ITSA-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子抑制剂，可抵抗曲古抑菌素 A (TSA) 诱导的细胞周期停滞。

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.

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 AnalysisCell 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.

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+/? miceDosage: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.

ITSA1 | ITSA 1

Cell Cycle/DNA Damage

HDAC

HDAC

Cancer

——

200626-61-5

292.1202

C13H7Cl2N3O

>98% (HPLC)

DMSO: ≥ 32 mg/mL

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

Methanone, 1H-benzotriazol-1-yl(2,4-dichlorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years