740 Y-P

740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.

Product information

CAS Number: 1236188-16-1

Molecular Weight: 3270.70

Formula: C141H222N43O39PS3

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)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S,3S)-2-[(2S)-6-amino-2-[(2S,3S)-2-[(2S)-2-[(2S)-2-amino-5-carbamimidamidopentanamido]-4-carbamoylbutanamido]-3-methylpentanamido]hexanamido]-3-methylpentanamido]-3-(1H-indol-3-yl)propanamido]-3-phenylpropanamido]-4-carbamoylbutanamido]-3-carbamoylpropanamido]-5-carbamimidamidopentanamido]-5-carbamimidamidopentanamido]-4-(methylsulfanyl)butanamido]hexanamido]-3-(1H-indol-3-yl)propanamido]hexanamido]hexanamido]-3-hydroxypropanamido]-3-carboxypropanamido]acetamido}acetamido)-3-[4-(phosphonooxy)phenyl]propanamido]-4-(methylsulfanyl)butanamido]-3-{[(1S)-1-{[(1S)-1-carboxy-2-hydroxyethyl]carbamoyl}-3-(methylsulfanyl)propyl]carbamoyl}propanoic acid

Smiles: C[C@@H](CC)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CCCNC(N)=N)[C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=CC=CC=C12)C(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)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](CC1=CNC2=CC=CC=C12)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](CC1C=CC(=CC=1)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

InChiKey: XCGMILZGRGEWHL-QYGSNONCSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 25 mg/mL (7.64 mM; Need ultrasonic). H2O : 2 mg/mL (0.61 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

740 Y-P (50 μg/mL; 48 hours) specificly stimulates mitogenesis in medium is better than EGF or FGF at stimulating entry into S-phase, it shows the percentage of cells in S-phase for 48.3% in C2 cells. Additionally, LY294002 (HY-10108) or Wortmannin (HY-10197) potently inhibits the mitogenic response stimulated by the peptide. 740 Y-P (1 μg/mL) stimulates mitogenesis at the lowest concentration tested. The peptide stimulates mitogenesis in both the presence and absence of serum (0.5%), and in the former instance a maximal response observed at 50 μg/mL. 740Y-P to stimulate mitogenesis is highly specific and not a general feature of a cell permeable SH2 domain binding peptides. 740 Y-P (30 μM; 24 hours) remarkably inhibits the level of LC3-II/LC3-I in GO-induced PC12 cells.

In Vivo:

740 Y-P is not only internalised in living cells but can also interact with p85 in vivo. 740 Y-P (intraperitoneal injection; 10 mg/kg; 6 weeks) decreases the degree of ROS levels in Aβ(25-32) treated hippocampal tissues and increases the extent of AKT and PI3K phosphorylation in alzheimer’s disease (AD) rat model.

Products are for research use only. Not for human use.