas subsequent incubation with ITSA1 at 50 μM for 2 hours reduced histone acetylation to the baseline level. In addition, cells pretreated with ITSA1 before addition of TSA showed increased acetylation levels, which was a characteristic of TSA treatment alone. These results suggested that the target of ITSA1 was not present until induced by TSA. Furthermore, the ITSA1 treatment alone at 50 or 100 μM was not effective on HDAC activity, demonstrating that ITSA1 could directly affect HDAC function [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, ITSA-1 (ITSA1) is still in the preclinical development stage.
Reference:
[1] Koeller KM, Haggarty SJ, Perkins BD, Leykin I, Wong JC, Kao MC, Schreiber SL. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation. Chem Biol. 2003 May;10(5):397-410.
| Cas No. | 200626-61-5 | SDF | |
| Chemical Name | (1H-benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone | ||
| Canonical SMILES | O=C(N1N=NC2=CC=CC=C21)C3=CC=C(Cl)C=C3Cl | ||
| Formula | C13H7Cl2N3O | M.Wt | 292.12 |
| Solubility | ≥ 89mg/mL in DMSO | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4233 mL | 17.1163 mL | 34.2325 mL |
| 5 mM | 0.6847 mL | 3.4233 mL | 6.8465 mL |
| 10 mM | 0.3423 mL | 1.7116 mL | 3.4233 mL |
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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