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
9 results for "FKBP12 Small Molecules and Peptides" in Products
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.
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) |
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) |
mTOR inhibitor; Immunosuppressant
| Alternate Names: | RAD001 |
| Chemical Name: | 42-O-(2-Hydroxyethyl)rapamycin |
| 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) |
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) |
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) |
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) |
