MC1568 - HDAC 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMC1568Cat. No.: HY-16914CAS No.: 852475-26-4分式: CHFNO分量: 314.31作靶點(diǎn): HDAC作通路: Cell Cycle/DNA Damage; Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 18.5 mg/mL (58.86 mM; Need ult

2、rasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.1816 mL 15.9079 mL 31.8157 mL5 mM 0.6363 mL 3.1816 mL 6.3631 mL10 mM 0.3182 mL 1.5908 mL 3.1816 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 MC1568組蛋脫酰酶(HDAC II)的抑制劑，可于癌癥研究。IC50 & Target HDAC體外研究MC1568 a

3、rrests myogenesis by decreasing myocyte enhancer factor 2D (MEF2D) expression, by stabilizingthe HDAC4HDAC3MEF2D complex, and paradoxically, by inhibiting differentiation-induced MEF2Dacetylation 1. MC1568 and MC1575 inhibits IL-8 levels and cell proliferation in either unstimulated or PMA-1/3 Maste

4、r of Small Molecules 您邊的抑制劑師www.MedChemEstimulated melanoma cells. They acts by suppressing c-Jun binding to the IL-8 promoter, recruitment ofhistones 3 and 4, RNA polymerase II and TFIIB to the c-Jun promoter, and c-Jun expression 2. MC1568interferes with the RAR- and PPAR-mediated differentiation-

5、inducing signaling pathways. In F9 cells, thisinhibitor specifically blocks endodermal differentiation. In 3T3-L1 cells, MC1568 attenuates PPAR-inducedadipogenesis 3.體內(nèi)研究 MC1568 shows an apparent tissue-selective HDAC inhibition. In skeletal muscle and heart, MC1568 inhibitsthe activity of HDAC4 and

6、 HDAC5 without affecting HDAC3 activity, thereby leaving MEF2HDACcomplexes in a repressed state 1. MC1568 increases mortality and lesion volume and did not improvefunctional outcome. In addition, MC1568 decreases microtubule associated protein 2, phosphorylatedneurofilament heavy chain and myelin ba

7、sic protein immunoreactivity in the periinfarct cortex 4.PROTOCOLCell Assay 2 For proliferation studies, 15 103 cells are seeded onto 24-well plates in RPMI-1640 medium supplementedwith 10% heat-inactivated fetal bovine serum, 3 mM L-glutamine, 2% penicillin/streptomycin. After 24 h,untreated or HDA

8、Cis-treated cells are incubated with either vehicle alone or PMA (50 ng/mL) for 6 h, and cellproliferation is evaluated by MTT assay and by cell number counting 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Adult male Wistar rats (n=15-17/gro

9、up) are subjected to 2 h MCAO and orally gavaged with MC1568 (aAdministration 4 selective class IIa HDAC inhibitor), SAHA (a non-selective HDAC inhibitor), or vehicle-control for 7 daysstarting 24 h after MCAO. A battery of behavioral tests is performed. Lesion volume measurement andimmunohistochemi

10、stry are performed 28 days after MCAO 4MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Jun 14. J Cell Physiol. 2018 Jan;233(1):673-687.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nebbioso A, e

11、t al. Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity ofHDAC-MEF2complexes. EMBO Rep. 2009 Jul;10(7):776-82.2. Venza I, et al. Class II-specific histone deacetylase inhibitors MC1568 and MC1575 suppress IL-8 expression in human melanoma cells.Pigment Cel

12、l Melanoma Res. 2013 Mar;26(2):193-204.3. Nebbioso A, et al. HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation. J Mol Endocrinol. 2010Oct;45(4):219-28.4. Kassis H, et al. Class IIa histone deacetylases affect neuronal remodeling and functional outcome after stroke. Neurochem Int. 2016Jun;96:24-31.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCautio