1. Cyclic Peptides

Cyclo(Arg-Gly-Asp-D-Phe-Lys)
$ 250/5 mg; $ 500/25 mg

An RGD tumor-targeting peptide, which binds to αvβ3 receptors. It can be easily conjugated to fluorophore tags, chelators, or carriers. Palecek et al. converted the ε-amino group into the azide by diazo transfer allowing further functionalization by click chemistry. Mercapto groups can be introduced via acylation of this peptide with S-acetylthio-acetic acid (SATA).

Ac-Nle-cyclo(-Asp-His-D-Phe-Arg-Trp-Lys)
$ 250/5 mg; $ 1016/25 mg

Melanotan II, a cyclic MSH analog, is a potent full agonist of the melanocortin-3 and melanocortin-4 receptors (MC3-R and MC4-R). Intracerebroventricular administration of MTII inhibited feeding in four different mouse models of hyperphagia. MTII is a valuable tool for the study of the agouti obesity syndrome and of the role of melanocortinergic neurons in feeding.

2. Phosphorylation

H-Tyr(PO3H2)-Val-Asn-Val-OH
$ 220/1 mg ; $ 800/5 mg

This peptide corresponds to residues 317 to 320 of the oncogenic protein Shc. Similar phosphotyrosine motifs are also found in receptor tyrosine kinases and substrates of them. This peptide binds with high affinity (18 nM) to the SH2 domain of the growth factor bound-2 protein (Grb2). It is a useful inhibitor of the interaction of Grb2 with Shc, or with other Grb-2-binding proteins involved in the cell signaling cascade.

H-Cys-Leu-Asn-Arg-Gln-Leu-Ser(PO3H2)-Ser-Gly-Val-Ser-Glu-Ile-Arg-OH
$ 305/1 mg ;$ 1220/5 mg

The small mammalian heat shock proteins show a highly conserved amino acid sequence and are suggested to play a major role in the increased thermal resistance acquired by cells after exposure to heat shock. They possess two major sites of phosphorylation which are each located in the conserved protein kinase phosphorylation site motif Arg-X-X-Ser. The above-mentioned phosphopeptide, which contains the second site of phosphorylation, has been isolated from a tryptic digest of phosphorylated native and recombinant mouse hsp 25. Only Ser86, the first of the three serine residues is phosphorylated.

3. Stapled Peptides

Ala-Gln-Trp-Leu-Glu-Leu-Arg-S5-Asp-Phe-Ile-Gly-Asn-Ala-R8-Tyr-Glu-Ile (Stapled between S5 & R8)
$ 600 /1 mg; $ 1800/5 mg

Stapled peptide is a full-carbon scaffold with an α-helical structure. The all-carbon scaffold stabilizes the α-helical structure, enhances the interaction between the peptide molecule and the protein, and the peptide can pass through the cell membrane and is not easily hydrolyzed. Stapled peptides have higher physiological activity than previous small molecule drugs and protein analogs.

4. Peptide-Protein Conjugates

  1. KLH (Keyhole Limpet Hemocyanin)
  2. BSA (Bovine Serum Albumin)
  3. OVA (Ovalbumin)

5. N-Methyl Modification

Thr-Ser-Arg-His-Lys-Lys(Me)-Leu-Met-Phe-Lys-Thr
$ 400 /5 mg;$ 1,800/ 25 mg

TSRHK-K(Me)-LMFKT peptide is derived from amino acid residues 377-387 of human p53 tumor suppressor protein, with monomethylation at Lys382. Methylation of p53 at Lys382 inhibits expression of p53 target genes and decreases apoptotic and cell cycle arrest functions of p53. This allows p53-dependent DNA repair without apoptosis. Levels of this peptide decrease in response to DNA damage.

6. PEG Modified Peptides

Cholesterol-PEG2K-VGWDFRQLYQPN
$ 1,000/1 mg; $ 2,500 /5 mg
H-Pro-PEG4-Cys-Pro-Glu-Asp-Asp-Arg-Thr-Cys-OH (Cys&Cys disulfide)
$ 200/5 mg; $ 800/25 mg

7. Fluorophore-labeled Peptide

7.1 Fluorescein Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
FITC 494 518 N-Terminal, Side Chain of Lys or Cys
FAM 494 522 N-Terminal, Side Chain of Lys or Cys

7.2 Rhodamine Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
Texas Red 595 615 N-Terminal, Side Chain of Lys or Cys
RF488 498 520 N-Terminal, Side Chain of Lys or Cys
TAMRA 565 580 N-Terminal, Side Chain of Lys or Cys
Rhodamine B 555 580 N-Terminal, Side Chain of Lys or Cys

7.3 Cy Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
Cy-3 550 565 N-Terminal, Side Chain of Lys or Cys
Cy-5 646 664 N-Terminal, Side Chain of Lys or Cys
Cy-5.5 673 692 N-Terminal, Side Chain of Lys or Cys
Cy-7 747 774 N-Terminal, Side Chain of Lys or Cys

7.4 QSY Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
QSY-7 560 None N-Terminal, Side Chain of Lys or Cys
QSY-9 562 None N-Terminal, Side Chain of Lys or Cys
QSY-21 661 None N-Terminal, Side Chain of Lys or Cys

7.5 Alexa Fluor Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
Alexa Fluor 350 346 445 N-Terminal, Side Chain of Lys or Cys
Alexa Fluor 405 400 424 N-Terminal, Side Chain of Lys or Cys
Alexa Fluor 430 430 545 N-Terminal, Side Chain of Lys or Cys
Alexa Fluor 488 494 517 N-Terminal, Side Chain of Lys or Cys
Alexa Fluor 514 517 542 N-Terminal, Side Chain of Lys or Cys
Alexa Fluor 532 530 555 N-Terminal, Side Chain of Lys or Cys
Alexa Fluor 594 590 617 N-Terminal, Side Chain of Lys or Cys

7.6 Bodipy Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
Bodipy 493/503 500 506 N-Terminal, Side Chain of Lys or Cys
Bodipy FL 505 513 N-Terminal, Side Chain of Lys or Cys
Bodipy R6G 528 550 N-Terminal, Side Chain of Lys or Cys
Bodipy 530/550 534 554 N-Terminal, Side Chain of Lys or Cys
Bodipy TMR-X 542 574 N-Terminal, Side Chain of Lys or Cys
Bodipy 558/568 558 569 N-Terminal, Side Chain of Lys or Cys
Bodipy 576/589 576 590 N-Terminal, Side Chain of Lys or Cys
Bodipy 581/591 584 592 N-Terminal, Side Chain of Lys or Cys
Bodipy TR 589 617 N-Terminal, Side Chain of Lys or Cys
Bodipy 630/650 625 640 N-Terminal, Side Chain of Lys or Cys

7.7 Other Series

Labeled groups Absorption maximum (nm) Emission maximum (nm) Modification sites
Dansyl 333 518 N-Terminal, Side Chain of Lys or Cys
Dabcyl broad None N-Terminal, Side Chain of Lys or Cys
DNP 350 None N-Terminal, Side Chain of Lys or Cys
MCA 358 69 N-Terminal, Side Chain of Lys or Cys
SBF 385 and 515 None N-Terminal, Side Chain of Lys or Cys
EDANS 335 493 N-Terminal, Side Chain of Lys or Cys
7-OHCCA 342 (pH=4) 447 (pH=4) N-Terminal, Side Chain of Lys or Cys
Dacia 376 465 N-Terminal, Side Chain of Lys or Cys

8. Radio-labeled Peptide

9. Evans Blue Modification

Plasma protein-based drug delivery is a good way to treat cancer; It has two main advantages: 1) Plasma protein-based drug carriers have higher permeability and retention in tumor cells; 2) There are two types of plasma protein binding proteins that are overexpressed in the environment in which tumor cells are born. These two proteins play important roles in the absorption and retention of plasma proteins in various cells.

Evans Blue (EB) is a kind of functional group with strong affinity for plasma proteins, it can be used to label plasma protein content and location in the body, Pharmacochemists can use this to assess permeability to the blood-brain barrier. EB can also be used for in vivo experiments; EB-bound plasma proteins can enter damaged or dead cells, but not healthy cells. Our company can conduct EB functional group modification and molecular imaging functional group modification for peptides active molecules at the same time, which can meet the frontier research of pharmaceutical chemists and pharmacologists.