BSJ-4-116

Catalog No.S9859 Batch:S985901

Technical Data

Formula	C₄₀H₄₉ClN₈O₈S
Molecular Weight	837.38	CAS No.	2519823-34-6
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (119.42 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.

Targets

CDK12 ^[1]

In vitro

BSJ-4-116 selectively degrads CDK12 as assessed through quantitative proteomics. BSJ-4-116 downregulates the expression of DDR genes and exhibits antiproliferative activity in cancer cells. BSJ-4-116 also substantially suppresses the phosphorylation of Pol II Ser2 and Thr4.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Jurkat cells Concentrations 50 nM Incubation Time 8 h Method For poly(A) 3'-end sequencing, Jurkat cells are exposed to DMSO or THZ531 (250 nM) or to BSJ-4-116 or BSJ-4-116-NC (50 nM) for 8 h. RNA extraction is performed with TRIzol following the manufacturer's instructions. Total RNA is treated with DNase I. Sequencing libraries are prepared with the RNA-sequencing library kit following the manufacturer's instructions. All samples are sequenced on a HiSeq 2500 sequencer.

Cell Assay:^{^[1]}

Cell lines
Jurkat cells
Concentrations
50 nM
Incubation Time
8 h
Method
For poly(A) 3'-end sequencing, Jurkat cells are exposed to DMSO or THZ531 (250 nM) or to BSJ-4-116 or BSJ-4-116-NC (50 nM) for 8 h. RNA extraction is performed with TRIzol following the manufacturer's instructions. Total RNA is treated with DNase I. Sequencing libraries are prepared with the RNA-sequencing library kit following the manufacturer's instructions. All samples are sequenced on a HiSeq 2500 sequencer.

References

[1] Baishan Jiang, et al. Nat Chem Biol. 2021 Jun;17(6):675-683.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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