Trichostatin-A-TSA-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETrichostatin ACat. No.: HY-15144CAS No.: 58880-19-6Synonyms: TSA分式: CHNO分量: 302.37作靶点: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25 mg/mL (8

2、2.68 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.3072 mL 16.5360 mL 33.0721 mL5 mM 0.6614 mL 3.3072 mL 6.6144 mL10 mM 0.3307 mL 1.6536 mL 3.3072 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使

3、；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.27 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.27 mM); Clear solution1/3 Master of Small Molecules 您边

4、的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Trichostatin A (TSA)有效的，特异的组蛋去酰化酶类型 I 和 II (HDAC class I/II) 抑制剂，对 HDAC 的IC50 值为 1.8 nM。IC50 & Target HDAC1.8 nM (IC50)体外研究 Trichostatin A is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.Trichostatin A (TSA) inhibit

5、s proliferation of eight breast carcinoma cell lines with meanSD IC50 of124.4120.4 nM (range, 26.4-308.1 nM). HDAC inhibitory activity of Trichostatin A is similar in all cell lineswith mean IC50 of 2.40.5 nM (range, 1.5-2.9 nM) 1. Trichostatin A (330 nM) increases Gs proteinexpression in human myom

6、etrial cells, but does not increase Gs mRNA levels 2. Trichostatin A (20-75nM)induces minimal cytotoxicity to adipose-derived stem cells (ADSCs), and enhances the osteogenicdifferentiation capacity of ADSCs 3. In addition, Trichostatin A (0, 10, 100, 500 nM) dose-dependentlydecreases HDAC class I/II

7、 activity 4.体内研究 Trichostatin A (500 g/kg, s.c.) pronounces antitumor activity without causing any measurable toxicity indoses of up to 5 mg/kg by s.c. injection, in randomized controlled efficacy studies using the N-methyl-N-nitrosourea carcinogen-induced rat mammary carcinoma model 1.PROTOCOLCell

8、Assay 3 Cells are cultured in a 96-well plate at 1103 cells per well with 100 L complete DMEM in the presence orabsence of a HDAC inhibitor Trichostatin A for 72 h. Cytotoxicity is measured by performing WST-8 assayusing a CCK-8 cell proliferation kit. The 450 nm absorbance is measured with a microp

9、late reader. Allexperiments are carried out in triplicate and 3 independent experiments are performed 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 1Administration 1 Twelve rats are randomized to receive 500 g/kg Trichostatin A in 50 L D

10、MSO, or 50 L DMSO as vehiclecontrol, by s.c. injection twice weekly for 4 weeks. In subsequent studies, 30 rats are randomized to receiveTrichostatin A 500 g/kg in 50 L DMSO, or 50 L DMSO as vehicle control, by s.c. injection daily for 4weeks. Weekly tumor measurements, estimated tumor volumes, and

11、body mass are recorded for eachanimal. Animals are sacrificed at the end of the 4-week study period; palpable tumors are resected andimmediately snap-frozen in liquid nitrogen. Animals with tumors 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发

12、表的科研献 Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):9967-76. Kidney Int. 2017 Sep;92(3):669-679. Theranostics. 2019 Apr 13;9(9):2424-2438.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Cell Death Dis. 2018 Apr 27;9(5):497. J Mol Med (Berl). 2019 Jun 14.See more customer validations on HYPERLINK /

13、www.MedChemEREFERENCES1. Vigushin DM et al. Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo. ClinCancer Res. 2001 Apr;7(4):971-6.2. Karolczak-Bayatti M, et al. Expression of the GTP-Binding Protein Gs in Human Myometrial Cells is Regulat

14、ed by Ubiquitination andProtein Degradation: Involvement of Proteasomal Inhibition by Trichostatin A.,Reprod Sci. 2012 Aug 8.3. Hu X, et al. Histone deacetylase inhibitor trichostatin A promotes the osteogenic differentiation of rat adipose-derived stem cells byaltering the epigenetic modifications on Runx2 promoter in a BMP signaling-dependent manner.,Stem Cells Dev. 2012 Aug 8.4. Azechi T, et al. Trichostatin A, an HDAC class I/II inhibitor, promotes Pi-induced vascular calcification via up-regulation of the expressionof alkaline phosphatase. J Atheroscler Thr