|(1H-苯并[d][1,2,3]三唑-1-基)(2,4-二氯苯基)甲酮|CsnPharm

CAS No.: 200626-61-5

(1H-Benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone Catalog No. CSN10407

Synonyms: ITSA-1

ITSA-1 is activator of HDAC by suppressing TSA.

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400-920-2911

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技术信息

生物活性

描述Histone acetylation is tightly associated with transcriptional regulation, differentiation, and cell cycle progression in mammalian cell lines and is controlled by histone deacetylases (HDACs). Trichostatin A (TSA) is an inhibitor of HDAC that promotes acetylation of α-tubulin as well as histones. ITSA-1 is an HDAC activator via TSA suppression. In TSA-treated A549 cells (300 nM, 22 hr), the total apoptotic rate was 43%, while this number was reduced to 1% in TSA-treated cells that also received ITSA1 (50 μM, 5 h). In actively cycling cells, TSA-treatment led to increase in G0-G1 (41%) and G2-M (55%) but decrease in S phase (4%), which were reverted by ITSA1 treatment. In murine ES cells, ITSA1 (50 μM, 2 h) dramatically suppressed TSA-induced acetylation within 30 min. ITSA1 at 10 μM reversed TSA-induced cell apoptosis and mesenchymal morphological changes in NPC cells and also enhanced cell migration ability. It was also showed that ITSA1 elevated protein level of HDAC1, HDAC2, HDAC4, HDAC7, HDAC10 and HDAC11 in CNE2 cells and HDAC1 and HDAC7 in C666–1 cells which were attenuated by TSA.
作用机制ITSA-1 activates HDAC by suppressing TSA, the inhibitor of HDAC.
动物研究
剂量
Mice: 0.5 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.5 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Haggarty SJ, Koeller KM, et al. Domain-selective small-molecule inhibitor of histone deacetylase 6 (HDAC6)-mediated tubulin deacetylation. Proc Natl Acad Sci U S A. 2003 Apr 15;100(8):4389-94.
[2] Koeller KM, Haggarty SJ, et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation. Chem Biol. 2003 May;10(5):397-410.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4232 mL
- 17.1162 mL
- 34.2325 mL
- 5 mM
- 0.6846 mL
- 3.4232 mL
- 6.8465 mL
- 10 mM
- 0.3423 mL
- 1.7116 mL
- 3.4232 mL

技术信息

CAS号

200626-61-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H7Cl2N3O

运输

蓝冰

分子量

292.12

别名

ITSA-1

溶解度

DMSO	58.0 mg/mL (198.5 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (17.1 mM)

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(1H-Benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone Catalog No. CSN10407

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