FK 506

Name: FK 506
Brand: Tocris Bioscience
SKU: 3631
Rating: 5 (2 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 3631

(2)

Citations (127)

COA / SDS

Potent calcineurin inhibitor; immunosuppressant

Key Product Details

Description:	Potent calcineurin inhibitor; immunosuppressant
Alternative 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)
Molecular Weight:	804.02

View Full Technical Details for FK 506

Technical Data
Citations / Reviews (2)

Biological Activity for FK 506

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.

Technical Data for FK 506

M. Wt	804.02
Formula	C₄₄H₆₉NO₁₂
Storage	Store at -20°C
Purity	≥99% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for FK 506

	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 will 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

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References for FK 506

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