Eg5 Inhibitor VII CAS: 912953-25-4
MF: C16H12F3NO
MW: 291.3
A very potent and selective Eg5/KSP inhibitor.

Eg5 Inhibitor VII (CAS 912953-25-4)

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Alternate Names: KSP Inhibitor VII; 6-(4-Trifluoromethyl)phenyl)-3,4-dihydro-2(1H)-quinolinone, GSK-1
Application: Eg5 Inhibitor VII is a very potent and selective Eg5/KSP inhibitor
CAS Number: 912953-25-4
Molecular Weight: 291.3
Molecular Formula: C16H12F3NO
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

Eg5 Inhibitor VII is a cell-permeable quinolinone compound that acts as a very potent and selective Eg5/KSP inhibitor by antagonizing ATP binding via an allosteric site. Eg5 Inhibitor VII effectively induces monopolar spindles in ovarian adenocarcinoma SKOV3 cells, and inhibits the proliferation of colorectal carcinoma HCT116 cells. Eg5 Inhibitor VII is not competitive with respect to microtubule and exhibits minimal activity against a panel of 7 other mitotic kinesins.


References

1. Luo, L., et al. 2007. Nat. Chem. Biol. 3: 722-726. PMID: 17922005

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml).
Storage :
Store at 4° C
Melting Point :
172.13° C (Predicted)
Boiling Point :
429.46° C at 760 mmHg (Predicted)
Density :
1.28 g/cm3 (Predicted)
Refractive Index :
n20D 1.54 (Predicted)
IC50 :
HCT-116: IC50 = 0.45 nM (human); Eg5: IC50 = 46 nM (human); HeLa: IC50 = 0.28 µM (human)
Ki Data :
Eg5/KSP: Ki= 1.4 nM (mutant A133D); Eg5/KSP: Ki= 1.7 nM (wild-type KSP); Eg5/KSP: Ki= 2.1 nM (mutant KHC-L5); Eg5/KSP: Ki= 2.2 nM (mutant D130V)
pK Values :
pKb: 0.69 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
12000936
SMILES :
C1CC(=O)NC2=C1C=C(C=C2)C3=CC=C(C=C3)C(F)(F)F

Download SDS (MSDS)

Certificate of Analysis

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Eg5 Inhibitor VII (CAS 912953-25-4)  Product Citations

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PMID: # 32084356  Structure. 28: 450-457.e5.

Citations 1 to 1 of 1 total
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