| Identification | Back Directory | [Name]
KUNB 31 | [CAS]
2220263-80-7 | [Synonyms]
KUNB 31
Methanone, (1,3-dihydro-2H-isoindol-2-yl)[4-hydroxy-7-(1-methylethyl)-1,2-benzisoxazol-5-yl]- | [Molecular Formula]
C19H18N2O3 | [MDL Number]
MFCD32264611 | [MOL File]
2220263-80-7.mol | [Molecular Weight]
322.36 |
| Chemical Properties | Back Directory | [Boiling point ]
544.1±50.0 °C(Predicted) | [density ]
1.314±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
6.92±0.50(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
KUNB31 is a selective inhibitor of SP90β with an Kd value of 0.18 μM[1]. | [Biological Activity]
KUNB31 is an isoform-selective inhibitor of Hsp90β with an IC50 value of 180 nM and > 50-fold selectivity over closely related isoforms Hsp90α and GRP94.Hsp90 inhibitors currently in clinical trials are all pan-inhibitors with multiple side effects including induction of the pro-survival he at shock response. KUNB31 was shown to induce the degradation of Hsp90β-dependent client proteinsbut not those of Hsp90α and GRP94and did not induce production of Hsp90. It showed anti-proliferative activity against NCI H23 (non-small cell lung cancer)UC3 (bladder cancer)and HT-29 (colon adenocarcinoma) cells with low micromolar IC50 valueswhile requiring more than 100 μM against non-cancerous human embryonic kidney HEK-293 cells. | [References]
[1] Lei Wang, et al. Modulation of protein fate decision by small molecules: targeting molecular chaperone machinery. Acta Pharm Sin B. 2020 Oct; 10(10): 1904–1925. |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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