SMARCA2 TR-FRET Assay Kit

Catalog #

40342

$550 *

Size: 384 reactions

Qty

Bulk/Custom

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*US Pricing only. For international pricing, please contact your local distributor.

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Description

The SMARCA2 TR-FRET Assay Kit is designed to measure the inhibition of SMARCA2 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 2) binding to its substrate in a homogeneous 384-reaction format. This FRET (Time Resolved Fluorescence Resonance Energy Transfer)-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward: a terbium-labeled donor, dye-labeled acceptor, SMARCA2 protein (amino acids 1375-1511), Bromodomain Ligand, and test inhibitor are incubated together for 120 minutes. Then, the fluorescence intensity is measured using a fluorescence reader capable of measuring TR-FRET.

Need us to run inhibitor screens or profile your compounds against SMARCA2? Check out our Bromodomain Screening Services.

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Synonyms

SMARCA2, BRM, SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2, AT-Rich Interaction Domain 1B, ARID1B, HTRF

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Product Data Gallery

Inhibition of SMARCA2 by PFI3.

Product Info

Storage and Usage

Citations

Assay Kit Format

TR-FRET

Species

Human

Materials Required But Not Supplied

Fluorescent reader capable of measuring Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET)
Adjustable micropipettor and tips

Format

Catalog #	Name	Amount	Storage
31141	SMARCA2, GST-Tag*	10 µg	-80°C
33003	Bromodomain Ligand 2	1 µg	-80°C
	Tb-Labeled Donor	2 x 10 µl	-20°C
	Dye-Labeled Acceptor	2 x 10 µl	-20°C
33012	3x BRD TR-FRET Assay Buffer 1	4 ml	-20°C
79969	White, Nonbinding, low volume, microtiter plate	1	Room temp.

*The concentrations of protein are lot-specific and will be indicated on the tubes containing the protein.

UniProt #

P51531

Background

SMARCA2 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 2), also known as SNF2L2 has helicase and ATPase activity and is part of the SNF/SWI (Switch/Sucrose Non-Fermentable) ATP-dependent chromatin remodeling complex. SMARCA2 is a multidomain protein. One its domains, the BRD (bromodomain) binds to acetylated lysine in histone tails. Mutations in SWI/SNF protein accounts for about 20% of tumors. Interestingly, in cancers involving SMARCA4 mutations, inactivation of SMARCA2 results in synthetic lethality. The use of inhibitors could thus be of interest, however so far, most inhibitors have dual specificity for both SMARCA2 and SMARCA4 and have dose-limiting tolerability issues. Few inhibitors are also targeting the BRD domain, the main one being PIF3. One alternative approach is the development of PROTACs (proteolysis targeting chimeras). Further studies on this protein and continued development of strategies to target it will open new doors in cancer treatment.

References

Schiaffino-Ortega S., et al., 2014. J. Hematol. Oncol. 7:81.
Lu T., et al., 2018 Acta Pharmacologica Sinica 39:1544-1552.
Cantley J., et al., 2022 Nature Communications 13:6814.

Storage/Stability

This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.

Applications

Study enzyme kinetics
Screen small molecular inhibitors in high throughput applications

Shipping Temperature

-80°C

Notes

Trouble Shooting Guide
Visit bpsbioscience.com/assay-kits-faq for detailed troubleshooting instructions. For all further questions, please email [email protected]

Contraindications

The final concentration of DMSO in the assay should not exceed 0.5%. Higher DMSO concentrations can significantly decrease the quality of the results.
Compounds that are fluorescent may interfere with the results, depending on their spectral excitation and emission properties.
It is recommended that the compound alone is tested to determine any potential interference of the compound on the assay results.

Warnings

Avoid freeze/thaw cycles.

Disclaimers and Limitations

BPS Bioscience assay kits are validated using the listed components according to our specific protocol. Any deviations to kit components or protocols, such as using different proteins, cell/tissue lysates, or buffers (including using the same component from other commercial sources) will void any warranties on the performance of the assay kit and is not recommended.

End-users should immediately report any issues to [email protected] upon receipt of the kit, such as missing components, damaged vials, no dry ice, etc.

Scientific Category

Bromodomain

Regulatory Status

Research Use Only