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/ Products Classification 点击展开+Cat. Number | A6132 |
Chemical Name | A6132 组蛋白脱乙酰酶抑制剂Apicidin 183506-66-3 |
CAS Number | [183506-66-3] |
Mol. Formula | C34H49N5O6 |
Mol. Weight | 623.78 |
Qty 1 |
1mg |
Qty 2 | 10mg |
Appearance | White Crystal Powder |
Application Notes | ≥98% |
Synonym | methyl 6-[(3S,6S,9S,12R)-3-butan-2-yl-6-[(1-methoxyindol-3-yl)methyl]-2,5,8, 11-tetraoxo-1,4,7,10-tetrazabicyclo[10.4.0]hexadecan-9-yl]hexanoate InChI: InChI=1S/C33H47N5O7/c1-5-21(2)29-33(43)37-18-12-11-16-27(37)32(42)34-24 (14-7-6-8-17-28(39)44-3)30(40)35-25(31(41)36-29)19-22-20-38(45-4)26-15- 10-9-13-23(22)26/h9-10,13,15,20-21,24-25,27,29H,5-8,11-12,14,16-19H2, 1-4H3,(H,34,42)(H,35,40)(H,36,41)/t21?,24-,25-,27+,29-/m0/s1 |
Melting Pt. | 190°C |
Solubility | Ethano (0.9 mg/mL)l, DMSO (0.9 mg/mL), Dichloromethane. Slightly soluble in water, methanol |
Storage condition | 4°C |
References | DescriptionApicidin is a cyclic tetrapeptide that inhibits histone deacetylase (HDAC) and exhibits anticancer benefit. In oral squamous cell carcinoma cells, apicidin upregulates expression of p21, inducing G2/M phase cell cycle arrest, apoptosis, and autophagy. In non-small cell lung cancer (NSCLC) cells, apicidin downregulates expression of checkpoint kinase (CHK) 1, decreases phosphorylation of cdc25C and cdc2, and upregulates expression of cdc25A, inducing apoptotic cell death. Additionally, apicidin increases apoptosis in Brc-Abl positive leukemia cells through disruption of the mitochondrial membrane potential, activation of caspases 3, 8, and 9, cleavage of poly(ADP)-ribose polymerase (PARP), and release of cytochrome c. Apicidin also induces apoptosis in eosinophils and neutrophils. |