YK-4-279
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.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 1037184-44-3
- Formula: C17H13Cl2NO4
- Molecular Weight:366.20
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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HY-L004
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Transcription Factor-Targeted Library
HY-L090
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Targeted Diversity Library
HY-L099
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Cell Death Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) YK-4-279
More- Nat Cell Biol. 2024 Jun;26(6):1003-1018. [Abstract]
- Cancer Lett. 2023 Feb 1:554:216028. [Abstract]
- NPJ Precis Oncol. 2023 May 18;7(1):44. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Int J Med Sci. 2017 Apr 7;14(4):356-366. [Abstract]
- bioRxiv. 2025 Sep 20.
- Research Square Preprint. 2023 May 31.
Customer Validation & Images
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WB
All DNA/RNA Synthesis Isoforms
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Biological Activity
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Helicase |
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Cell Line
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Type | Value | Description | References |
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| COS-7 | IC50 |
0.35 μM
Compound: YK-4-279
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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
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[PMID: 25432018] |
| PANC-1 | GI50 |
>10 μM
Compound: YK-4-279
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Growth inhibition of human PANC1 cells after 3 days by WST1 assay
Growth inhibition of human PANC1 cells after 3 days by WST1 assay
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[PMID: 25432018] |
| TC-32 | GI50 |
0.94 μM
Compound: YK-4-279
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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
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[PMID: 25432018] |
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.
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Cell Line:TC32, ES925, GUES1, TC71, A673, A4573, CHP100, PANC1, ASP1, MCF-7, MDA-MB-231, PC-3, HFK and HEC cell lines
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Concentration:3-30 µM
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Incubation Time:72 h
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Result:Inhibited cell growth with IC50s of 900 nM, 1 μM and 8 μM for TC32, ES925 and GUES1 cells, respectively.
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Cell Line:TC32, HEK, HEC and HFK cell lines
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Concentration:50 µM
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Incubation Time:6 h
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Result:Induced apoptosis of ESFT cells and increased caspase-3 activity.
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Cell Line:TC32, TC71, RDES, SKES, MMH-ES-1, STA-ET 7.2, A4573, PC3, MCF7, MDA-MB-231, PANC1 and ASPC1cell lines
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Concentration:0.1-30 µM
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Incubation Time:72 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beige mice with orthotopic ESFT and ESFT xenografts[1]
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Dosage:1.5 mg
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Administration:Intraperitoneal injection; 1.5 mg once
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Result:Effectively redeced tumor volume of CHP100 and ESFT xenografts (TC71 and CHP100).
Chemical Information
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CAS No. 1037184-44-3
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Appearance Solid
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Molecular Weight 366.20
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Formula C17H13Cl2NO4
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Color White to off-white
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SMILES
ClC1=C2C(C(O)(CC(C3=CC=C(OC)C=C3)=O)C(N2)=O)=C(Cl)C=C1
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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 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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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
2023 May 18;7(1):44. PMID: 37202469 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Int J Med Sci
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,
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Solvent & Solubility
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)
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.
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.
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 (6.83 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%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 (284 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]. 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]
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, 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 |
YK-4-279 Related Classifications
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