Molecular Formula | C13H7Cl2N3O |
Molar Mass | 292.12 |
Melting Point | 119-121°C |
Solubility | DMSO: ~28mg/mL |
Appearance | solid |
Color | White to Off-White |
Storage Condition | Inert atmosphere,2-8°C |
In vitro study | ITSA1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA1 is also able to effect cell cycle rescue over longer duration. ITSA1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells. ITSA1 (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. ITSA1 (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. |
In vivo study | ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS +/− mice) treatment 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. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.423 ml | 17.116 ml | 34.233 ml |
5 mM | 0.685 ml | 3.423 ml | 6.847 ml |
10 mM | 0.342 ml | 1.712 ml | 3.423 ml |
5 mM | 0.068 ml | 0.342 ml | 0.685 ml |
biological activity | ITSA-1 is an activator of HDAC, which can offset trichostatin A (trichostatin A, TSA)-induced cell cycle arrest, histone acetylation and transcription levels. |
target | HDAC |
in vitro study | ITSA1 (50 μM; a549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA1 is also able to effect cell cycle over longer duration. ITSA1 (50 μ M; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells. ITSA1 (50 μ M; 2 hours; A549 and murine es 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. ITSA1 (50 μ M; 30 minutes; Murine ES cells) suppresses TSA-activated transcription in murine ES cells. Cell Cycle Analysis Cell Line: Murine ES cells Concentration: 50 μ m Incubation Time: Result: Served to reverse the TSA-arrested population to a normal cell 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. |
Cell Line: | Murine ES cells A549 cells A549 and murine ES cells Murine ES cells |
Concentration: | 50 μM 50 μM 50 μM 50 μM |
Incubation Time: | 5 hours 2 hours 30 minutes |
Result: | Served to revert the TSA-arrested population to a normal cell cycle distribution. Reduced the number of apoptosis. Reduced histone acetylation to the baseline level. Suppressed TSA-activated transcription. Balanced deacetylation activity and suppressed IL-6 and TNF-α expression. |
in vivo study | ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS /− nice) treatment balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling. Animal Model: CBS /− nice 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. |
Animal Model: | CBS /− mice |
Dosage: | 0.5 mg/kg |
Administration: | Intraperitoneal injection; 3 times/week; for 8 weeks |