SML2273

KUNB31

≥98% (HPLC)

• Synonym(e): (4-Hydroxy-7-isopropylbenzo[d]isoxazol-5-yl)(isoindolin-2-yl)methanone
• Empirische Formel (Hill-System): C₁₉H₁₈N₂O₃
• CAS-Nummer: 2220263-80-7
• Molekulargewicht: 322.36
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: N3(Cc4c(cccc4)C3)C(=O)c1c(c2c([o]nc2)c(c1)C(C)C)O
• InChI key: MFZKTINXWPQHBG-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

Isoform-selective inhibitor of Hsp90β

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 heat shock response. KUNB31 was shown to induce the degradation of Hsp90β-dependent client proteins, but not those of Hsp90α and GRP94, and 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 values, while requiring more than 100 μM against non-cancerous human embryonic kidney HEK-293 cells.

Sicherheitshinweise

• Lagerklasse: 13 - Non Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable