Home Cell Cycle CDK inhibitor NU2058 For research use only.

NU2058

Synonyms: O(6)-Cyclohexylmethylguanine

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.

NU2058 Chemical Structure

NU2058 Chemical Structure

CAS: 161058-83-9

Selleck's NU2058 has been cited by 1 publication

Purity & Quality Control

Batch: S531601 DMSO] 49 mg/mL] false] Ethanol] 49 mg/mL] false] Water] Insoluble] false Purity: 99.32%
99.32

NU2058 Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Choose Selective CDK Inhibitors

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
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].
Cell Research 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.

Chemical Information & Solubility

Molecular Weight 247.30 Formula

C12H17N5O
CAS No. 161058-83-9 SDF --
Smiles C1CCC(CC1)COC2=NC(=NC3=C2NC=N3)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 49 mg/mL ( (198.13 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 49 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy NU2058 | NU2058 supplier | purchase NU2058 | NU2058 cost | NU2058 manufacturer | order NU2058 | NU2058 distributor