2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis Apoptosis
  4. YK-4-279

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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CAS 番号 : 1037184-44-3

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 74 在庫あり
Solution
10 mM * 1 mL in DMSO USD 74 在庫あり
Solid
5 mg $68 在庫あり
10 mg $106 在庫あり
25 mg $240 在庫あり
50 mg $407 在庫あり
100 mg $600 在庫あり
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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

YK-4-279 関連抗体

Top Publications Citing Use of Products

    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,

    DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    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[1][2].

    IC50 & Target

    Helicase

     

    Cellular Effect
    Cell Line Type Value Description References
    COS-7 IC50
    0.35 3
    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]
    COS-7 IC50
    0.35 3
    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]
    COS-7 IC50
    0.35 3
    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 3
    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]
    PANC-1 GI50
    > 10 3
    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]
    PANC-1 GI50
    > 10 3
    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 3
    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]
    TC-32 GI50
    0.94 3
    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]
    TC-32 GI50
    0.94 3
    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]
    体外実験

    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.

    YK-4-279 関連抗体

    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.
    体内実験

    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).
    分子量

    366.20

    分子式

    C17H13Cl2NO4
    CAS 番号
    Appearance

    Solid

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    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, 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.

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    一般には略語で表示されます：C1V1 = C2V2

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    体内:

    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 (6.83 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.
    • 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.

      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.
    In Vivo Dissolution Calculator
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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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    +
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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.
    純度とドキュメンテーション
    参考文献

    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
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    YK-4-279 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
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    • 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-4-2791037184-44-3DNA/RNA SynthesisApoptosisapoptosisanti-proliferationchiralenantiomerESFTprostatebreastpancreaticmiceInhibitorinhibitorinhibit

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    製品名:
    YK-4-279
    製品番号:
    HY-14507
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