FK 506
Tocris Bioscience, part of Bio-Techne | Catalog # 3631
Potent calcineurin inhibitor; immunosuppressant
Key Product Details
Description
Potent calcineurin inhibitor; immunosuppressant
Alternative Names
Tacrolimus,Fujimycin
Product Description
FK 506 is a potent calcineurin (protein phosphatase 2B) inhibitor that requires FK 506-binding protein 12 (FKBP12) for activity (IC50 = 3 nM). Inhibits secretion of IL-1, IL-2 (IC50 = 1 nM), IL-3, IL-4, IL-6 (IC50 = 35 nM), GM-CSF, TNFα (IC50 = 10 nM), IFNγ and Myc from activated T cells in vitro. Exhibits potent immunosuppressive, neuroprotective and anticonvulsant activity in vivo. Identified as targeting human host cell proteins that interact with SARS-CoV-2.Analog also available.
Product Specifications
Molecular Weight
804.02
Formula
C44H69NO12
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
CAS Number
104987-11-3
PubChem ID
445643
InChI Key
QJJXYPPXXYFBGM-LFZNUXCKSA-N
SMILES
O[C@H]1[C@H](OC)C[C@H](/C=C(C)/[C@@H](O4)[C@H](C)[C@@H](O)CC([C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@@]2([H])O[C@](C(C(N3[C@@](C4=O)([H])CCCC3)=O)=O)(O)[C@H](C)C[C@@H]2OC)=O)CC1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 80.4 | 100 | |
| Ethanol | 80.4 | 100 |
Preparing Stock Solutions
for FK 506
The following data is based on the product molecular weight 804.02
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.24 mL | 6.22 mL | 12.44 mL |
| 5 mM | 0.25 mL | 1.24 mL | 2.49 mL |
| 10 mM | 0.12 mL | 0.62 mL | 1.24 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.25 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Gordon A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 2020 PMID: 32353859
- Baughman Tissue distribution and abundance of human FKBP51, and FK506-binding protein that can mediate calcineurin inhibition. Biochem.Biophys.Res.Commun. 1997 PMID: 9125197
- Sierra-Paredes and Sierra-Marcuno Ascomycin and FK506: Pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci.Ther. 2008 PMID: 18482098
- Fruman The complex of FK506-binding protein 12 and FK506 inhibits calcineurin phosphatase activity and IgE activation-induced cytokine transcripts, but not exocytosis, in mouse mast cells. J.Immunol. 1995 PMID: 7530743
Product Specific Notices for FK 506
For research use only
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