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| 25mg |
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| 50mg |
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Purity: ≥98%
ITSA-1 is a novel, potent, cell-membrane permeable and specific HDAC (Histone deacetylase) activator that suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC inhibitors. ITSA-1 may prove to be valuable probes of many biological processes. HDAC inhibitors are being developed as new clinical agents in cancer therapy, in part because they interrupt cell cycle progression in transformed cell lines.
| ln Vitro |
Treatment with ITSA-1 (50 μM; A549 cells) returned the cell population collected by TSA to a normal cell cycle distribution. Additionally, ITSA-1 has a long duration of cell cycle rescue capability [1]. TSA-treated cells have less apoptotic cells when treated with ITSA-1 (50 μM; 5 hours; A549 cells) [1]. The treatment of A549 and murine ES cells with ITSA-1 (50 μM) for two hours prevented TSA-induced histone acetylation. Crucially, acetylation levels were only inhibited when ITSA1 was introduced either concurrently with or following TSA treatment [1]. TSA-activated transcription in murine ES cells is inhibited by ITSA-1 (50 μM; 30 min) [1].
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| ln Vivo |
ITSA-1 (0.5 mg/kg; intraperitoneal; three times weekly; for eight weeks; CBS+/? mice) attenuates inflammatory signaling that is dependent on histone acetylation by balancing deacetylation activity and inhibiting the production of TNF-α and IL-6 [2].
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| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: Mouse ES Cells Tested Concentrations: 50 μM Incubation Duration: Experimental Results: Used to restore the TSA-captured population to normal cell cycle distribution. Apoptosis analysis[1] Cell Types: A549 Cell Tested Concentrations: 50 μM Incubation Duration: 5 hrs (hours) Experimental Results: diminished number of apoptotic cells. Western Blot Analysis[1] Cell Types: A549 and mouse ES cells Tested Concentrations: 50 μM Incubation Duration: 2 hrs (hours) Experimental Results: Histone acetylation diminished to baseline levels. RT-PCR[1] Cell Types: Mouse ES cells Tested Concentrations: 50 μM Incubation Duration: 30 minutes Experimental Results: Inhibition of TSA-activated transcription. |
| Animal Protocol |
Animal/Disease Models: CBS+/- mice [2]
Doses: 0.5 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times a week; for 8 weeks Experimental Results: Balance deacetylation activity and inhibit IL-6 and TNF-α expression. |
| References |
[1]. Koeller KM et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histoneand tubulin acetylation. Chem Biol. 2003 May;10(5):397-410.
[2]. Behera J, et al. Hydrogen Sulfide Promotes Bone Homeostasis by Balancing Inflammatory Cytokine Signaling in CBS-Deficient Mice through an Epigenetic Mechanism. Sci Rep. 2018 Oct 15;8(1):15226. |
| Molecular Formula |
C13H7N3OCL2
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|---|---|
| Molecular Weight |
292.12018
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| CAS # |
200626-61-5
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| SMILES |
O=C(C1=CC=C(Cl)C=C1Cl)N2N=NC3=CC=CC=C32
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| InChi Key |
UVNLAUGZMOPBPR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H7Cl2N3O/c14-8-5-6-9(10(15)7-8)13(19)18-12-4-2-1-3-11(12)16-17-18/h1-7H
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| Chemical Name |
(1H-benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone
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| Synonyms |
ITSA-1; ITSA 1; ITSA1.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 32 mg/mL (~109.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.56 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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