Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listNSC 663284

NSC 663284

Synonym(s):6-Chloro-7-(2-morpholin-4-yl-ethylamino)quinoline-5,8-dione, DA3003-1, PTP Inhibitor XXI, VHR Inhibitor II;CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem

NSC 663284 Structural

What is NSC 663284?

Description

NSC663284 (383907-43-5) is a potent, selective and irreversible inhibitor of CDC25 phosphatases, Ki=29, 95 and 89 nM for human CDC25A, B2 and C respectively and >20- and >450-fold selective over VHR and PTP1B.1?Arrests cells at G1 and G2/M and inhibits cdk1 and 2 activation.2 Inhibits the growth of a variety of human tumor cell lines.3 NSC663284 acts via irreversible oxidation of the catalytic cysteine of CDC25.4

The Uses of NSC 663284

CDC25 Phosphatase Inhibitor II, NSC 663284 is a competitive CDC25 inhibitor and cell cycle arresting compound.

What are the applications of Application

CDC25 Phosphatase Inhibitor II, NSC 663284 is a competitive CDC25 inhibitor and cell cycle arresting compound

Definition

ChEBI: 6-chloro-7-[2-(4-morpholinyl)ethylamino]quinoline-5,8-dione is a quinolone.

General Description

A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (Ki = 29 nM, 95 nM, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively) with anti-proliferative properties. Displays nearly 20- and 450-fold greater selectivity over VHR and PTP1B (IC50 = 4.0 μM and >100 μM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation, and delay tumor growth (mean IC50 = 1.5 μM in NCI-60 tumor cell panel). Also shown to block ERK dephosphorylation caused by ectopic Cdc25A expression.

Biological Activity

Potent, selective inhibitor of Cdc25 dual specificity phosphatases (K i values are 29, 95 and 89 nM for human Cdc25A, Cdc25B 2 and Cdc25C respectively); > 20- and > 450-fold selective over VHR and PTP1B phosphatases respectively. Arrests cells at both G 1 and G 2 /M phase and blocks cdk2 and cdk1 activation. Blocks proliferation of a range of human tumor cell lines (IC 50 = 0.2-35 μ M).

Biochem/physiol Actions

Cell permeable: yes

storage

Store at +4°C

References

1) Lazo et al. (2001), Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatases Cdc25; J. Med. Chem., 44 4042 2) Pu et al. (2002), Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 6-chloro-7-(2-morpholin-4-ylethylamino)-quinoline-3,8-dione; J. Biol. Chem., 277 46877 3) Han et al. (2004), NAD(P)H:quinone oxidoreductase-1-dependent and independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors; J. Pharmacol. Exp. Ther., 309 64 4) Brisson et al. (2005), Redox regulation of Cdc25B by cell-active quinolonediones; Mol. Pharmacol., 68 1810

Properties of NSC 663284

Boiling point: 478.8±45.0 °C(Predicted)
Density  1.41±0.1 g/cm3(Predicted)
storage temp.  2-8°C
solubility  DMSO: 16 mg/mL
form  solid
pka 6.79±0.10(Predicted)
color  red
Sensitive  Light Sensitive
Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

Safety information for NSC 663284

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P304+P340:IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P405:Store locked up.

Computed Descriptors for NSC 663284

Related products of tetrahydrofuran

You may like

  • Thermo Scientific Chemicals NSC 663284 CAS 383907-43-5
    Thermo Scientific Chemicals NSC 663284 CAS 383907-43-5
    383907-43-5
    View Details
  • CDC25 Phosphatase Inhibitor II, NSC 663284 CAS 383907-43-5
    CDC25 Phosphatase Inhibitor II, NSC 663284 CAS 383907-43-5
    383907-43-5
    View Details
  • NSC 663284 CAS 383907-43-5
    NSC 663284 CAS 383907-43-5
    383907-43-5
    View Details
  • 1823368-42-8 98%
    1823368-42-8 98%
    1823368-42-8
    View Details
  • 2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%
    1307449-08-6
    View Details
  • Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%
    25408-95-1
    View Details
  • 2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%
    1805639-70-6
    View Details
  • Lithium Clavulanate
    Lithium Clavulanate
    61177-44-4
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.