ITSA-1 | HDAC inhibitor | CAS#200626-61-5

MedKoo Cat#: 407434 | Name: ITSA-1

Description:

WARNING: This product is for research use only, not for human or veterinary use.

ITSA-1 (ITSA1) is selective HDAC inhibitor. ITSA-1 may prove to be valuable probes of many biological processes. Histone deacetylase (HDAC) inhibitors are being developed as new clinical agents in cancer therapy, in part because they interrupt cell cycle progression in transformed cell lines.

Chemical Structure

ITSA-1

CAS#200626-61-5

Theoretical Analysis

MedKoo Cat#: 407434

Name: ITSA-1

CAS#: 200626-61-5

Chemical Formula: C13H7Cl2N3O

Exact Mass: 290.9966

Molecular Weight: 292.12

Elemental Analysis: C, 53.45; H, 2.42; Cl, 24.27; N, 14.38; O, 5.48

Price and Availability

Size	Price	Availability
100mg	USD 350.00	2 Weeks
250mg	USD 650.00	2 Weeks
500mg	USD 950.00	2 Weeks
1g	USD 1,650.00	2 Weeks

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Related CAS #

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Synonym

ITSA-1; ITSA1.

IUPAC/Chemical Name

(1H-benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone

InChi Key

UVNLAUGZMOPBPR-UHFFFAOYSA-N

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

SMILES Code

O=C(C1=CC=C(Cl)C=C1Cl)N2N=NC3=CC=CC=C32

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

Since this study observed a decrease of HDACs expression in ALS-induced vEC inflammation (Figure 2D), this study induced HDACs expression in HSVECs under ALS by initiating ITSA-1 (150 μM) treatment and measured H3K9me3 expression and cell inflammation in ISTA-1 and ALS treatments. Taken together, these data suggest that the increased expressions of HDACs and H3K9me3 by ITSA-1 could reverse inflammation in ALS-induced vECs. Reference: Front Cell Dev Biol. 2021 Apr 9;9:642150. https://pubmed.ncbi.nlm.nih.gov/33898431/

In vivo activity:

A blockade of HDAC3 inhibition in CBS+/- mice by HDAC activator ITSA-1, led to the remodeling of histone landscapes in the genome and thereby attenuated histone acetylation-dependent inflammatory signaling. Collectively, restoration of H2S may provide a novel treatment for CBS-deficiency induced metabolic osteoporosis. Reference: Sci Rep. 2018 Oct 15;8(1):15226. https://pubmed.ncbi.nlm.nih.gov/30323246/

	Solvent	mg/mL	mM
Solubility
	Ethanol	3.5	11.98

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 292.12 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Wang TY, Chang MM, Li YJ, Huang TC, Chien S, Wu CC. Maintenance of HDACs and H3K9me3 Prevents Arterial Flow-Induced Venous Endothelial Damage. Front Cell Dev Biol. 2021 Apr 9;9:642150. doi: 10.3389/fcell.2021.642150. PMID: 33898431; PMCID: PMC8063156. 2. Shen Z, Liao X, Shao Z, Feng M, Yuan J, Wang S, Gan S, Ha Y, He Z, Jie W. Short-term stimulation with histone deacetylase inhibitor trichostatin a induces epithelial-mesenchymal transition in nasopharyngeal carcinoma cells without increasing cell invasion ability. BMC Cancer. 2019 Mar 22;19(1):262. doi: 10.1186/s12885-019-5482-y. PMID: 30902084; PMCID: PMC6431036. 3. Behera J, Kelly KE, Voor MJ, Metreveli N, Tyagi SC, Tyagi N. 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. doi: 10.1038/s41598-018-33149-9. PMID: 30323246; PMCID: PMC6189133.

In vitro protocol:

In vivo protocol:

1. Behera J, Kelly KE, Voor MJ, Metreveli N, Tyagi SC, Tyagi N. 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. doi: 10.1038/s41598-018-33149-9. PMID: 30323246; PMCID: PMC6189133.

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. PubMed PMID: 12770822.