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AP1903

Chemical Structure : AP1903

CAS No.: 195514-63-7

AP1903 (Rimiducid;AP-1903)

Catalog No.: PC-35967Not For Human Use, Lab Use Only.

AP1903 (Rimiducid, AP-1903) is a potent, specific synthetic ligand of FKBP Phe36Val mutant (F36V-FKBP) with binding IC50 of 1.8 nM.

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Biological Activity

AP1903 (Rimiducid, AP-1903) is a potent, specific synthetic ligand of FKBP Phe36Val mutant (F36V-FKBP) with binding IC50 of 1.8 nM.
AP1903 displaces the Fluoresceinated FK506 probe from F36V-FKBP with an IC50 of 5 nM, but shows negligible binding activity to the wild-type protein.
AP1903 elicited potent and dose-dependent apoptotic death of human fibrosarcoma line HT1080 expressing dimerizer-dependent Fas constructs with EC50 of 0.1 nM.
AP1903 induces activation of Fas signaling both in vitro and in vivo, AP1903 is a lipid-permeant dimerizing ligand induced oligomerization and activation of FKBP.

Physicochemical Properties

M.Wt 1411.65
Formula C78H98N4O20
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S,2R,2'R)-(1R,1'R)-((((ethane-1,2-diylbis(azanediyl))bis(2-oxoethane-2,1-diyl))bis(oxy))bis(3,1-phenylene))bis(3-(3,4-dimethoxyphenyl)propane-1,1-diyl) bis(1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate)

References

1. Clackson T, et al. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10437-42.

2. Richard RE, et al. Blood. 2000 Jan 15;95(2):430-6.

3. Thomis DC, et al. Blood. 2001 Mar 1;97(5):1249-57.

4. Narayanan P, et al. J Clin Invest. 2011 Apr;121(4):1524-34.

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