NSC663284 Inhibitor – NSC 663284

Name: NSC663284 Inhibitor; NSC 663284; MyBioSource
Brand: MyBioSource
SKU: MBS5755287
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755287

NSC 663284 is a cell-permeable and irreversible Cdc25 dual specificity phosphatase inhibitor (IC50 for Cdc25B2: 0.21uM). NSC 663284 inhibits NSD2 (IC50 of 170nM) through direct interaction with the catalytic SET domain (Kd of 370nM). NSC 663284 displays mixed… More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

NSC 663284 (NSC663284), Inhibitor

Full Product Name

NSC 663284

Product Gene Name

NSC663284, inhibitor

Product Synonym Names

DA-3003-1

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

321.76

Solubility

DMSO: 150mg/mL (466.19mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C15H16ClN3O3

SMILES

O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O

CAS Number

383907-43-5

Target & IC50

Cdc25B2: ic50 0.21uM

In Vitro

NSC 663284 is not detectable in plasma or tissues beyond 5 minutes, after a single dose of 5mg/kg. NSC 663284 (intravenous injection; 2, 3, and 5mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. Following NSC 663284 treatment of tumor-bearing SCID mice, decreases glutathione concentrations in HT29 tumors are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in the liver and kidneys[3].

Product Categories/Family for NSC663284, inhibitor

Membrane transporter/Ion channel; Calcium Channel; Metabolic Enzyme/Protease

Product References and Citations for NSC663284, inhibitor

Lazo JS, et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44(24):4042-9.
Lazo JS, et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44(24):4042-9.
Coussens NP, et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSDJ Biol Chem. 2018 Aug 31;293(35):13750-13765.
Coussens NP, et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2. J Biol Chem. 2018 Aug 31;293(35):13750-13765.
Guo J, et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res. 2007 Sep-Oct;27(5A):3067-73.
Guo J, et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res. 2007 Sep-Oct;27(5A):3067-73.

Other Notes

Small volumes of NSC663284, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for NSC663284 purchase

MBS5755287 is an inhibitor targeting NSC663284. Also known as NSC 663284.