ITSA-1

SKU: orb1225755

Description

A small molecule suppressor that counteracts trichostatin A (TSA)-induced cell cycle arrest, histone acetylation and transcriptional activation; also suppresses acetylation of cytoplasmic alpha-tubulin as well as histones induced by hydroxamic acid-based HDAC inhibitors like TSA and SAHA.

Key Properties

• CAS Number: 200626-61-5
• MW: 292.1202
• Purity: >98% (HPLC)
• Formula: C₁₃H₇Cl₂N₃O
• SMILES: O=C(C1=CC=C(Cl)C=C1Cl)N2N=NC3=CC=CC=C32
• Target: HDAC
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• 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. Animal model: CBS+/ mice. 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.
• 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. ITSA-1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells. 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. ITSA-1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells. Cell Cycle Analysis 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 Cell line: A549 cells. Concentration: 50 μM. Incubation time: 5 hours. Result: Reduced the number of apoptosis. Western blot analysis. Cell line: A549 and murine ES cells. Concentration: 50 μM. Incubation time: 2 hours. Result: Reduced histone acetylation to the baseline level. RT-PCR Cell line: Murine ES cells. Concentration: 50 μM. Incubation time: 30 minutes. Result: Suppressed TSA-activated transcription.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ITSA1 | ITSA 1

Quick Database Links

Gene Symbol

HDAC