YK-4-279

Alias: YK-4-279; YK-4279; YK4279; YK4-279; YK 4-279; YK 4279

Cat No.:V1436 Purity: ≥98%

COA Product Data Instructions for use SDS

YK-4-279 (YK-4279; YK4279;YK4-279; YK 4-279) is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA) with potential anticancer activity.

YK-4-279 Chemical Structure CAS No.: 1037184-44-3
Product category: DNA(RNA) Synthesis

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

YK-4-279 (YK-4279; YK4279; YK4-279; YK 4-279) is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA) with potential anticancer activity. It blocks the interactions between RHA and ES-FLI1 proteins. In a transgenic mouse model, YK-4-279 effectively counteracts the leukemia caused by EWS-FLI1. Targeting the oncogene EWS-FLI1, YK-4-279 exhibits specificity. By preventing EWS-FLI1 from interacting with RHA in TC32 cells that have EWS-FLI1 present, YK-4-279 reduces the amount of cyclin D. Additionally, YK-4-279 induces apoptosis and selectively inhibits the growth of ESFT cells. Additionally, YK-4-279 reduces cell motility and invasion by blocking the biological activity of ERG and ETV1 in fusion-positive prostate cancer cells.

Biological Activity I Assay Protocols (From Reference)

Targets

TC32 ( IC50 = 0.94 µM ); TC71 ( IC50 = 1.83 µM ); RDES ( IC50 = 1.03 µM ); SKES ( IC50 = 0.33 µM ); MMH-ES-1 ( IC50 = 0.94 µM ); STA-ET 7.2 ( IC50 = 0.60 µM ); A4573 ( IC50 = 1.46 µM ); PC3 ( IC50 = 4.95 µM ); MCF7 ( IC50 = 22.82 µM ); MDA-MB-231 ( IC50 = 0.82 µM ); PANC1 ( IC50 = 1.514 µM ); ASPC1 ( IC50 = 14.28 µM )

ln Vitro

YK-4-279 reduces the amount of cyclin D by preventing EWS-FLI1 from interacting with RHA in TC32 cells that have EWS-FLI1. Additionally, YK-4-279 specifically causes apoptosis and suppresses the growth of ESFT cells.[1] In fusion-positive prostate cancer cells, YK-4-279 also suppresses the biological activity of ERG and ETV1, which further reduces cell invasion and motility.[2]

ln Vivo

YK-4-279 (1.5 mg/dose i.p.) inhibits ESFT xenograft tumor growth in vivo.[1] YK-4-279 specifically inhibits the growth and metastasis of prostate cancer in fusion-positive LNCaP-luc-M6 tumors in a mouse model.[3]

Cell Assay

Cell Line: TC32, ES925, GUES1, TC71, A673, A4573, CHP100, PANC1, ASP1, MCF-7, MDA-MB-231, PC-3, HFK and HEC cell lines
Concentration: 3-30 µM
Incubation Time: 72 h
Result: Inhibited cell growth with IC50s of 900 nM, 1 μM and 8 μM for TC32, ES925 and GUES1 cells, respectively.

Animal Protocol

Dissolved in DMSO; 1.5 mg/dose; i.p. injection

Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts

References

[1]. Nat Med . 2009 Jul;15(7):750-6.

[2]. PLoS One . 2011 Apr 29;6(4):e19343.

[3]. PLoS One . 2014 Dec 5;9(12):e114260.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C17H13CL2NO4

Molecular Weight

366.20

Exact Mass

365.02

Elemental Analysis

C, 55.76; H, 3.58; Cl, 19.36; N, 3.83; O, 17.48

CAS #

1037184-44-3

Related CAS #

1037184-44-3

Appearance

White solid powder

SMILES

COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O

InChi Key

HLXSCTYHLQHQDJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H13Cl2NO4/c1-24-10-4-2-9(3-5-10)13(21)8-17(23)14-11(18)6-7-12(19)15(14)20-16(17)22/h2-7,23H,8H2,1H3,(H,20,22)

Chemical Name

4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one

Synonyms

YK-4-279; YK-4279; YK4279; YK4-279; YK 4-279; YK 4279

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 25~73 mg/mL (68.3~199.3 mM)

Water:<1 mg/mL

Ethanol:51 mg/mL (139.3 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.7307 mL	13.6537 mL	27.3075 mL
	5 mM	0.5461 mL	2.7307 mL	5.4615 mL
	10 mM	0.2731 mL	1.3654 mL	2.7307 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

PLoS One. 2014 Dec 5;9(12):e114260.
PLoS One. 2014 Dec 5;9(12):e114260.