Choosing & Using Chemical Probes

news November 09 2021

NEW Guide:
Choosing & Using Chemical Probes

Chemical probes are well-characterized small molecules that potently and selectively modulate target protein activity.

Use this guide, which includes the defining criteria for chemical probes, important “do’s and don’ts”, and a step-by-step guide for evaluating compound quality and suitability, to help you choose the best chemical probe for your experiments.

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BYL719

A selective inhibitor of phosphoinositide 3-kinase α (PI3Kα)

BYL719 is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM). It is less effective against PI3K isoforms β, γ, and δ as well as a range of related kinases. BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice.  Learn more.

SGC Probe Set

A library of epigenetic probes from the Structural Genomics Consortium (SGC)

The SGC, in conjunction with academic and industrial partners, has developed numerous small, drug-like molecules that inhibit or antagonize epigenetic readers, writers, and erasers. We provide these probes as part of our expanding epigenetics product portfolio. The SGC Probe Set contains a collection of these compounds each packaged as a 1 mg sample size for ease of preclinical target validation during early stages of drug discovery.  Learn More.

GSK484 (hydrochloride)

A reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme. It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.  Learn More.

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Chemical Synthesis

Cayman Chemicals team of synthetic organic and medicinal chemists brings decades of industry experience to perform complex, multi-step organic syntheses.

Contact our experts today to learn how we can help you!