E8405
EB-47
≥98% (HPLC), solid
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关于此项目
经验公式（希尔记法）:
C24H29N9O6Cl2
化学文摘社编号:
分子量:
610.45
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality Segment
assay
≥98% (HPLC)
form
solid
solubility
H2O: soluble 10 mg/mL
shipped in
dry ice
storage temp.
−20°C
SMILES string
Nc1ncnc2n(cnc12)[C@@H]3O[C@@H]([C@@H](O)[C@H]3O)C(=O)N4CCN(CC4)CC(=O)Nc5cccc6C(=O)NCc56
InChI
1S/C24H27N9O6/c25-20-16-21(28-10-27-20)33(11-29-16)24-18(36)17(35)19(39-24)23(38)32-6-4-31(5-7-32)9-15(34)30-14-3-1-2-12-13(14)8-26-22(12)37/h1-3,10-11,17-19,24,35-36H,4-9H2,(H,26,37)(H,30,34)(H2,25,27,28)/t17-,18+,19-,24+/m0/s1
InChI key
DDFLFKTXUWPNMV-UAKAABGRSA-N
Application
EB-47 has been used as a poly [ADP-ribose] polymerase 1 (PARP/PARP1/PARPi) inhibitor:
- to investigate its effect on the activity of matrix metalloproteinase-2 (MMP-2) and compare its inhibitory potencies with the MMP inhibitors
- in treating human acute monocytic leukemia cells to confirm if PARP1 is responsible for the decrease in high mobility group box protein 1 (HMGB1) supernatant levels
- to study chromosomal aberrations in response to ionizing radiation (IR) and PARPi in BRCA1-deficient cells that overcome growth arrest (BOGA) cells
Biochem/physiol Actions
1-piperazineacetamide-4-[1-(6-amino-9H-purin-9-yl)-1-deoxy-d-ribofuranuron]-N-(2,3-dihydro-1H-isoindol-4-yl)-1-one (EB-47) can mimic the substrate NAD+ binding. This inhibitor targets the nicotinamide (NI) and adenosine (AD)-subsite within the tankyrase 2 (TNKS2) catalytic domain. EB-47 is one of the most effective TNKS2 inhibitors, with an IC50 of 32 nM, in the presence of piperazine and succinyl linkers that connect the adenosine and isoindolinone cores.
Potent inhibitor of poly (ADP-ribose) polymerase (PARP).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)