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Products > Biosensors > PLCglow™

PLCglow™

$350 – $1,100

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SKU: N/A Category: Biosensors
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Product information

PLCglow™is a small molecule that directly reports the enzymatic activity of phospholipase C (PLC) isozymes1,2. PLCglow™ is hydrolyzed by PLCs to generate inositol trisphosphate (IP3), quinomethide, and 6-aminoquinoline. Relative to PLCglow™, the aminoquinoline is highly fluorescent (λex/em = 344/530 nm) (Fig. 1).

  1. Huang et al., A fluorogenic, small molecule reporter for mammalian phospholipase C isozymes. ACS Chemical Biology 6(3), 223-8 (2011).
  2. Huang et al., Small molecule inhibitors of phospholipase C from a novel high-throughput screen. JBC 288(8), 5840-8 (2013).

Properties:

Molecular weight: 1127 g/mol as triethylamine salt (824 g/mol for compound alone).
Amount: 50 μg or 200 μg
Form: Powder.

Storage and stability:

Storage temperature: -80 °C.
Stability: Stable for up to 12 months at -80 °C and up to 14 days at 4 °C in water. PLCglow™ is not stable for long periods in several common buffers and stock solutions should be stored only in water. Repeated freezing and thawing is not recommended.
Notes: Results will vary depending on the sensitivity of the fluorometer and the specific activity of the PLC isozyme. In order to obtain optimal results, we recommend testing a dilution series of WH-15 and PLC isozyme. WH-15 is designed to work with purified proteins and cellular lysates. In contrast, WH-15 will not enter intact cells and is therefore inappropriate for measuring intracellular PLCs.

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Additional information

Weight

10 µg $100, 50 µg $350, 200 µg $1,100

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Product literature

PLCglow™ Information sheet

PLCglow™ Quality control information

Related publications

Huang et al., A fluorogenic, small molecule reporter for mammalian phospholipase C isozymes. ACS Chemical Biology 6(3), 223–8 (2011).
+ Read abstract
Phospholipase C isozymes (PLCs) catalyze the conversion of the membrane lipid phosphatidylinositol 4,5-bisphosphate (PIP2) into two second messengers, inositol 1,4,5-trisphosphate and diacylglycerol. This family of enzymes are key signaling proteins that regulate the physiological responses of many extracellular stimuli such as hormones, neurotransmitters, and growth factors. Aberrant regulation of PLCs has been implicated in various diseases including cancer and Alzheimer’s disease. How, when, and where PLCs are activated under different cellular contexts are still largely unknown. We have developed a fluorogenic PLC reporter, WH-15, that can be cleaved in a cascade reaction to generate fluorescent 6-aminoquinoline. When applied in enzymatic assays with either pure PLCs or cell lysates, this reporter displays more than a 20-fold fluorescence enhancement in response to PLC activity. Under assay conditions, WH-15 has comparable Km and Vmax with the endogenous PIP2. This novel reporter will likely find broad applications that vary from imaging PLC activity in live cells to high throughput screening of PLC inhibitors. Read the full article here

Huang et al., Small molecule inhibitors of phospholipase C from a novel high-throughput screen. JBC 288(8), 5840-8 (2013).
+ Read abstract
Phospholipase C (PLC) isozymes are important signaling molecules, but few small molecule modulators are available to pharmacologically regulate their function. With the goal of developing a general approach for identification of novel PLC inhibitors, we developed a high-throughput assay based on the fluorogenic substrate reporter WH-15. The assay is highly sensitive and reproducible: screening a chemical library of 6280 compounds identified three novel PLC inhibitors that exhibited potent activities in two separate assay formats with purified PLC isozymes in vitro. Two of the three inhibitors also inhibited G protein-coupled receptor-stimulated PLC activity in intact cell systems. These results demonstrate the power of the high-throughput assay for screening large collections of small molecules to identify novel PLC modulators. Potent and selective modulators of PLCs will ultimately be useful for dissecting the roles of PLCs in cellular processes, as well as provide lead compounds for the development of drugs to treat diseases arising from aberrant phospholipase activity. Read the full article here

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