REVERSIN 121 Chemical Properties

Melting point:

200°C

Boiling point:

786.8±60.0 °C(Predicted)

Density 

1.163±0.06 g/cm3(Predicted)

storage temp. 

−20°C

solubility 

DMSO or ethanol: soluble

form 

powder

pka

10.75±0.46(Predicted)

color 

white

Safety Information

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

REVERSIN 121 Usage And Synthesis

Description

Reversin 121 is a hydrophobic peptide chemosensitizer that can reverse P-glycoprotein-mediated multidrug resistance. It binds to the P-glycoprotein multidrug transporter (MDR1) with a K_d value of 77 nM. Reversin 121 modulates P-glycoprotein ATPase activity in Sf9 insect cell membranes expressing human MDR1, plasma membrane vesicles from multidrug-resistant cells, and reconstituted proteoliposomes as well as in a variety of MDR1-expressing intact tumor cells.

Uses

Reversin 121 has been used to determine the activity of P-glycoprotein in human retinal pigment epithelium.

General Description

Reversin 121 is an analog of reversin and a dipeptide derivative.

Biochem/physiol Actions

Peptide chemosensitizer, inhibitor of P-glycoprotein.

in vivo

References

[1] FRANCES J SHAROM . Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells[J]. Biochemical pharmacology, 1999, 58 4: Pages 571-586. DOI: 10.1016/s0006-2952(99)00139-2
[2] EUNICE L KWAK. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2005, 102 21: 7665-7670. DOI: 10.1073/pnas.0502860102
[3] PRIYANKA S. RANA . Calibration and characterization of intracellular Asante Potassium Green probes, APG-2 and APG-4[J]. Analytical biochemistry, 2019, 567: Pages 8-13. DOI: 10.1016/j.ab.2018.11.024