FKBP12: Small Molecules and Peptides
FK506 binding protein, also called FKBP12 and FKBP1A, was originally characterized as a peptidyl-prolyl isomerase that catalyzes the transition between cis- and trans-proline residues critical for proper folding of proteins. The macrolide immunosuppressants FK506 (Tacrolimus) and rapamycin bind to FKBP12 with high affinity, while the structurally related-compound cyclosporine binds with a much lower affinity. The binding of these drugs causes FKBP12 to become a potent inhibitor of calcineurin phosphatase activity and TOR kinase activity. Knockout mice lacking FKBP12 are morphologically normal, but develop cardiomyopathies that may be related to dysregulation of ryanodyne receptors.
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FKBP12: Small Molecules and Peptides
FK506 binding protein, also called FKBP12 and FKBP1A, was originally characterized as a peptidyl-prolyl isomerase that catalyzes the transition between cis- and trans-proline residues critical for proper folding of proteins. The macrolide immunosuppressants FK506 (Tacrolimus) and rapamycin bind to FKBP12 with high affinity, while the structurally related-compound cyclosporine binds with a much lower affinity. The binding of these drugs causes FKBP12 to become a potent inhibitor of calcineurin phosphatase activity and TOR kinase activity. Knockout mice lacking FKBP12 are morphologically normal, but develop cardiomyopathies that may be related to dysregulation of ryanodyne receptors.
9 results for "FKBP12 Small Molecules and Peptides" in Products
Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
| Chemical Name: | 1-[(2S)-1-Oxo-2-(3,4,5-trimethoxyphenyl)butyl]-(2S)-2-piperidinecarboxylate (1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]hexyl]amino]-2-oxoethoxy]phenyl]propyl ester |
| Purity: | ≥98% (HPLC) |
Selective binding ligand for FKBP12F36V; precursor for dTAG compounds
| Chemical Name: | 2-(2-((R)-3-(3,4-Dimethoxyphenyl)-1-(((S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carbonyl)oxy)propyl)phenoxy)acetic acid |
| Purity: | ≥98% (HPLC) |
Fluorescent probe for labeling mutant FKBP12 (F36V) proteins
| Chemical Name: | (R)-1-(2-(2-((3',6'-Dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9'-xanthen]-5-yl)amino)-2-oxoethoxy)phenyl)-3-(3,4-dimethoxyphenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate |
| Purity: | ≥95% (HPLC) |
Potent calcineurin inhibitor; immunosuppressant
| Alternate Names: | Tacrolimus,Fujimycin |
| Chemical Name: | (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone |
| Purity: | ≥99% (HPLC) |
mTOR inhibitor; Immunosuppressant
| Alternate Names: | RAD001 |
| Chemical Name: | 42-O-(2-Hydroxyethyl)rapamycin |
| Purity: | ≥98% (HPLC) |
First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
| Chemical Name: | (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-((19-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)-2,18-dioxo-7,10,13-trioxa-3,17-diazanonadecyl)oxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate |
| Purity: | ≥98% (HPLC) |
Affinity probe for mutant FKBP12F36V proteins
| Chemical Name: | (R)-3-(3,4-Dimethoxyphenyl)-1-(2-((2,16-dioxo-20-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-6,9,12-trioxa-3,15-diazaicosyl)oxy)phenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate |
| Purity: | ≥98% (HPLC) |
Selective binding ligand for FKBP12F36V
| Chemical Name: | (1R)-1-[3-(Carboxymethoxy)phenyl]-3-(3,4-dimethoxyphenyl)propyl (2S)-1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-2-piperidinecarboxylate |
| Purity: | ≥98% (HPLC) |
Chemical inducer of proximity for dTAG protein FKBPF36V and ecDHFR tags
| Chemical Name: | (R)-1-(3-(2-((3-(4-((2,4-Diaminopyrimidin-5-yl)methyl)-2,6-dimethoxyphenoxy)propyl)amino)-2-oxoethoxy)phenyl)-3-(3,4-dimethoxyphenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate |
| Purity: | ≥98% (HPLC) |
