YK-3-237
Based on 1 publication(s) in Google Scholar
YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells.
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 1215281-19-8
- Formula: C19H21BO7
- Molecular Weight:372.18
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) YK-3-237
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Biological Activity
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SIRT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
0.39 μM
Compound: 4
|
Growth inhibition of human 786-0 cells after 48 hrs by SRB assay
Growth inhibition of human 786-0 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| A10 | EC50 |
16.5 μM
Compound: 4
|
Inhibition of tubulin in rat A10 cells assessed as induction of cellular microtubule disassembly after 18 hrs by indirect immunofluorescence technique
Inhibition of tubulin in rat A10 cells assessed as induction of cellular microtubule disassembly after 18 hrs by indirect immunofluorescence technique
|
[PMID: 20006519] |
| A498 | GI50 |
4.76 μM
Compound: 4
|
Growth inhibition of human A498 cells after 48 hrs by SRB assay
Growth inhibition of human A498 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| A549 | GI50 |
0.45 μM
Compound: 4
|
Growth inhibition of human A549 cells after 48 hrs by SRB assay
Growth inhibition of human A549 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| ACHN | GI50 |
0.52 μM
Compound: 4
|
Growth inhibition of human ACHN cells after 48 hrs by SRB assay
Growth inhibition of human ACHN cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| BT-549 | GI50 |
0.021 μM
Compound: 4
|
Growth inhibition of human BT549 cells after 48 hrs by SRB assay
Growth inhibition of human BT549 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| CAKI-1 | GI50 |
6.39 μM
Compound: 4
|
Growth inhibition of human Caki1 cells after 48 hrs by SRB assay
Growth inhibition of human Caki1 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| CCRF-CEM | GI50 |
2.39 μM
Compound: 4
|
Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay
Growth inhibition of human CCRF-CEM cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| COLO 205 | GI50 |
2.2 μM
Compound: 4
|
Growth inhibition of human COLO205 cells after 48 hrs by SRB assay
Growth inhibition of human COLO205 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| DU-145 | GI50 |
0.05 μM
Compound: 4
|
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
Growth inhibition of human DU145 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| EKVX | GI50 |
1.31 μM
Compound: 4
|
Growth inhibition of human EKVX cells after 48 hrs by SRB assay
Growth inhibition of human EKVX cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| HCC 2998 | GI50 |
0.41 μM
Compound: 4
|
Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay
Growth inhibition of human HCC2998 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| HCT-116 | GI50 |
0.37 μM
Compound: 4
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Growth inhibition of human HCT116 cells after 48 hrs by SRB assay
Growth inhibition of human HCT116 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| HCT-15 | GI50 |
<0.01 μM
Compound: 4
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Growth inhibition of human HCT15 cells after 48 hrs by SRB assay
Growth inhibition of human HCT15 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| HOP-62 | GI50 |
0.098 μM
Compound: 4
|
Growth inhibition of human HOP62 cells after 48 hrs by SRB assay
Growth inhibition of human HOP62 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| HOP-92 | GI50 |
0.38 μM
Compound: 4
|
Growth inhibition of human HOP92 cells after 48 hrs by SRB assay
Growth inhibition of human HOP92 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| Hs-578T | GI50 |
0.046 μM
Compound: 4
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Growth inhibition of human Hs 578T cells after 48 hrs by SRB assay
Growth inhibition of human Hs 578T cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| IGROV-1 | GI50 |
0.088 μM
Compound: 4
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Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay
Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| K562 | GI50 |
3.46 μM
Compound: 4
|
Growth inhibition of human K562 cells after 48 hrs by SRB assay
Growth inhibition of human K562 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| KM12 | GI50 |
15.4 μM
Compound: 4
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Growth inhibition of human KM12 cells after 48 hrs by SRB assay
Growth inhibition of human KM12 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| LOX IMVI | GI50 |
0.06 μM
Compound: 4
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Growth inhibition of human LOXIMVI cells after 48 hrs by SRB assay
Growth inhibition of human LOXIMVI cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| M14 | GI50 |
1.19 μM
Compound: 4
|
Growth inhibition of human M14 cells after 48 hrs by SRB assay
Growth inhibition of human M14 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| Malme-3M | GI50 |
5.49 μM
Compound: 4
|
Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay
Growth inhibition of human MALME-3M cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| MCF7 | GI50 |
0.034 μM
Compound: 4
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Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
Growth inhibition of human MCF7 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| MCF7 | IC50 |
0.9 μM
Compound: 4
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Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay
Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay
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[PMID: 20006519] |
| MDA-MB-231 | GI50 |
0.11 μM
Compound: 4
|
Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay
Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| MDA-MB-435 | GI50 |
1.95 μM
Compound: 4
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Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay
Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| MOLT-4 | GI50 |
3.6 μM
Compound: 4
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Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay
Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| NCI/ADR-RES | GI50 |
0.05 μM
Compound: 4
|
Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay
Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| NCI-H226 | GI50 |
4.14 μM
Compound: 4
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Growth inhibition of human NCI-H226 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H226 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| NCI-H23 | GI50 |
0.14 μM
Compound: 4
|
Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H23 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| NCI-H322M | GI50 |
8.44 μM
Compound: 4
|
Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H322M cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| NCI-H460 | GI50 |
0.028 μM
Compound: 4
|
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| NCI-H522 | GI50 |
0.2 μM
Compound: 4
|
Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay
Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| OVCAR-3 | GI50 |
2.08 μM
Compound: 4
|
Growth inhibition of human OVCAR-3 cells after 48 hrs by SRB assay
Growth inhibition of human OVCAR-3 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| OVCAR-4 | GI50 |
2.06 μM
Compound: 4
|
Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay
Growth inhibition of human OVCAR4 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| OVCAR-5 | GI50 |
1.81 μM
Compound: 4
|
Growth inhibition of human OVCAR5 cells after 48 hrs by SRB assay
Growth inhibition of human OVCAR5 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| OVCAR-8 | GI50 |
0.3 μM
Compound: 4
|
Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay
Growth inhibition of human OVCAR8 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| PC-3 | GI50 |
0.25 μM
Compound: 4
|
Growth inhibition of human PC3 cells after 48 hrs by SRB assay
Growth inhibition of human PC3 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| RXF 393 | GI50 |
0.39 μM
Compound: 4
|
Growth inhibition of human RXF393 cells after 48 hrs by SRB assay
Growth inhibition of human RXF393 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| SF-268 | GI50 |
0.8 μM
Compound: 4
|
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
Growth inhibition of human SF268 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| SF-295 | GI50 |
2.73 μM
Compound: 4
|
Growth inhibition of human SF295 cells after 48 hrs by SRB assay
Growth inhibition of human SF295 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| SF-539 | GI50 |
0.035 μM
Compound: 4
|
Growth inhibition of human SF539 cells after 48 hrs by SRB assay
Growth inhibition of human SF539 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| SK-MEL-2 | GI50 |
3.33 μM
Compound: 4
|
Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay
Growth inhibition of human SK-MEL-2 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| SK-MEL-5 | GI50 |
0.31 μM
Compound: 4
|
Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay
Growth inhibition of human SK-MEL-5 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| SK-OV-3 | GI50 |
<0.01 μM
Compound: 4
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Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay
Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| SN12C | GI50 |
0.46 μM
Compound: 4
|
Growth inhibition of human SN12C cells after 48 hrs by SRB assay
Growth inhibition of human SN12C cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| SNB-19 | GI50 |
<0.01 μM
Compound: 4
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Growth inhibition of human SNB19 cells after 48 hrs by SRB assay
Growth inhibition of human SNB19 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| SR | GI50 |
2.18 μM
Compound: 4
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Growth inhibition of human SR cells after 48 hrs by SRB assay
Growth inhibition of human SR cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| SW-620 | GI50 |
0.037 μM
Compound: 4
|
Growth inhibition of human SW620 cells after 48 hrs by SRB assay
Growth inhibition of human SW620 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| TK-10 | GI50 |
20.9 μM
Compound: 4
|
Growth inhibition of human TK10 cells after 48 hrs by SRB assay
Growth inhibition of human TK10 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| U-251 | GI50 |
0.025 μM
Compound: 4
|
Growth inhibition of human U251 cells after 48 hrs by SRB assay
Growth inhibition of human U251 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
| UACC-257 | GI50 |
4.41 μM
Compound: 4
|
Growth inhibition of human UACC257 cells after 48 hrs by SRB assay
Growth inhibition of human UACC257 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| UACC-62 | GI50 |
0.034 μM
Compound: 4
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Growth inhibition of human UACC62 cells after 48 hrs by SRB assay
Growth inhibition of human UACC62 cells after 48 hrs by SRB assay
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[PMID: 20006519] |
| UO-31 | GI50 |
0.32 μM
Compound: 4
|
Growth inhibition of human UO31 cells after 48 hrs by SRB assay
Growth inhibition of human UO31 cells after 48 hrs by SRB assay
|
[PMID: 20006519] |
YK-3-237 exhibits the anti-proliferative activities toward most of the breast cancer cell lines tested at submicromolar concentration. YK-3-237 preferentially inhibits the proliferation of breast cancer cell lines carrying mtp53[1].
YK-3-237 inhibits the proliferation of triple-negative breast cancer (TNBC) HS578T, MDA-MB-453, SUM1315MO2, SUM149PT, BT549, MDA-MB-231, MDA-MB-436, MDA-MB-468, HCC1937 with IC50s of 0.160±0.043, 0.241±0.086, 0.253±0.028, 0.289±0.066, 0.353±0.017, 0.431±0.136, 0.501±0.062, 1.436±0.754, 5.031±2.010 μM, respectively[1].
YK-3-237 inhibits the proliferation of Luminal T47D, MCF7, and ZR-75-1 with IC50s of 1.573±0.370, 2.402±0.256, 3.822±0.967 μM, respectively[1].
YK-3-237 inhibits the proliferation of HER2 BT474 and SK-BR-3 with IC50s of 1.249±0.372 and 0.346±0.066 μM, respectively[1].
YK-3-237 (0.01-10 μM; 24 hours) deacetylates mtp53 in TNBC cell lines[1].
YK-3-237 is a potent activator of Sirt1, on the activation of renal interstitial fibroblasts using NRK-49F cells[2].
Exposure of cells to YK-3-237 also significantly reduces expression of α-SMA and fibronectin in a dose-dependent manner, with the maximum inhibition occurring at 10 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT549, MDA-MB-468, HS578T, SUM149PT
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Concentration:0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM
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Incubation Time:24 hours
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Result:Reduced both the acetylation of K382 and the level of mtp53 in a dose-dependent manner in mtp53 TNBC cell lines.
Chemical Information
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CAS No. 1215281-19-8
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Appearance Solid
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Molecular Weight 372.18
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Formula C19H21BO7
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Color White to light yellow
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SMILES
COC1=C(C=C(C=C1OC)C(/C=C/C2=CC(B(O)O)=C(C=C2)OC)=O)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (268.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yong Weon Yi, et al. Targeting mutant p53 by a SIRT1 activator YK-3-237 inhibits the proliferation of triple-negative breast cancer cells. Oncotarget. 2013 Jul;4(7):984-94. [Content Brief]
[2]. Murugavel Ponnusamy, et al. Activation of Sirtuin-1 Promotes Renal Fibroblast Activation and Aggravates Renal Fibrogenesis. J Pharmacol Exp Ther. 2015 Aug;354(2):142-51. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6869 mL | 13.4344 mL | 26.8687 mL | 67.1718 mL |
| 5 mM | 0.5374 mL | 2.6869 mL | 5.3737 mL | 13.4344 mL | |
| 10 mM | 0.2687 mL | 1.3434 mL | 2.6869 mL | 6.7172 mL | |
| 15 mM | 0.1791 mL | 0.8956 mL | 1.7912 mL | 4.4781 mL | |
| 20 mM | 0.1343 mL | 0.6717 mL | 1.3434 mL | 3.3586 mL | |
| 25 mM | 0.1075 mL | 0.5374 mL | 1.0747 mL | 2.6869 mL | |
| 30 mM | 0.0896 mL | 0.4478 mL | 0.8956 mL | 2.2391 mL | |
| 40 mM | 0.0672 mL | 0.3359 mL | 0.6717 mL | 1.6793 mL | |
| 50 mM | 0.0537 mL | 0.2687 mL | 0.5374 mL | 1.3434 mL | |
| 60 mM | 0.0448 mL | 0.2239 mL | 0.4478 mL | 1.1195 mL | |
| 80 mM | 0.0336 mL | 0.1679 mL | 0.3359 mL | 0.8396 mL | |
| 100 mM | 0.0269 mL | 0.1343 mL | 0.2687 mL | 0.6717 mL |