ITSA-1

Name: ITSA-1
Brand: MedChemExpress
SKU: HY-100508
Rating: 5.0 (16 reviews)

Cat. No.: HY-100508 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.

For research use only. We do not sell to patients.

ITSA-1 Chemical Structure

CAS No. : 200626-61-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 25	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 16 publication(s) in Google Scholar

14 Publications Citing Use of MCE ITSA-1

: ITSA-1 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Jan 14. [Abstract]; ITSA-1 (10 μM) nullifies the promoting impacts of sh-HDAC2 on H3K27ac and SNRK protein expression in HK-2 cells.

: ITSA-1 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2019 Mar 22;19(1):262. [Abstract]; Western blot is used to examine the protein levels of cell proliferation (PCNA), cell cycle (cyclinD1, CDK2 and p16) and EMT-associated genes (E-cadherin and Vimentin) in the treatment of TSA or TSA plus ITSA-1.

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Biological Activity
Purity & Documentation
References
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Description

ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation^[1].

IC₅₀ & Target^[1]

HDAC

In Vitro

ITSA-1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA-1 is also able to effect cell cycle rescue over longer duration^[1].
ITSA-1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells^[1].
ITSA-1 (50 μM; 2 hours; A549 and murine ES cells cells) treatment suppresses TSA-induced histone acetylation. Importantly, suppression of acetylation levels is only observable when ITSA1 is added concurrent with or post TSA treatment^[1].
ITSA-1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	Murine ES cells
Concentration:	50 μM
Incubation Time:
Result:	Served to revert the TSA-arrested population to a normal cell cycle distribution.

Apoptosis Analysis^[1]

Cell Line:	A549 cells
Concentration:	50 μM
Incubation Time:	5 hours
Result:	Reduced the number of apoptosis.

Western Blot Analysis^[1]

Cell Line:	A549 and murine ES cells
Concentration:	50 μM
Incubation Time:	2 hours
Result:	Reduced histone acetylation to the baseline level.

RT-PCR^[1]

Cell Line:	Murine ES cells
Concentration:	50 μM
Incubation Time:	30 minutes
Result:	Suppressed TSA-activated transcription.

In Vivo

ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS^+/ mice) balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	CBS^+/− mice^[2]
Dosage:	0.5 mg/kg
Administration:	Intraperitoneal injection; 3 times/week; for 8 weeks
Result:	Balanced deacetylation activity and suppressed IL-6 and TNF-α expression.

Molecular Weight

292.12

Formula

C₁₃H₇Cl₂N₃O

CAS No.

200626-61-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1N=NC2=CC=CC=C21)C3=CC=C(Cl)C=C3Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 32 mg/mL (109.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.56 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (286 KB) SDS (392 KB)

COA (258 KB) HNMR (254 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4233 mL	17.1163 mL	34.2325 mL	85.5813 mL
	5 mM	0.6847 mL	3.4233 mL	6.8465 mL	17.1163 mL
	10 mM	0.3423 mL	1.7116 mL	3.4233 mL	8.5581 mL
	15 mM	0.2282 mL	1.1411 mL	2.2822 mL	5.7054 mL
	20 mM	0.1712 mL	0.8558 mL	1.7116 mL	4.2791 mL
	25 mM	0.1369 mL	0.6847 mL	1.3693 mL	3.4233 mL
	30 mM	0.1141 mL	0.5705 mL	1.1411 mL	2.8527 mL
	40 mM	0.0856 mL	0.4279 mL	0.8558 mL	2.1395 mL
	50 mM	0.0685 mL	0.3423 mL	0.6847 mL	1.7116 mL
	60 mM	0.0571 mL	0.2853 mL	0.5705 mL	1.4264 mL
	80 mM	0.0428 mL	0.2140 mL	0.4279 mL	1.0698 mL
	100 mM	0.0342 mL	0.1712 mL	0.3423 mL	0.8558 mL

ITSA-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ITSA-1200626-61-5ITSA1ITSA 1HDACHistone deacetylasesInhibitorinhibitorinhibit

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ITSA-1

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ITSA-1 Related Antibodies

14 Publications Citing Use of MCE ITSA-1

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•Related Screening Libraries:

•Related Small Molecules:

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View All HDAC Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ITSA-1 Related Antibodies

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Complete Stock Solution Preparation Table

ITSA-1 Related Classifications

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