Tacrolimus (FK506)

Catalog No.S5003 Synonyms: FR900506

Tacrolimus (FK506) Chemical Structure

Molecular Weight(MW): 804.02

Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 90 In stock
USD 170 In stock
USD 430 In stock
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7 Customer Reviews

  • FK506 reduces NCCE(Non-capacitative calcium entry) independently of its inhibitory effect in CaN activity. Fura-2-loaded human platelets were suspended in HBS medium containing 300 μM Ca2+ and preincubated for 5 min with increasing concentration of FK506 (0.5-50 μM), after which OAG (100 μM) was added to initiate NCCE.

    Biochim Biophys Acta, 2015, 1853(10 Pt A):2684-96.. Tacrolimus (FK506) purchased from Selleck.

    FK506 production of S. tsukubaensis L19 and its recombinant pression of fkbN in S. tsukubaensis L19); L22, S. tsukubaensis L22 (overexpression of tcs7 in S. tsukubaensis L19); L23, S. tsukubaensis L23 (overexpression of fkbN and tcs7 in S. tsukubaensis L19).

    J Ind Microbiol Biotechnol, 2016, 43(12):1693-1703.. Tacrolimus (FK506) purchased from Selleck.

  • Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry.

    Biochim Biophys Acta 2013 1833(3), 652-62. Tacrolimus (FK506) purchased from Selleck.

    Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. I IL-17A, J TARC, K IL-13, L IL-1ra, M IL-5, N IL-10.

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. A IL-1β, B IL-6, C IFNγ, D MCP-1

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

    Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. E IL-8, F IP-10, G TNFα, H IL-4

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • JCI Insight, 2016, 1(10):e86331.. Tacrolimus (FK506) purchased from Selleck.

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Biological Activity

Description Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex.
Targets
FKBP12 [1]
(T cells)
In vitro

FK-506 and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. [1] FK-506 prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. [2] FK 506 binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). FK-506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. [3] FK-506 and CsA exert nearly identical biological effects in cells by inhibiting the same subset of early calcium-associated events involved in lymphokine expression, apoptosis, and degranulation. FK-506 binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs). [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
rat RBL2H3 cells NYTkNW9ZTnWwY4Tpc44h[XO|YYm= NEH3eHMyPiCq NFnlepRKdmirYnn0bY9vKG:oIGTOSk1idHCqYTDwdo9lfWO2aX;uJIlvKHKjdDDSRmwzUDNiY3XscJMh[W[2ZYKgNVYhcHK|IHL5JGVNUVODLDDJR|UxRTBwMkWgcm0> NVjyUXRXOjN5OUGwO|Y>
rat RBL2H3 cells M4noXWZ2dmO2aX;uJIF{e2G7 NY\rVZB1OTVibXnudy=> MWTBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJJJifCCUQlyyTFMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDEUnAuSlODLXnu[JVk\WRiVF7GMYFteGijIIDyc4R2[3Srb36gdJJmcW6ldXLheIVlKG[xcjCxOUBucW6|IIDybY9zKESQUD3CV2Eh[2ijbHzlcodmKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhTUyLU1GsJGlEPTB;MD6yOUBvVQ>? NUXlZpoyOjJ2MUCwPFQ>
human T-cell M{DZfHBzd2yrZnXyZZRqd25iYYPzZZk> MUHJckB3cXS{bzDpcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVD3j[YxtKHC{b3zp[oVz[XSrb36sJGlEPTB;MD61JI5O MkjNO|U{PzN|MR?=
human WiDr cells Mo[zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3H6OWlvcGmkaYTpc44hd2ZiU1HQNVMxKG2nZHnheIVlKGOnbHyg[5Jwf3SqIHnuJIh2dWGwIGfpSJIh[2WubIOsJGlEPTB;MUCuPUBvVQ>? MYGxO|Y1OzFzMh?=
human U251 cells NX3ScIRmTnWwY4Tpc44h[XO|YYm= MkH2TY5pcWKrdHnvckBw\iCVQWCxN|AhcW5iVlXHSk1{fGmvdXzheIVlKGi3bXHuJHUzPTFiY3XscJMh[nliUFzBVEBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVE{Njhibl2= NXfkeJpbOTd4NEOxNVI>

... Click to View More Cell Line Experimental Data

In vivo FK-506 results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. FK-506 also leads to a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, rise in tissue reduced glutathione levels in rats. FK-506 ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R). [5]

Protocol

Solubility (25°C)

In vitro DMSO 94 mg/mL (116.91 mM)
Ethanol 83 mg/mL (103.23 mM)
Water Insoluble
In vivo Add solvents individually and in order:
5% DMSO+corn oil
15mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 804.02
Formula

C44H69NO12

CAS No. 104987-11-3
Storage powder
Synonyms FR900506

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01303965 Active, not recruiting Multiple Myeloma Sherif S. Farag|Celgene Corporation|Indiana University February 7, 2011 Phase 1|Phase 2
NCT00514982 Withdrawn Hermanski-Pudlak Syndrome|Colitis|Cytokines|Lymphocytes|Drug Evaluation National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) August 7, 2007 Phase 2
NCT02891603 Not yet recruiting Graft Vs Host Disease|GVHD H. Lee Moffitt Cancer Center and Research Institute April 30, 2017 Phase 1|Phase 2
NCT02782546 Recruiting Acute Myeloid Leukemia Washington University School of Medicine January 30, 2017 Phase 2
NCT01338987 Active, not recruiting Myelodysplastic Syndrome RAEB 2|Acute Lymphocytic Leukemia|Acute Myelogenous Leukemia|Myelodysplastic Syndrome RAEB 1 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 30, 2011 Phase 2
NCT01875237 Active, not recruiting Leukemia|Myeloma|Myeloproliferative Diseases M.D. Anderson Cancer Center|Bellicum Pharmaceuticals December 27, 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    we would like to inject it subcutaneously into rats, Can we mix the FK506 with 5% dextrose to a concentration of 5mg/ml to prepare the solution?

  • Answer:

    You can dissolve FK506 with DMSO to prepare the stock solution, and then dilute by 5% dextrose. However, we don't have the information about the solubility in this condiation. Or you can use the vehicle we tested: 30% PEG400/0.5% Tween80/5% propylene glycol (Solubility: 30mg/ml).

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID