1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEActinomycin DCat. No.: HY-17559CAS No.: 50-76-0Synonyms: Dactinomycin; Actinomycin IV分式: CHNO分量: 1255.42作靶點(diǎn): DNA/RNA Synthesis; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy儲(chǔ)存式: 4C, stored under nitrogen* In solvent : -80C, 6 m

2、onths; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 27 mg/mL (21.51 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (1.66 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (1.66 mM); Suspended solution; Need ultrasonic1/3 Master of Sm

3、all Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Actinomycin D 抑制 DNA 修復(fù)，IC50 為 0.42 M。IC50 & Target IC50: 0.42 M (DNA repair) 1體外研究 Actinomycin D is an inhibitor of DNA transcription and replication 1. Actinomycin D markedly reduces thevascular smooth muscle cells (SMC) proliferation via the

4、 inhibition of BrdU incorporation at 80 nM. This isfurther supported by the G1-phase arrest using a flowcytometric analysis. Actinomycin D is extremely potentwith an inhibitory concentration IC50 at 0.4 nM, whereas the lethal dose LD50 is at 260 microM. The proteinexpression levels of proliferating

5、cell nuclear antigen (PCNA), focal adhesion kinase (FAK), and Raf are allsuppressed by Actinomycin D. Extracellular signal-regulated kinases (Erk) involved in cell-cycle arrest arefound to increase by Actinomycin D 2.體內(nèi)研究 The pluronic gel containing 80 nM and 80M Actinomycin D is applied topically t

6、o surround the rat carotidadventitia, the thickness of neointima is substantially reduced (45 and 55%, respectively) 2. Mice in theActinomycin D and fludarabine group lives significantly longer than the control group with P values of 3.PROTOCOLKinase Assay 1 Actinomycin D is co-incubated for 3 h at

7、30C with a reaction mixture containing: 120 mg of a whole-cellextract of HeLa cells, 70 mM KCl, 0.4 mM each of dGTP, dCTP, dATP, and digoxygenylated-dUTP inreaction buffer containing 40mM Hepes-KOH (pH 7.6), 5 mM MgCl2, 0.5 mM Dithiotreitol, 2 mM EGTA, 10mM phosphocreatine, 50 mg/mL creatine phospha

8、te, and 360 mg/mL of bovine serum albumin. During thisreaction, DNA damage is recognized and the excised patches are replaced by neosynthesized DNAfragments. Throughout this DNA synthesis, digoxygenylated-dUMPs are incorporated. The DNA repairreaction is stopped by three washes 1.MCE has not indepen

9、dently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 The original E-TCL1a transgenic mice have been backcrossed to C57BL/6 mice for 9 generations.TheC57BL/6 wild-type mice are engrafted with tumor cells from E-TCL-1 transgenic mice. The percentage

10、 ofCD5+/CD19+ cells in the peripheral blood is routinely checked in mice by taking blood from the tail vein andanalyzing it via flow cytometry. When the percentage of tumor cells in the peripheral blood reached 40-60%,treatment is started. Actinomycin D (0.06 mg/kg by 10 days) is applied daily via i

11、.p. injections.MCE 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) Cell Metab. 2019 Jul 2;30(1):157-173.e7 Cell Res. 2019 Jan;29(1):23-41. Nucleic Acids Res. 2019 Jun 19. pii: gkz532.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Mol Cancer.

12、2019 Jun 24;18(1):112. Mol Cancer. 2018 Mar 6;17(1):69.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Barret JM, et al. Evaluation of DNA repair inhibition by antitumor or antibiotic drugs using a chemiluminescence microplateassay.Carcinogenesis. 1997 Dec;18(12):2441-5.2. Wu C

13、H, et al. The molecular mechanism of actinomycin D in preventing neointimal formation in rat carotid arteries after balloon injury. JBiomed Sci. 2005;12(3):503-12.3. Merkel O, et al. Actinomycin D induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.Leukemia. 2012 Dec;26(12):2508-16.McePd