Benzisoxazole Hsp90 InhibitorAn inhibitor that binds to the N-terminal domain of Hsp90

Benzisoxazole Hsp90 Inhibitor (CAS 1012788-65-6)

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Synonym: 4-chloro-6-[5-[[2-(4-morpholinyl)ethyl]amino]-1,2-benzisoxazol-3-yl]-1,3-benzenediol
Application: An inhibitor that binds to the N-terminal domain of Hsp90
CAS Number: 1012788-65-6
Purity: ≥98%
Molecular Weight: 389.84
Molecular Formula: C19H20ClN3O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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Heat shock protein 90 (Hsp90) is a molecular chaperone that modulates intracellular signaling and protein folding, trafficking, and turnover. Inhibitors of Hsp90, such as geldanamycin, have shown potential as anti-tumor agents. Benzisoxazole Hsp90 Inhibitor binds the N-terminal domain of Hsp90, efficiently displacing geldanamycin from the ATP binding site (IC50 = 30 nM). It also inhibits the proliferation of several cancer cell lines (IC50~ 0.28 μM), promotes the degradation of the Hsp90 client proteins Her-2 and androgen receptor, and has no effect on a variety of kinases.


References

1 Gopalsamy, A., Shi, M., Golas, J., et al. Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90. J Med Chem 51 373-375 (2008).

Physical State :
Solid
Solubility :
Soluble in 1:10 EtOH: PBS (pH 7.2) (0.1 mg/ml), ethanol (~20 mg/ml), DMSO (~20 mg/ml), and DMF (~20 mg/ml).
Storage :
Store at -20° C
Boiling Point :
~655.1° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
N-terminal domain of Hsp90: IC50 = 30 nM; HCT-116: IC50 = 50 nM (human); LNCaP: IC50 = 170 nM (human); DU-145: IC50 = 290 nM (human); the proliferation of several cancer cell lines : IC50 = 0.28 µM
pK Values :
pKa: 7.07 (Predicted), pKb: 6.88 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
51538650
MDL Number :
MFCD18382085
SMILES :
C1COCCN1CCNC2=CC3=C(C=C2)ONC3=C4C=C(C(=CC4=O)O)Cl

Download SDS (MSDS)

Certificate of Analysis

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