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AdipoGen Life Sciences
KUNB31
80
CHF
CHF 80.00
In stock
AG-CR1-3758-M0011 mgCHF 80.00
NEW
| Product Details | |
|---|---|
| Synonyms | (4-Hydroxy-7-isopropylbenzo[d]isoxazol-5-yl)(isoindolin-2-yl)methanone |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H18N2O3 |
| MW | 322.4 |
| CAS | 2220263-80-7 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white powder. |
| Solubility | Soluble in DMSO (2mg/ml). |
| InChi Key | MFZKTINXWPQHBG-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC(C(C)C)=C(ON=C2)C2=C1O)N3CC(C=CC=C4)=C4C3 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
- KUNB31 is an isoform-selective potent inhibitor of HSP90β with an IC50 value of 180 nM and > 50-fold selectivity over the isoforms HSP90α and GRP94. KUNB31 was shown to induce the degradation of HSP90β-dependent client proteins, but not those of Hsp90α and GRP94. It showed anti-proliferative activity against NCI H23 (non-small cell lung cancer), UC3 (bladder cancer) and HT-29 (colon adenocarcinoma) cells. KUNB31 specificly induces the degradation of HSP90β-dependent client proteins (EGFR, HER2, CDK4, CDK6, CXCR4 etc.) in cells.
- Heat-shock protein 90 (HSP90) is an abundant protein involved in many cellular signaling processes, including inflammation. HSP90 binds NLRP3 and regulates inflammasome activation and IL-1β secretion. HSP90 inhibitors are used to inhibit NLRP3-dependent inflammation and study inflammasome responses in disease. Recently, it has been shown that while NLRP3 WT does not need HSP90β, mutated NLRP3 proteins (except E567K) that are autoactivated and responsible for the disease cryopyrin-associated periodic syndromes (CAPS) need the chaperone HSP90β during their autoactivation. KUNB31 is used as a selective HSP90β inhibitor in such NLRP3 inflammasome studies to inhibit NLRP3 activity.
Product References
- Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor: A. Khandelwal, et al.; Nat. Commun. 9, 425 (2018)
- Inhibitors of the NLRP3 inflammasome by HSP90 inhibitors: S. Nizami, et al.; Immunol. 162, 84 (2020)
- Selective Inhibition of the Hsp90α isoform: S.J. Mishra, et al.; Angew. Chem. Int. Ed. Engl. 60, 10547 (2021)
- Hiding in plain sight: Optimizing topoisomerase IIα inhibitors into Hsp90β selective binders: J. Dernovsek, et al.; Eur. J. Med. Chem. 280, 116934 (2024)
- HSP90β controls NLRP3 autoactivation: L. Spel, et al.; Sci. Adv. (ePub ahead of print) (2024)
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