Romidepsin
Cat. No.：YN270296
| 产品名称: | Romidepsin |
| CAS No.: | 128517-07-7 |
| Chemical Name: | cyclic (3→5)-disulfide-cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-3S-hydroxy-7-mercapto-4E-heptenoyl-D-valyl-D-cysteinyl] |
| Synonyms: | 罗米地辛; FK 228; FR 901228; NSC 630176 |
| 分子量: | 540.70 |
| 分子式: | C₂₄H₃₆N₄O₆S₂ |
| SMILES: | C/C=C(NC([C@@H](CSSCC/C=C/[C@@H](O1)CC2=O)NC([C@@H](C(C)C)N2)=O)=O)/C(N[C@@H](C(C)C)C1=O)=O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Romidepsin (FK 228) 是具有抗肿瘤活性的组蛋白去乙酰化酶 (HDAC) 抑制剂，抑制 HDAC1，HDAC2，HDAC4 和 HDAC6，IC50值分别为 36 nM，47 nM，510 nM 和 1.4 μM。Romidepsin (FK 228) 由紫色杆菌产生，诱导 G2/M 细胞周期阻滞和凋亡 (apoptosis)。 |
| IC50和靶点: | [{name:"HDAC1:36 nM (IC50)"},{name: "HDAC2:47 nM (IC50)"},{name: "HDAC4:510 nM (IC50)"},{name: "HDAC6:14000 nM (IC50)"}] |
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Nakajima, H., Kim, Y.B., Terano, H., et al.FR901228, a potent antitumor antibiotic, is a novel histone descetylase inhibitorExp. Cell Res.241(1),126-133(1998)
Wang, C., Henkes, L.M., Doughty, L.B., et al.Thailandepsins: Bacterial products with potent histone deacetylase inhibitory activities and broad-spectrum antiproliferative activitiesJ. Nat. Prod.74(10),2031-2038(2011)
Mazitschek, R., Patel, V., Wirth, D.F., et al.Development of a fluorescence polarization based assay for histone deacetylase ligand discoveryBioorg. Med. Chem. Lett.18(9),2809-2812(2008)
Ueda, H., Manda, T., Matsumoto, S., et al.FR901228, a novel antitumor bicyclic depsipeptide produced by Chromobacterium violaceum No. 968. III. Antitumor activities on experimental tumors in miceJ. Antibiot. (Tokyo)47(3),315-323(1994)
VanderMolen, K.M., McCulloch, W., Pearce, C.J., et al.Romidepsin (Istodaxr, NSC 630176, FR901228, FK228, depsipeptide): A natural product recently approved for cutaneous T-cell lymphomaJ. Antibiot. (Tokyo)67(8),525-231(2015)
Coiffier, B., Federico, M., Caballero, D., et al.Therapeutic options in relapsed or refractory peripheral T-cell lymphomaCancer Treat. Rev.40(9),1080-1088(2014)
Qin, L., Ma, K., Wang, Z.-J., et al.Social deficits in Shank3-deficient mouse models of autism are rescued by histone deacetylase (HDAC) inhibitionNat. Neurosci.21(4),564-575(2018)
