| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: ~10 μM (calcineurin)[1]
Calcineurin (Ca2+/calmodulin-dependent protein phosphatase, also known as protein phosphatase 2B, PP2B). Calcineurin autoinhibitory peptide is a selective inhibitor with an IC50 of approximately 10 microM. It does not inhibit PP1 (protein phosphatase 1). |
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| ln Vitro |
Calcineurin autoinhibitory peptide is a selective inhibitor of calcineurin, blocking its phosphatase activity with an IC50 of approximately 10 microM. It mimics the endogenous autoinhibitory domain of calcineurin, binding to the enzyme and preventing substrate dephosphorylation. This peptide does not inhibit PP1, demonstrating selectivity. It protects neurons from excitatory neuronal death in vitro.
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| ln Vivo |
In vivo, calcineurin autoinhibitory peptide has been shown to protect neurons from excitatory neuronal death in animal models of stroke, traumatic brain injury, and neurodegenerative diseases. By inhibiting calcineurin, it blocks the dephosphorylation and activation of pro-apoptotic factors (e.g., Bad, NFAT), thereby promoting neuronal survival. It can also function as an immunosuppressant by inhibiting T-cell activation.
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| Enzyme Assay |
For non-cellular assays, purified calcineurin (PP2B) is incubated with a fluorogenic substrate such as RII phosphopeptide or p-nitrophenyl phosphate (pNPP) in assay buffer containing Ca2+ and calmodulin. Calcineurin autoinhibitory peptide is added at varying concentrations (1-100 uM). Phosphate release is measured by colorimetric (malachite green) or fluorescence methods, and IC50 values are calculated from dose-response curves.
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| Cell Assay |
For cell-based assays, primary neurons or T-cells are treated with calcineurin autoinhibitory peptide. Because the peptide is cell-permeable, it can be added directly to culture media (10-50 uM). In neurons, excitotoxicity is induced by glutamate or NMDA treatment. Cell viability is assessed by MTT or LDH release. NFAT nuclear translocation is measured by immunofluorescence or Western blot. T-cell activation is assessed by IL-2 production (ELISA).
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| Animal Protocol |
For animal studies, calcineurin autoinhibitory peptide is administered via intracerebroventricular (ICV) injection (typically 1-10 ug/mouse) or intraperitoneally in models of stroke, traumatic brain injury, or neurodegeneration. Neuroprotection is assessed by measuring infarct volume (TTC staining) or neuronal survival (Nissl staining). Behavioral outcomes (e.g., rotarod, Morris water maze) are evaluated. Tissues are collected for analysis of calcineurin activity and apoptosis markers.
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| ADME/Pharmacokinetics |
Calcineurin autoinhibitory peptide is a synthetic peptide that is stable in lyophilized form at -20degC for long-term storage. For in vivo use, it is dissolved in saline or artificial cerebrospinal fluid (aCSF). The peptide has a molecular weight of 2930.34 and a molecular formula of C124H205N39O39S2. It is cell-permeable, allowing direct addition to cell culture media.
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| Toxicity/Toxicokinetics |
Calcineurin autoinhibitory peptide is generally well tolerated at research doses. In animal studies, no significant systemic toxicity has been reported at the doses used for neuroprotection (1-10 ug ICV). High doses may cause immunosuppression or off-target effects. Standard safety precautions for handling synthetic peptides should be followed. It is intended for research use only.
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| References | |
| Additional Infomation |
The amino acid sequence is described in the first reference; 25 amino acid residues; amino acid residues 476-501 of the calcineurin Aβ subunit; a non-competitive inhibitor of calcineurin in vitro.
Calcineurin autoinhibitory peptide (CAS: 148067-21-4) has a molecular weight of 2930.34 and a sequence based on the autoinhibitory domain of calcineurin. It is a selective inhibitor of calcineurin (PP2B) and does not inhibit PP1. It is a valuable tool for studying calcineurin signaling in T-cell activation, neuronal survival, cardiac hypertrophy, and synaptic plasticity. It is not approved for clinical use. |
| Molecular Formula |
C124H205N39O39S2
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|---|---|
| Molecular Weight |
2930.32
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| Exact Mass |
2928.47
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| CAS # |
148067-21-4
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| Related CAS # |
Calcineurin autoinhibitory peptide TFA
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| PubChem CID |
16131045
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| Appearance |
White to off-white solid powder
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| LogP |
1.972
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| Hydrogen Bond Donor Count |
42
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| Hydrogen Bond Acceptor Count |
49
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| Rotatable Bond Count |
103
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| Heavy Atom Count |
204
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| Complexity |
6690
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| Defined Atom Stereocenter Count |
27
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)OC(=O)CC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)OC(=O)CC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCSC)C(=O)N2CCC[C@H]2C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N4CCC[C@H]4C(=O)O)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)N)NC(=O)[C@H](CCC(=O)O)N)N
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| InChi Key |
QKXOLPYOGCLSCP-TVQDNDAUSA-N
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| InChi Code |
InChI=1S/C124H205N39O39S2/c1-12-62(5)94(129)112(191)160-96(66(9)165)114(193)158-83(60-164)110(189)157-82(55-67-26-15-14-16-27-67)120(200)202-93(175)40-37-75(148-99(178)68(126)36-39-89(168)169)102(181)143-64(7)97(176)146-70(28-17-18-44-125)101(180)142-59-88(167)145-81(54-61(3)4)119(199)201-92(174)41-38-76(151-109(188)79(57-87(128)166)156-113(192)95(63(6)13-2)159-107(186)74(32-22-48-141-124(136)137)147-100(179)69(127)56-90(170)171)106(185)150-71(29-19-45-138-121(130)131)104(183)154-78(43-53-204-11)115(194)162-50-24-34-85(162)117(196)161-49-23-33-84(161)111(190)152-73(31-21-47-140-123(134)135)103(182)149-72(30-20-46-139-122(132)133)105(184)155-80(58-91(172)173)108(187)144-65(8)98(177)153-77(42-52-203-10)116(195)163-51-25-35-86(163)118(197)198/h14-16,26-27,61-66,68-86,94-96,164-165H,12-13,17-25,28-60,125-127,129H2,1-11H3,(H2,128,166)(H,142,180)(H,143,181)(H,144,187)(H,145,167)(H,146,176)(H,147,179)(H,148,178)(H,149,182)(H,150,185)(H,151,188)(H,152,190)(H,153,177)(H,154,183)(H,155,184)(H,156,192)(H,157,189)(H,158,193)(H,159,186)(H,160,191)(H,168,169)(H,170,171)(H,172,173)(H,197,198)(H4,130,131,138)(H4,132,133,139)(H4,134,135,140)(H4,136,137,141)/t62-,63-,64-,65-,66+,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,94-,95-,96-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-5-[(2S)-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]-5-[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]oxy-5-oxopentanoyl]amino]propanoyl]amino]hexanoyl]amino]acetyl]amino]-4-methylpentanoyl]oxy-2-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 100 mg/mL (34.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (34.13 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3413 mL | 1.7063 mL | 3.4126 mL | |
| 5 mM | 0.0683 mL | 0.3413 mL | 0.6825 mL | |
| 10 mM | 0.0341 mL | 0.1706 mL | 0.3413 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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