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Purity: = 98.57%
740 Y-P is a cell-permeable peptide acting as a phosphopeptide activator of PI3K. PI3K/AKT signaling pathway benefits from the presence of 740 Y-P. 20 M 740 Y-P for 24 hours treatment significantly decreased the number of M6PR-positive vacuoles brought on by sucrose when tested with human melanoma MNT-1 cells by activating PI3K. By binding to p85 and affecting the PI 3-kinase-dependent phosphorylation of the Akt process, 740 Y-P treatments in cerebellar granule cells under serum deprivation decreased the rate of cell death.
| Targets |
PI3K
|
|---|---|
| ln Vitro |
The PDGFR 740Y-P peptide stimulates a mitogenic response in muscle cells. The ability of the 740Y-P peptide to stimulate mitogenesis is highly specific and not a general feature of a cell permeable SH2 domain binding peptides[2].
Through the well-known PI 3-kinase-Akt survival cascade, 740Y-P is just as effective as a growth factor (FGF2) at promoting neuronal cell survival. The PDGFR740Y-P peptide does not require insulin and can stimulate neuronal cell survival[1]. |
| ln Vivo |
740 Y-P increases the extent of AKT and PI3K phosphorylation in the Alzheimer's disease rat model and decreases the degree of ROS levels in the hippocampal tissues treated with A(25-32).
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| Enzyme Assay |
The binding of small phosphopeptides to the SH2 domains of the p85 regulatory subunit of PI 3-kinase can activate the enzyme in vitro. In the present study a cell-permeable peptide that binds specifically to the SH2 domains of p85 has been evaluated for its ability to stimulate a mitogenic response in the C2 muscle cell line. This peptide, in contrast to four other SH2-binding peptides, was as effective as serum, EGF, and FGF at stimulating entry into S-phase. The response to the p85 binding peptide, but not FGF, was inhibited by wortmannin and rapamycin, indicating that the peptide activates the PI 3-kinase/S6 kinase signalling pathway. The peptide response was not inhibited by the MEK inhibitor (PD098059) and did not stimulate Erk phosphorylation. Thus, there would appear to be no direct cross-talk between the pathway activated by the p85 binding peptide and the p42/p44 MAPK cascade [2].
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| Cell Assay |
740 Y-P increases the extent of AKT and PI3K phosphorylation in the Alzheimer's disease rat model and decreases the degree of ROS levels in the hippocampal tissues treated with A(25-32).NIH HBSS with 10% FCS, Ca2+ and Mn2+ free, and either 50 g/ml of the 740Y-P peptide or an equal volume of PBS as a control are incubated with 2 106 3T3 cells in suspension at 37°C. Cells are centrifuged, cleaned, and trypsinized after 2 hours to break down non-internalized peptide. Then, the cells are resuspended in lysis buffer (50 mM Tris pH 7.4, 150 mM NaCl, 10% Glycerol, 2% NP40, 0.25% deoxycholate, 1 mM EDTA, 1 mM Vanadate, Protease Inhibitors Complete" Cocktail from Boehringer-Mannheim) and incubated at 4°C for 1 hour. Lysates are clarified by centrifuging at 1.4×104g for 5 min, and the supernatants are then incubated with streptavidin-agarose beads for 1h. After that, beads are washed three times in lysis buffer, boiled in SDS sample buffer, resolved by SDS-PAGE on a 12% gel, transferred to nitrocellulose, and immunoblotted with the p85 monoclonal antibody.
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| Animal Protocol |
To evaluate this hypothesis, a rat AD model was established by intraperitoneal injection of the GABAB receptor agonist (baclofen), PI3K/Akt signaling pathway agonist (740 Y-P), and antagonist (LY294002), respectively. The effects of GABAB activation on spatial memory and learning ability in the AD rats were measured by Morris water maze. Whereas the effects of GABAB and PI3K/Akt signaling pathway on apoptosis and oxidative stress injury were determined in vivo and in vitro using primary neuronal cultures [3].
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| References |
[3]. J Alzheimers Dis. 2020;76(4):1513-1526. doi: 10.3233/JAD-191032.
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| Molecular Formula |
C141H222N43O39PS3
|
|---|---|
| Molecular Weight |
3270.7049
|
| Exact Mass |
3268.561035
|
| CAS # |
1236188-16-1
|
| Related CAS # |
740 Y-P TFA
|
| Sequence |
Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Ser-Asp-Gly-Gly-{PO2-Tyr}-Met-Asp-Met-SerSequence
|
| SequenceShortening |
R-Q-I-K-I-W-F-Q-N-R-R-M-K-W-K-K-S-D-G-G-{PO2-Y}-M-D-M-S
|
| Appearance |
White to off-white solid
|
| LogP |
-18.3
|
| tPSA |
1470Ų
|
| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC4=CNC5=CC=CC=C54)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)NCC(=O)N[C@@H](CC6=CC=C(C=C6)OP(=O)(O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CO)C(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCNC(=N)N)N
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| InChi Key |
XCGMILZGRGEWHL-QYGSNONCSA-N
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| InChi Code |
InChI=1S/C141H222N43O39PS3/c1-8-75(3)114(184-128(208)94(46-48-108(148)188)164-116(196)84(146)32-25-56-156-139(150)151)136(216)174-90(38-20-24-55-145)127(207)183-115(76(4)9-2)137(217)180-101(65-80-70-160-86-34-16-14-31-83(80)86)132(212)175-99(62-77-28-11-10-12-29-77)130(210)170-93(45-47-107(147)187)123(203)177-102(66-109(149)189)133(213)169-92(40-27-58-158-141(154)155)119(199)167-91(39-26-57-157-140(152)153)120(200)171-95(49-59-225-5)124(204)166-88(36-18-22-53-143)121(201)176-100(64-79-69-159-85-33-15-13-30-82(79)85)131(211)168-87(35-17-21-52-142)118(198)165-89(37-19-23-54-144)122(202)181-105(73-185)135(215)178-103(67-112(192)193)117(197)162-71-110(190)161-72-111(191)163-98(63-78-41-43-81(44-42-78)223-224(220,221)222)129(209)172-96(50-60-226-6)125(205)179-104(68-113(194)195)134(214)173-97(51-61-227-7)126(206)182-106(74-186)138(218)219/h10-16,28-31,33-34,41-44,69-70,75-76,84,87-106,114-115,159-160,185-186H,8-9,17-27,32,35-40,45-68,71-74,142-146H2,1-7H3,(H2,147,187)(H2,148,188)(H2,149,189)(H,161,190)(H,162,197)(H,163,191)(H,164,196)(H,165,198)(H,166,204)(H,167,199)(H,168,211)(H,169,213)(H,170,210)(H,171,200)(H,172,209)(H,173,214)(H,174,216)(H,175,212)(H,176,201)(H,177,203)(H,178,215)(H,179,205)(H,180,217)(H,181,202)(H,182,206)(H,183,207)(H,184,208)(H,192,193)(H,194,195)(H,218,219)(H4,150,151,156)(H4,152,153,157)(H4,154,155,158)(H2,220,221,222)/t75-,76-,84-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,114-,115-/m0/s1
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| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]hexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]acetyl]amino]acetyl]amino]-3-(4-phosphonooxyphenyl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-[[(2S)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid
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| Synonyms |
740 Y-P; 740 YP; 740YPDGFR; PDGFR740Y-P;740 Y P; 740-YPDGFR; PDGFR 740 Y-P; 740 YPDGFR; PDGFR 740Y-P
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO: 25~100 mg/mL (7.6~30.6 mM)
Ethanol: 8 mg/mL (~2.5 mM) H2O: 5 mg/mL (1.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (0.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (0.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (0.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3057 mL | 1.5287 mL | 3.0574 mL | |
| 5 mM | 0.0611 mL | 0.3057 mL | 0.6115 mL | |
| 10 mM | 0.0306 mL | 0.1529 mL | 0.3057 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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