์ฐ๊ตฌ์ฉ
์ ํ ๋ฒํธS2298
| ๊ด๋ จ ํ๊ฒ | HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK |
|---|---|
| ๊ธฐํ Sirtuin ์ต์ ์ | SRT 1720 Hydrochloride Selisistat (EX-527) Sirtinol 3-TYP AGK2 SRT2104 (GSK2245840) OSS_128167 SirReal2 SRT2183 Thiomyristoyl |
| ์ธํฌ์ฃผ | ๋ถ์ ์ ํ | ๋๋ | ๋ฐฐ์ ์๊ฐ | ์ ํ | ํ์ฑ ์ค๋ช | PMID |
|---|---|---|---|---|---|---|
| MDA-MB-453 | Cell viability assay | 0, 20, 40, 60, 80, and 100 ยตM | 24, 48, and 72 hours | With increasing concentrations of fisetin (0, 20, 40, 60, 80, and 100 ยตM), there was a decrease observed in cell number in different time intervals (24, 48, and 72 hours). | ||
| SGC7901 | Proliferation assay | 0, 1, 5, 10, 15 or 20 ยตM | 48 h | inhibits proliferation | ||
| A549 | Cell viability assay | 0, 10, 20, 30 or 40 ยตM | 24, 48 or 72 h | fisetin was effective in inhibiting the growth of A549 cells in a dose- and time-dependent manner | ||
| ARPE-19 | Cell migration assay | 5 or 10 ฮผM | 24 h | pretreatment with fisetin markedly reduced cell migration in EGF-treated ARPE-19 cells | ||
| SCC-23 | Cell viability assay | 0-100 ฮผM | 24 h | fisetin significantly inhibited cell viability in a dose-dependent manner (significantly when the concentration is higher than 20 ฮผM) | ||
| Tca-8113 | Cell viability assay | 0-100 ฮผM | 24 h | fisetin significantly inhibited cell viability in a dose-dependent manner (significantly when the concentration is higher than 20 ฮผM) | ||
| ํด๋ฆญํ์ฌ ๋ ๋ง์ ์ธํฌ์ฃผ ์คํ ๋ฐ์ดํฐ ๋ณด๊ธฐ | ||||||
| ๋ถ์๋ | 286.24 | ํํ์ | C15H10O6 |
๋ณด๊ด (์๋ น์ผ๋ก๋ถํฐ) | |
|---|---|---|---|---|---|
| CAS ๋ฒํธ | 528-48-3 | SDF ๋ค์ด๋ก๋ | ์์ก ๋ณด๊ด |
|
|
|
In vitro |
DMSO
: 57 mg/mL
(199.13 mM)
Ethanol : 9 mg/mL Water : Insoluble |
|
In vivo |
|||||
1๋จ๊ณ: ์๋ ์ ๋ณด ์ ๋ ฅ (๊ถ์ฅ: ์คํ ์ค ์์ค์ ๊ณ ๋ คํ์ฌ ์ถ๊ฐ ๋๋ฌผ ํฌํจ)
2๋จ๊ณ: ์์ฒด ๋ด ์ ํ ์ ๋ ฅ (์ด๊ฒ์ ๊ณ์ฐ๊ธฐ์ผ ๋ฟ ์ ํ์ด ์๋๋๋ค. ์ฉํด๋ ์น์ ์ ์์ฒด ๋ด ์ ํ์ด ์๋ ๊ฒฝ์ฐ ๋จผ์ ๋น์ฌ์ ๋ฌธ์ํ์ญ์์ค.)
๊ณ์ฐ ๊ฒฐ๊ณผ:
์์ ๋๋: mg/ml;
DMSO ์์ก ์ค๋น ๋ฐฉ๋ฒ: mg ์ฝ๋ฌผ ์ฌ์ ์ฉํด ฮผL DMSO ( ์์ก ๋๋ mg/mL, ๋๋๊ฐ ํด๋น ์ฝ๋ฌผ ๋ฐฐ์น์ DMSO ์ฉํด๋๋ฅผ ์ด๊ณผํ๋ ๊ฒฝ์ฐ ๋จผ์ ๋น์ฌ์ ๋ฌธ์ํ์ญ์์ค. )
์์ฒด ๋ด ์ ํ ์ค๋น ๋ฐฉ๋ฒ: ์ทจํ๋ค ฮผL DMSO ์์ก, ๋ค์ ์ถ๊ฐฮผL PEG300, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํ ๋ค์ ์ถ๊ฐฮผL Tween 80, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํ ๋ค์ ์ถ๊ฐ ฮผL ddH2O, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํฉ๋๋ค.
์์ฒด ๋ด ์ ํ ์ค๋น ๋ฐฉ๋ฒ: ์ทจํ๋ค ฮผL DMSO ์์ก, ๋ค์ ์ถ๊ฐ ฮผL ์ฅ์์ ๊ธฐ๋ฆ, ํผํฉํ๊ณ ํฌ๋ช ํ๊ฒ ํฉ๋๋ค.
์ฐธ๊ณ : 1. ๋ค์ ์ฉ๋งค๋ฅผ ์ถ๊ฐํ๊ธฐ ์ ์ ์ก์ฒด๊ฐ ํฌ๋ช
ํ์ง ํ์ธํ์ญ์์ค.
2. ์ฉ๋งค๋ฅผ ์์๋๋ก ์ถ๊ฐํด์ผ ํฉ๋๋ค. ๋ค์ ์ฉ๋งค๋ฅผ ์ถ๊ฐํ๊ธฐ ์ ์ ์ด์ ์ถ๊ฐ์์ ์ป์ ์ฉ์ก์ด ํฌ๋ช
ํ ์ฉ์ก์ธ์ง ํ์ธํด์ผ ํฉ๋๋ค. ์๋, ์ด์ํ ๋๋ ๋จ๊ฑฐ์ด ๋ฌผ ์คํ๊ณผ ๊ฐ์ ๋ฌผ๋ฆฌ์ ๋ฐฉ๋ฒ์ ์ฌ์ฉํ์ฌ ์ฉํด๋ฅผ ๋์ธ ์ ์์ต๋๋ค.
| Targets/IC50/Ki |
Sirtuin
|
|---|---|
| ์ํ๊ด ๋ด(In vitro) |
Fisetin selectively kills SPiDER-β-Gal positive senescence neural cells in vitro. |
| ์์ฒด ๋ด(In vivo) |
Oral administration of fisetin, a senolytic drug, reduces the number of senescent neural cells observed, the SASP expression level, and depressive behavior in MRL/lpr mice. |
์ฐธ์กฐ |
|
| ๋ฐฉ๋ฒ | ๋ฐ์ด์ค๋ง์ปค | ์ด๋ฏธ์ง | PMID |
|---|---|---|---|
| Western blot | p-IKKฮฑ/ฮฒ / IKKฮฒ / IKKฮฑ / p-IฮบBฮฑ / IฮบBฮฑ / p-p65 / p65 XBP1s / ATF6 / CHOP / ATF4 / PERK DR3 / pNF-ฮบB / NF-ฮบB p-mTOR / mTOR / Raptor / Rictor |
|
23861901 |
| Immunofluorescence | p-4EBP1 / p-eIF4B / p-rpS6 uPA |
|
20530556 |
| Growth inhibition assay | Cell viability |
|
19670328 |
(๋ฐ์ดํฐ ์ถ์ฒ https://clinicaltrials.gov, ์ ๋ฐ์ดํธ ๋ ์ง 2024-05-22)
| NCT ๋ฒํธ | ๋ชจ์ง | ์กฐ๊ฑด | ์คํฐ์/ํ๋ ฅ์ | ์์์ผ | ๋จ๊ณ |
|---|---|---|---|---|---|
| NCT05758246 | Recruiting | Sepsis|Acute Infection|Organ Failure |
University of Minnesota |
August 23 2023 | Phase 2 |