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Ispinesib

Catalog No. T2103   CAS 336113-53-2
Synonyms: CK0238273, SB-715992

Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Ispinesib Chemical Structure
Ispinesib, CAS 336113-53-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 46.00
5 mg In stock $ 72.00
10 mg In stock $ 121.00
25 mg In stock $ 222.00
50 mg In stock $ 356.00
100 mg In stock $ 587.00
500 mg In stock $ 1,280.00
1 mL * 10 mM (in DMSO) In stock $ 82.00
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Purity: 99.57%
Purity: 98.59%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.
Targets&IC50 KSP (HsEg5):1.7 nM(Ki app)
Kinase Assay Steady-State Kinetic Analysis of Human KSP ATPase Activity and Inhibition by Ispinesib: Kinesin specificity analysis is carried out using a pyruvate kinase-lactate dehydrogenase detection system that couples the production of ADP to oxidation of NADH. Absorbance changes are monitored at 340 nm. Steady-state studies using nanomolar concentrations of KSP are performed using a sensitive fluorescence-based assay utilizing a pyruvate kinase, pyruvate oxidase, and horseradish peroxidase (HRP) coupled detection system that couples the generation of ADP to oxidation of Amplex Red to fluorescent resorufin. Generation of resorufin is monitored by fluorescence (λexcitation = 520 nm and λemission = 580 nm). Steady-state biochemical experiments are performed in PEM25 buffer [25 mM Pipes-K+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM paclitaxel for experiments involving microtubules. The IC50 for steady-state inhibition is determined at 500 μM ATP, 5 μM Microtubules, and 1 nM KSP in PEM25 buffer. Ki app (apparent inhibitor dissociation constant) values of Ispinesib are extracted from the dose-response curves, with explicit correction for enzyme concentration by using the Morrison equation. Inhibitor modality (e.g., competitive, noncompetitive, uncompetitive, or mixed) under steady-state conditions is determined by measuring the effect of inhibitor concentration on initial velocity as a function of substrate concentrations. Data are fit using equations in GraFit to velocity equations for the various modes of inhibition.
Cell Research Cells are plated in log phase of growth in 96-well plates and treated with Ispinesib for 72 hours. Then, cell growth is measured using CellTiter-Glo, and luminescence is detected using BioTek FLx800. Data are analyzed and the IC50 value, defined as the drug concentration that results in 50% growth inhibition relative to control, is calculated.(Only for Reference)
Synonyms CK0238273, SB-715992
Molecular Weight 517.06
Formula C30H33ClN4O2
CAS No. 336113-53-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 95 mg/mL (183.7 mM)

DMSO: 95 mg/mL (183.7 mM)

TargetMolReferences and Literature

1. Lad L, et al. Biochemistry, 2008, 47(11), 3576-3585. 2. Johnson RK, et al. Proc Am Assoc Cancer Res, 2002, 43, 269. 3. Davis DA, et al. BMC Cancer, 2006, 6, 22. 4. Purcell JW, et al. Clin Cancer Res, 2010, 16(2), 566-576.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Cell Cycle Compound Library Apoptosis Compound Library Clinical Compound Library NO PAINS Compound Library

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Keywords

Ispinesib 336113-53-2 Apoptosis Cell Cycle/Checkpoint Cytoskeletal Signaling Kinesin KSP CK-0238273 inhibit SB715992 Inhibitor CK0238273 CK 0238273 SB 715992 SB-715992 inhibitor

 

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