NU2058

Catalog No.S5316 Batch:S531601

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Technical Data

Formula

C12H17N5O
Molecular Weight 247.30 CAS No. 161058-83-9
Solubility (25°C)* In vitro DMSO 49 mg/mL (198.13 mM)
Ethanol 49 mg/mL (198.13 mM)
Water 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 NU2058 (O(6)-Cyclohexylmethylguanine) is an inhibitor of CDK2 with IC50 value of 17 μM in an isolated enzyme assay. It also potentiates melphalan (DMF 2.3), and monohydroxymelphalan (1.7), but not temozolomide or ionising radiation.
Targets
CDK2 [1]
(Cell-free assay)		 CDK1 [2]
(Cell-free assay)
17 μM 26 μM
In vitro NU2058 alters the transport of cisplatin, causing more Pt-DNA adducts, as well as sensitizing cells to cisplatin- and melphalan-induced DNA damage. However, the effects of NU2058 are independent of CDK2 inhibition[1]. In LNCaP cells and their Casodex-resistant derivative, LNCaP-cdxR, growth inhibition by NU2058 is accompanied by a concentration-dependent increase in p27 levels, reduced CDK2 activity and pRb phosphorylation, a decrease in early gene expression and G1 cell cycle phase arrest in both cell lines. NU2058 induces cell cycle reduction in S phase and inhibits phosphorylation of pRb. It induces a G1 arrest and increases p27 protein expression in LNCaP cells, showing no significant effect on p21 levels[2].

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    The human head and neck cancer cell line, SQ20b

  • Concentrations

    100 μM

  • Incubation Time

    4 h

  • Method

    Cells are seeded into six-well plates (350,000 cells/well) and allowed to attach overnight. On the day of the experiment, growth media are replaced with media containing 100 μM of either NU2058, NU6102, NU6230 or DMSO (0.1% (v/v) final concentration) for 2 h followed by a further 2 h in the additional presence of cytotoxic drugs, unless otherwise indicated. For the radiation experiments, cells are treated for a total of 4 h with NU2058, and irradiated after the first 2 h. After treatment, the cells are washed twice with PBS, trypsinised, and replated into 100 mm Petri dishes at various cell densities (300-50,000 cells per plate). After approximately 12 days, media is removed, and cells are fixed with Carnoy's reagent (75% (v/v) methanol, 25% (v/v) acetic acid), stained with crystal violet (0.4% (w/v) in water) and colonies are counted.

Selleck's NU2058 has been cited by 1 publication

Blockade of Nuclear β-Catenin Signaling via Direct Targeting of RanBP3 with NU2058 Induces Cell Senescence to Suppress Colorectal Tumorigenesis [ Adv Sci (Weinh), 2022, e2202528] PubMed: 36270974

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.