A potent immunosuppressant; binds to FK-506 binding protein 12 (Ki = 0.2 nM) to inhibit calcineurin; regulates NO neurotoxicity

FK-506 – 5 mg

Brand:
Cayman
CAS:
104987-11-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

FK-506 is a potent immunosuppressant in the same molecular class as cyclosporin A (Item No. 12088) and rapamycin (Item No. 13346).{5285} Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 binding protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T cell activation.{13842} The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.{7042} In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors leaky to Ca2+.  

 

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SKU: 10007965 - 5 mg Category:

Description

A potent immunosuppressant; binds to FK-506 binding protein 12 (Ki = 0.2 nM) to inhibit calcineurin; regulates NO neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and IP3 receptors,

Formal 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

Synonyms:  Tacrolimus

Molecular weight: 804

CAS: 104987-11-3

Purity: ≥99%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphatases||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Immunosuppressants||Research Area|Neuroscience

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