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
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 9 Publications

7 Customer Reviews

  • 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.

  • 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.

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

Purity & Quality Control

Choose Selective mTOR Inhibitors

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 M4jt[WZ2dmO2aX;uJIF{e2G7 NWTuT2E1OTZiaB?= NVfCVFFIUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGgdJJw\HWldHnvckBqdiC{YYSgVmJNOkh|IHPlcIx{KGGodHXyJFE3KGi{czDifUBGVEmVQTygTWM2OD1yLkK1JI5O MWCyN|c6OTB5Nh?=
rat RBL2H3 cells NYTrWYxRTnWwY4Tpc44h[XO|YYm= NEjhTFQyPSCvaX7z Mn7yRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBz[XRiUlLMNmg{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSG5RNUKVQT3pcoR2[2WmIGTOSk1idHCqYTDwdo9lfWO2aX;uJJBz\WmwY4XiZZRm\CCob4KgNVUhdWmwczDwdolweiCGTmCtRnNCKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIJ6KEWOSWPBMEBKSzVyPUCuNlUhdk1? M13STlIzPDFyMEi0
human T-cell NFnvfYFRem:uaX\ldoF1cW:wIHHzd4F6 NW\mNmZHUW5idnn0do8hcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJHQu[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVAvPSCwTR?= M{P0clc2Ozd|M{G=
human WiDr cells MnzJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MljjTY5pcWKrdHnvckBw\iCVQWCxN|AhdWWmaXH0[YQh[2WubDDndo94fGhiaX6gbJVu[W5iV3nEdkBk\WyuczygTWM2OD1zMD65JI5O NX;lZYJZOTd4NEOxNVI>
human U251 cells MnXVSpVv[3Srb36gZZN{[Xl? M2rEZmlvcGmkaYTpc44hd2ZiU1HQNVMxKGmwIG\FS2Yue3SrbYXsZZRm\CCqdX3hckBWOjVzIHPlcIx{KGK7IGDMRXAhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0yOy56IH7N MVexO|Y1OzFzMh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin; 

PubMed: 26455952     


Representative immunoblots and quantitative analysis of synaptosomes from cultured mutant hippocampal neurons in the presence and absence of FK506 treatment showing a selective increase in total GluA1 and GluA1 S845 phosphorylation [pGluA1(S845)] (n=10 experiments, *p<0.05 and ***p<0.001, unpaired two-tailed student's t-test). 

p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3; 

PubMed: 23470533     


Effect of FK506 on protein expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3. Cells were incubated either in the absence of (control) or in the presence of FK506 (12.5, 25 and 50 μM) for 8 h, and protein expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3 were determined using western blotting. Increasing expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3 were observed in fibroblasts after FK506 treatment at increasing concentrations, and peaked at the concentration of 50 μM.

p-S6K(S371) / S6K / p-Erα(S167) / Erα; 

PubMed: 29344249     


MCF-7 cells were incubated with PS, OA (100 nM), Cal A (1 nM), FK506 (10 nM), or DMSO (0.1%, vehicle) in E2 (10 nM) medium. Phosphorylation was determined by western blotting. 

26455952 23470533 29344249
Immunofluorescence
FKBP52 / p23 / hsp90; 

PubMed: 20796173     


Subcellular localization of FKBP52, hsp90 and p23 in N2a cells. (a) Images by confocal microscopy of undifferentiated cells prior (0 h) or after (3 h and 24 h) of treatment with FK506. Image on the right hand shows a wider field.

FKBP51; 

PubMed: 20796173     


FKBP51 concentrates in transcriptionally active nuclear domains. Cells were treated with FK506 for 6 h and pre-mRNAs were labeled with Br-UTP. Bars= 10 μm

Tom20 / JC-1 / ROS / NF-κB; 

PubMed: 30294901     


TH2849 protects mitochondrial from damage induced by MPP+. Representative confocal image of MDA‐MB‐231 cells incubated with treated with 1‰ DMSO, 10 μmol/L MPP+ alone, or co‐treated with 1 μmol/L rapamycin, 10 μmol/L FK506, 1 μmol/L TH 2451, and 1 μmol/L TH 2849 for 24 h, and then, the immunofluorescence experiment was performed with the primary antibody against (A) Tom20 and (D) NF‐Κb, or the fluorogenic probe DCFH‑DA was used to detect the ROS levels (C). B, EGFP‐LC3 transfected PC12 cells were treated with 10 μmol/L MPP+ alone or co‐treated with 1‰ DMSO, 1 μmol/L rapamycin, 10 μmol/L FK506, 1 μmol/L TH 2451, and 1 μmol/L TH 2849 for 24 h. Mitochondrial transmembrane potential (ΔΨm) was detected by JC‐1. All the substances were dissolved in DMSO. Scale bars: 10 μm. n = 3

20796173 30294901
Growth inhibition assay
Cell viability; 

PubMed: 23470533     


Effect of FK506 on fibroblast proliferation in vitro. Rat skin fibroblasts were treated with increasing concentrations of FK506 for 8 h. The viable cells were measured by CCK-8 assay. FK506 inhibited fibroblast proliferation in a dose-dependent manner. Cell viability reached a relatively minimal level at 75 μM. *P<0.05, **P<0.01 compared with control. All experiments were preformed three times with comparable results

23470533
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 to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing. 		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
in solvent
Synonyms FR900506

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03066466 Recruiting Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Myelodysplastic Syndrome Loyola University December 10 2019 Phase 3
NCT03066466 Recruiting Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Myelodysplastic Syndrome Loyola University December 10 2019 Phase 3
NCT03781414 Not yet recruiting Liver Transplant Rejection Novartis Pharmaceuticals|Novartis June 25 2019 Phase 2
NCT03781414 Not yet recruiting Liver Transplant Rejection Novartis Pharmaceuticals|Novartis June 25 2019 Phase 2
NCT03249831 Recruiting Sickle Cell Disease|Sickle Cell Disorder|Hemoglobinopathies|Thalassemia|Anemia Sickle Cell City of Hope Medical Center|California Institute for Regenerative Medicine (CIRM) June 2019 Phase 1
NCT03856216 Not yet recruiting Acute Lymphoblastic Leukemia|Allogeneic Hematopoietic Stem Cell Transplantation Recipient|B Acute Lymphoblastic Leukemia|CD22 Positive|Lymphocytic Neoplasm|Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) June 30 2019 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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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).

selleck catalog

mTOR Signaling Pathway Map

Related mTOR Products0

  • MHY1485 New

    MHY1485 is a potent, and cell-permeable mTOR activator, and also potently inhibits autophagy.

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

  • Dorsomorphin (Compound C) New

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus) is a specific mTOR inhibitor with IC50 of ~0.1 nM HEK293 cells.

  • Everolimus (RAD001)

    Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay.

  • AZD8055

    AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM in MDA-MB-468 cells with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1.

    Features:First drug to inhibit both types of mTOR protein.

  • Torin 1

    Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM in cell-free assays; exhibits 1000-fold selectivity for mTOR than PI3K.

  • Temsirolimus (CCI-779, NSC 683864)

    Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay.

  • Sapanisertib (INK 128, MLN0128,TAK-228)

    Sapanisertib (INK 128, MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

  • KU-0063794

    KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM in cell-free assays; no effect on PI3Ks.

Tags: buy Tacrolimus (FK506) | Tacrolimus (FK506) supplier | purchase Tacrolimus (FK506) | Tacrolimus (FK506) cost | Tacrolimus (FK506) manufacturer | order Tacrolimus (FK506) | Tacrolimus (FK506) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID