YK-3-237

Name: YK-3-237
Brand: MedChemExpress
SKU: HY-19634
Rating: 4.5 (1 reviews)

Cat. No.: HY-19634 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

YK-3-237 Chemical Structure

CAS No. : 1215281-19-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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

Cellular Effect

Cell Line	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	[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	[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	[PMID: 20006519]
HCT-116	GI₅₀	0.37 μM Compound: 4	Growth inhibition of human HCT116 cells after 48 hrs by SRB assay Growth inhibition of human HCT116 cells after 48 hrs by SRB assay	[PMID: 20006519]
HCT-15	GI₅₀	< 0.01 μM Compound: 4	Growth inhibition of human HCT15 cells after 48 hrs by SRB assay Growth inhibition of human HCT15 cells after 48 hrs by SRB assay	[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	[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	[PMID: 20006519]
Hs-578T	GI₅₀	0.046 μM Compound: 4	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	[PMID: 20006519]
IGROV-1	GI₅₀	0.088 μM Compound: 4	Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay Growth inhibition of human IGROV1 cells after 48 hrs by SRB assay	[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	[PMID: 20006519]
KM12	GI₅₀	15.4 μM Compound: 4	Growth inhibition of human KM12 cells after 48 hrs by SRB assay Growth inhibition of human KM12 cells after 48 hrs by SRB assay	[PMID: 20006519]
LOX IMVI	GI₅₀	0.06 μM Compound: 4	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	[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	[PMID: 20006519]
MCF7	GI₅₀	0.034 μM Compound: 4	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 20006519]
MCF7	IC₅₀	0.9 μM Compound: 4	Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay Antiproliferative activity against human MCF7 cells after 24 hrs by SRB assay	[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	[PMID: 20006519]
MDA-MB-435	GI₅₀	1.95 μM Compound: 4	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	[PMID: 20006519]
MOLT-4	GI₅₀	3.6 μM Compound: 4	Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay Growth inhibition of human MOLT4 cells after 48 hrs by SRB assay	[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	[PMID: 20006519]
NCI-H226	GI₅₀	4.14 μM Compound: 4	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	[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	[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	[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	[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	[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	Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay Growth inhibition of human SKOV3 cells after 48 hrs by SRB assay	[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	[PMID: 20006519]
SNB-19	GI₅₀	< 0.01 μM Compound: 4	Growth inhibition of human SNB19 cells after 48 hrs by SRB assay Growth inhibition of human SNB19 cells after 48 hrs by SRB assay	[PMID: 20006519]
SR	GI₅₀	2.18 μM Compound: 4	Growth inhibition of human SR cells after 48 hrs by SRB assay Growth inhibition of human SR cells after 48 hrs by SRB assay	[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	[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	[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	[PMID: 20006519]
UACC-62	GI₅₀	0.034 μM Compound: 4	Growth inhibition of human UACC62 cells after 48 hrs by SRB assay Growth inhibition of human UACC62 cells after 48 hrs by SRB assay	[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]

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.

1215281-19-8

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
10 mM	0.2687 mL	1.3434 mL	2.6869 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

Purity: 99.54%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) LCMS (94 KB)

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

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

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.

Keywords:

YK-3-2371215281-19-8SirtuinMutantp53mtp53deacetylationtriple-negativebreastcancerTNBCInhibitorinhibitorinhibit

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Complete Stock Solution Preparation Table

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