WS3 --- β Cell Proliferation Inducer

WS3 is a highly potent and selective small molecule that promotes pancreatic β cell and RPE cells expansion, identified by a high-throughput, cell-based screening. It can induce proliferation of mouse R7T1 β cells with an EC50 ~0.074 µM, and expansion of primary rat and human β cells in dissociated and intact islet format with similar EC50. WS3 can also reversibly proliferate primary RPE cells isolated from fetal and adult human donors. Following withdrawal of WS3, RPE cells differentiate into a functional monolayer, as exhibited by their expression of mature RPE genes and phagocytosis of photoreceptor outer segments. Furthermore, chemically expanded RPE cells preserve vision when transplanted into dystrophic Royal College of Surgeons (RCS) rats, a well-established model of retinal degeneration.

Product information

CAS Number: 1421227-52-2

Molecular Weight: 569.58

Formula: C28H30F3N7O3

Chemical Name: N-(6-(4-(3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide

Smiles: CN1CCN(CC2=CC=C(C=C2C(F)(F)F)NC(=O)NC2C=CC(=CC=2)OC2=CC(NC(=O)C3CC3)=NC=N2)CC1

InChiKey: KIKOYRNAERIVSJ-UHFFFAOYSA-N

InChi: InChI=1S/C28H30F3N7O3/c1-37-10-12-38(13-11-37)16-19-4-5-21(14-23(19)28(29,30)31)35-27(40)34-20-6-8-22(9-7-20)41-25-15-24(32-17-33-25)36-26(39)18-2-3-18/h4-9,14-15,17-18H,2-3,10-13,16H2,1H3,(H2,34,35,40)(H,32,33,36,39)

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 100 mM

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:

WS3 was used at 0.05-0.2 µM concentration in beta cell proliferation assays in vitro. WS3 was used at 25 nM concentration in RPE cells expansion assays.

References:

1. Shen W, et al. Small-Molecule Inducer of β Cell Proliferation Identified by High-Throughput Screening. (2013) J Am Chem Soc. 135(5):1669-72.
2. Swoboda JG, et al. Small Molecule Mediated Proliferation of Primary Retinal Pigment Epithelial Cells. (2013) ACS Chem Biol. In press.

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

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