MC1568 - HDAC 抑制剂 - 生命科学试剂 - 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 : 18.5 mg/mL (58.86 mM; Need ult

2、rasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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。BIOLOGICAL ACTIVITY物活性 MC1568组蛋脱酰酶(HDAC II)的抑制剂，可于癌症研究。IC50 & Target HDAC体外研究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 您边的抑制剂师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.体内研究 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.户使本产品发表的科研献 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 您边的抑制剂师www.MedChemEMcePdfHeightCautio