Description
EB-47 dihydrochloride, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD+ and extends from the nicotinamide to the adenosine subsite.
Product information
CAS Number: 1190332-25-2
Molecular Weight: 610.45
Formula: C24H29Cl2N9O6
Chemical Name: 2-{4-[(2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolane-2-carbonyl]piperazin-1-yl}-N-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)acetamide dihydrochloride
Smiles: Cl.Cl.NC1=NC=NC2=C1N=CN2[C@@H]1O[C@@H]([C@@H](O)[C@H]1O)C(=O)N1CCN(CC(=O)NC2=CC=CC3=C2CNC3=O)CC1
InChiKey: VVMQSDIMNDTMII-MYXHFVDASA-N
InChi: InChI=1S/C24H27N9O6.2ClH/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);2*1H/t17-,18+,19-,24+;;/m0../s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (102.38 mM; Need ultrasonic). H2O : 33.33 mg/mL (54.60 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
EB-47 dihydrochloride shows inhibition in excess of 50% with CdPARP, and it is able to inhibit CdPARP and HsPARP with IC50 values of 0.86 and 1.0 µM, respectively.
In Vivo:
EB-47 dihydrochloride (2 μM; 5 days) decreases the number of embryo implantation sites and blastocysts at day 5. PARP1 participates in the process of embryo implantation.
Products are for research use only. Not for human use.
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