Replaces Prod. #: BML-A235
Immunosuppressant that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK506 binding protein and to inhibit the Ca2+-dependent phosphatase and protein phosphatase 2B (PP2B; calcineurin). Activates NF-κB through phosphorylation and degradation of IκBα.
Product Details
| Alternative Name: | Tacrolimus |
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| Formula: | C44H69NO12 |
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| MW: | 804.0 |
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| Source: | Isolated from Streptomyces tsukubaensi. |
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| CAS: | 104987-11-3 |
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| MI: | 14: 9025 |
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| RTECS: | KD4200000 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | FT-IR |
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| Appearance: | White to off-white crystalline powder. |
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| Solubility: | Soluble in DMSO, 100% ethanol, methanol, ethyl acetate or acetone; insoluble in water. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Dynamic changes in β-cell [Ca 2+] regulate NFAT activation, gene transcription, and islet gap junction communication: J.G. Miranda, et al.; Mol. Metab.
57, 101430 (2022),
Abstract;
Fluorescence imaging detection of nanodomain redox signaling events at organellar contacts: D.M. Booth, et al.; STAR Protoc.
3, 101119 (2022),
Abstract;
Full Text
Novel use of FDA-approved drugs identified by cluster analysis of behavioral profiles: S.T. Edmister, et al.; Sci. Rep.
12, 6120 (2022),
Abstract;
Oxidative bursts of single mitochondria mediate retrograde signaling toward the ER: D.M. Booth, et al.; Mol. Cell
81, 3866 (2021),
Abstract;
Full Text
Safety and efficacy of tacrolimus-coated silicone plates as an alternative to mitomycin C in a rabbit model of conjunctival fibrosis: S.Y. Yoon, et al.; PLoS One
14, e0219194 (2019),
Abstract;
Full Text
Calcineurin A beta deficiency ameliorates HFD-induced hypothalamic astrocytosis in mice: K. Pfuhlmann, et al.; J. Neuroinflammation
15, 35 (2018),
Abstract;
Full Text
Perturbed Calcineurin-NFAT Signaling Is Associated with the Development of Alzheimer’s Disease: M. Asai, et al.; Biol. Pharm. Bull.
39, 1646 (2016),
Application(s):,
Abstract;
Full Text
Tacrolimus Modulates TGF-β Signaling to Induce Epithelial-Mesenchymal Transition in Human Renal Proximal Tubule Epithelial Cells: J. Bennett, et al.; J. Clin. Med.
5, 50 (2016),
Application(s): Cell treatment,
Abstract;
The Sur1-Trpm4 channel regulates NOS2 transcription in TLR4-activated microglia: D.B. Kurland, et al. ; J. Neuroinflammation
13, 130 (2016),
Application(s): Cell culture,
Abstract;
Full Text
Distinct biological activity of threonine monophosphorylated MAPK isoforms during the stress response in fission yeast: B. Vazquez, et al.; Cell. Signal.
27, 2534 (2015),
Application(s): Cell Culture,
Abstract;
Effects of embryonic cyclosporine exposures on brain development and behavior: D.E. Clift, et al.; Behav. Brain Res.
282, 117 (2015),
Application(s): Cell Culture,
Abstract;
Feedback Mechanisms Regulate Ets variant 2 (Etv2) Gene Expression and Hematoendothelial Lineages: N. Koyano-Nakagawa, et al.; J. Biol. Chem.
290, 28107 (2015),
Application(s): Calcineurin inhibition,
Abstract;
Full Text
A review of the action of tacrolimus (FK506) on experimental models of rheumatoid arthritis: S. Miyata, et al.; Inflamm. Res.
54, 1 (2005), Review,
Abstract;
FK506 and its analogs - therapeutic potential for neurological disorders: A. Klettner and T. Herdegen; Curr. Drug Targets CNS Neurol. Disord.
2, 153 (2003), Review,
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FK506, an immunosuppressant targeting calcineurin function: F.J. Dumont; Curr. Med. Chem.
7, 731 (2000),
Abstract;
Immunosuppressant FK506 activates NF-kappaB through the proteasome-mediated degradation of IkappaBalpha. Requirement for Ikappabalpha n-terminal phosphorylation but not ubiquitination sites: Y. Zhang, et al.; J. Biol. Chem.
274, 34657 (1999),
Abstract;
Full Text
Cyclosporin A and FK506: molecular mechanisms of immunosuppression and probes for transplantation biology: B.E. Bierer, et al.; Curr. Opin. Immunol.
5, 763 (1993),
Abstract;
Cyclosporin A, FK506 and rapamycin: more than just immunosuppression: J. Kunz and M.N. Hall; TIBS
18, 334 (1993),
Abstract;
FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics: T. Kino, et al.; J. Antibiot. (Tokyo)
40, 1249 (1987),
Abstract;
