1. Cell Cycle/DNA Damage Epigenetics
  2. Sirtuin
  3. YK-3-237

YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells.

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YK-3-237 Chemical Structure

YK-3-237 Chemical Structure

CAS No. : 1215281-19-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
1 mg USD 33 In-stock
5 mg USD 70 In-stock
10 mg USD 110 In-stock
25 mg USD 230 In-stock
50 mg USD 390 In-stock
100 mg USD 680 In-stock
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Description

YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells[1].

IC50 & Target[1]

SIRT1

 

In Vitro

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.

Cell Viability Assay[1]

Cell Line: BT549, MDA-MB-468, HS578T, SUM149PT
Concentration: 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM
Incubation Time: 24 hours
Result: Reduced both the acetylation of K382 and the level of mtp53 in a dose-dependent manner in mtp53 TNBC cell lines.
Molecular Weight

372.18

Formula

C19H21BO7

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

COC1=C(C=C(C=C1OC)C(/C=C/C2=CC(B(O)O)=C(C=C2)OC)=O)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6869 mL 13.4344 mL 26.8687 mL
5 mM 0.5374 mL 2.6869 mL 5.3737 mL
View the 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.

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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
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YK-3-237 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
YK-3-237
Cat. No.:
HY-19634
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