Art. -Nr.: HY-14507

YK-4-279

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

YK-4-279 blocks RNA Helicase A (RHA) binding with EWS-FLI1 (oncogenic protein). YK-4-279 induces apoptosis and shows anti-proliferation activities towards various cancer cells. YK-4-279 has a chiral center and it can be separated into two enantiomers. YK-4-279 can be used for the research of cancer.

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Reinheit: 99.91%
CAS. Nr.: 1037184-44-3
Formel: C₁₇H₁₃Cl₂NO₄
Molecular Weight:366.20

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

YK-4-279 Chemical Structure

CAS. Nr.: 1037184-44-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Helicase

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	0.35 μM Compound: YK-4-279	Inhibition of transcriptional activity of full-length EWS-FLI1 (unknown origin) expressed in COS7 cells by NR0B1-luciferase reporter gene assay Inhibition of transcriptional activity of full-length EWS-FLI1 (unknown origin) expressed in COS7 cells by NR0B1-luciferase reporter gene assay	[PMID: 25432018]
PANC-1	GI₅₀	>10 μM Compound: YK-4-279	Growth inhibition of human PANC1 cells after 3 days by WST1 assay Growth inhibition of human PANC1 cells after 3 days by WST1 assay	[PMID: 25432018]
TC-32	GI₅₀	0.94 μM Compound: YK-4-279	Growth inhibition of human TC32 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay Growth inhibition of human TC32 cells harboring EWS-FLI1 fusion protein after 3 days by WST1 assay	[PMID: 25432018]

In Vitro

YK-4-279 (3-30 μM; overight) dissociates EWS-FLI1 from RHA in Ewing’s sarcoma family tumor (ESFT) cells^[1].
YK-4-279 (3-30 μM; 14 h) nearly eliminates cyclin D1 in TC32 cells^[1].
YK-4-279 (3-30 μM; 72 h) potently and specifically inhibits ESFTs^[1].
YK-4-279 (50 μM; 6 h) induces substantial apoptosis of ESFT cells^[1].
YK-4-279 (0.1-30 μM; 72 h) inhibits the growth of ESFT, prostate, breast and pancreatic cancer cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

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.

Apoptosis Analysis^[1]

Cell Line:

TC32, HEK, HEC and HFK cell lines
Concentration:

50 µM
Incubation Time:

6 h
Result:

Induced apoptosis of ESFT cells and increased caspase-3 activity.

Cell Viability Assay^[2]

Cell Line:

TC32, TC71, RDES, SKES, MMH-ES-1, STA-ET 7.2, A4573, PC3, MCF7, MDA-MB-231, PANC1 and ASPC1cell lines
Concentration:

0.1-30 µM
Incubation Time:

72 h
Result:

Inhibited cell growth with IC₅₀s of 0.94, 1.83, 1.03, 0.33, 0.94, 0.60, 1.46, 4.95, 22.82, 0.82, 1.514 and 14.28 µM for TC32, TC71, RDES, SKES, MMH-ES-1, STA-ET 7.2, A4573, PC3, MCF7, MDA-MB-231, PANC1 and ASPC1 cells, respectively.

In Vivo

YK-4-279 (1.5 mg; i.p. once) inhibited ESFT tumor growth^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Beige mice with orthotopic ESFT and ESFT xenografts^[1]
Dosage:

1.5 mg
Administration:

Intraperitoneal injection; 1.5 mg once
Result:

Effectively redeced tumor volume of CHP100 and ESFT xenografts (TC71 and CHP100).

Chemical Information

CAS. Nr. 1037184-44-3
Appearance Solid
Molecular Weight 366.20
Formel C₁₇H₁₃Cl₂NO₄
Color White to off-white
SMILES

ClC1=C2C(C(O)(CC(C3=CC=C(OC)C=C3)=O)C(N2)=O)=C(Cl)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

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Journal Impact Factor

Nat Cell Biol

Tumour microenvironment programming by an RNA-RNA-binding protein complex creates a druggable vulnerability in IDH-wild-type glioblastoma. [Abstract]

2024 Jun;26(6):1003-1018. PMID: 38858501
Cancer Lett

High-content drug screening in zebrafish xenografts reveals high efficacy of dual MCL-1/BCL-XL inhibition against Ewing sarcoma. [Abstract]

2023 Feb 1:554:216028. PMID: 36462556
NPJ Precis Oncol

Refined high-content imaging-based phenotypic drug screening in zebrafish xenografts. [Abstract]

2023 May 18;7(1):44. PMID: 37202469
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
Int J Med Sci

The Effects and Mechanism of YK-4-279 in Combination with Docetaxel on Prostate Cancer. [Abstract]

2017 Apr 7;14(4):356-366. PMID: 28553168

YK-4-279 purchased from MedChemExpress. Usage Cited in: Int J Med Sci. 2017 Apr 7;14(4):356-366. [Abstract]

Effects of Docetaxel and YK-4-279 alone or in combination on the levels of ETV1, AR, PSA, p-STAT3, survivin, Bcl-2 and p-Akt in LNCaP and PC-3 cells. LNCaP and PC-3 cells are cultured at a density of 1 × 10⁵ cells/mL in 100 mm tissue culture dishes (10 mL/dish) for 24 h. The cells are then treated with Docetaxel (0.5 nM) and YK-4-279(0.5 µM) alone or in combination for 24 h (for analysis of p-Akt, survivin, PSA, p-STAT3 and AR) and 48 h (for analysis of Bcl-2). The levels of AR,Bcl-2,
bioRxiv

2025 Sep 20.
Research Square Preprint

2023 May 31.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (68.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (6.83 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.83 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.83 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Erkizan HV, et al. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. Nat Med. 2009 Jul;15(7):750-6. [Content Brief]

[2]. Barber-Rotenberg JS, et al. Single enantiomer of YK-4-279 demonstrates specificity in targeting the oncogene EWS-FLI1. Oncotarget. 2012 Feb;3(2):172-82. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7307 mL	13.6537 mL	27.3075 mL	68.2687 mL
	5 mM	0.5461 mL	2.7307 mL	5.4615 mL	13.6537 mL
	10 mM	0.2731 mL	1.3654 mL	2.7307 mL	6.8269 mL
	15 mM	0.1820 mL	0.9102 mL	1.8205 mL	4.5512 mL
	20 mM	0.1365 mL	0.6827 mL	1.3654 mL	3.4134 mL
	25 mM	0.1092 mL	0.5461 mL	1.0923 mL	2.7307 mL
	30 mM	0.0910 mL	0.4551 mL	0.9102 mL	2.2756 mL
	40 mM	0.0683 mL	0.3413 mL	0.6827 mL	1.7067 mL
	50 mM	0.0546 mL	0.2731 mL	0.5461 mL	1.3654 mL
	60 mM	0.0455 mL	0.2276 mL	0.4551 mL	1.1378 mL

Keywords

YK-4-279

7 Cited Publications

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YK-4-279

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Pancreatic Cancer Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Cell Death Library

MCE Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) YK-4-279

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YK-4-279

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Pancreatic Cancer Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Cell Death Library

MCE Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) YK-4-279

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (7)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YK-4-279 Related Classifications

HY-14507 Related Classifications