Name: YK-4-279
Brand: GlpBio
SKU: GC17386
Availability: InStock
Rating: 5 (30 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

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618, 1017–1023 (2023)

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33, 273–287 (2023)

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33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
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Cancer Cell
39 (2021): 1-16

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30.8 (2022): 1124-1138

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34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
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Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

Cell experiment [1-3]:
Cell lines	VCaP cells, LNCaP cells
Preparation method	The solubility of this compound in DMSO is >16.35 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	10 μM, 48 hr
Applications	YK-4-279 inhibited ERG and ETV1 mediated transcriptional activity. YK-4-279 bound to ERG with an affinity (KD) of 11.7 μM and bound to ETV1 with an affinity of 17.4 μM. In LNCaP cells, YK-4-279 (1 μM) resulted in decreased gene expression of MMP13 without significant reduction in ETV1 levels. In VCaP cells, YK-4-279 (10 μM, 48 hours) decreased expression of PLAU, ADAM19 and PLAT mRNA. YK-4-279 inhibited VCaP (10 μM) and LNCaP (1 μM) cell invasion of HUVECs. YK-4-279 (10 μM) inhibited motility in a scratch assay in high-passage LNCaP cells. YK-4-279 showed anti-proliferative activity with the IC50 values of 1 and 8 μM in primary cell lines ES925 and GUES1. YK-4-279 induced caspase-3 activity in four ESFT cell lines (TC32, A4573, TC71, and ES925). Treatment of TC32, HEK293, HFK, and HEC with short-term (6 hours) high dose (50 μM) YK-4-279 resulted in significant apoptosis of the ESFT cells. In LNCaP-luc-M6 cells, YK-4-279 (1 μM) significantly reduced mRNA levels of several ETV1 target genes, including MMP7, MMP13, FKBP10 and GLYATL2, without affecting the expression of ETV1. YK-4-279 treatment of LNCaP-luc-M6 cells resulted in a significant decrease in cell migration.
Animal experiment [2,3]:
Animal models	SCID/bg mice bearing ESFT (orthotopic) or prostate cancer cell xenograft tumors, SCID/beige mice subcutaneously injected with LNCaP-luc-M6
Dosage form	Intraperitoneal injection, 1.5mg/dose, three times per week; 75 mg/kg YK-4-279 three times a week and 150 mg/kg YK-4-279 five times a week
Application	YK-4-279 (1.5 mg/dose i.p.) inhibited the growth of ESFT xenograft tumors. In SCID/beige mice were subcutaneously injected with LNCaP-luc-M6 cells, YK-4-279 (75 mg/kg YK-4-279 three times a week and 150 mg/kg YK-4-279 five times a week) reduced tumor growth and inhibited lung metastasis. YK-4-279 treatment resulted in decreased gene expression of MMP7, GLYATL2 and FKBP10 in LNCaP-luc-M6 animals.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Rahim S, Beauchamp E M, Kong Y, et al. YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion[J]. PloS one, 2011, 6(4): e19343. [2]. Erkizan H V, Kong Y, Merchant M, et al. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma[J]. Nature medicine, 2009, 15(7): 750-756. [3]. Rahim S, Minas T, Hong S H, et al. A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model[J]. PloS one, 2014, 9(12): e114260.

YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.

EWS-FLI1 is a disordered protein that precludes standard structure-based small-molecule inhibitor design. EWS-FLI1 binding to RNA helicase A (RHA) is important for its oncogenic function.

In vitro: ESFT cells treated with YK-4-279 showed a dissociation of EWS-FLI1 from RHA by 10 mM, consistent with the KD value. The EWS-FLI1–transfected cells showed a dose-dependent decrease in promoter activity when treated for 18 h with 3 mM and 10 mM YK-4-279. YK-4-279 was relatively specific for ESFT cells as compared to the nontransformed HEK293 cells [1].

In vivo: The tumor growth rate of YK-4-279–treated mice bearing CHP-100 was lower than that in mice having PC3 prostate tumors. The cumulative data from five independent experiments with the ESFT xenografts (TC71 and CHP-100) show a marked overall tumor reduction in the YK-4-279–treated mice. Pathological analysis of mice treated with YK-4-279 did not show any signs of toxicity, except for sterile inflammatory lesions in the abdominal cavities of mice [1].

Clinical trial: No clinical data are available currently.

Reference:
[1] Erkizan HV, Kong Y, Merchant M, Schlottmann S, Barber-Rotenberg JS, Yuan L, Abaan OD, Chou TH, Dakshanamurthy S, Brown ML, Uren A, Toretsky JA. A small molecule blocking oncogenic protein EWS-FLI1 interaction with RNA helicase A inhibits growth of Ewing's sarcoma. Nat Med. 2009;15(7):750-6.

Cas No.	1037184-44-3	SDF
Synonyms	YK 4-279
Chemical Name	4,7-dichloro-3-hydroxy-3-[2-(4-methoxyphenyl)-2-oxoethyl]-1H-indol-2-one
Canonical SMILES	COC1=CC=C(C=C1)C(=O)CC2(C3=C(C=CC(=C3NC2=O)Cl)Cl)O
Formula	C₁₇H₁₃Cl₂NO₄	M.Wt	366.2
Solubility	≥ 16.35 mg/mL in DMSO, ≥ 24.25 mg/mL in EtOH with ultrasonic	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		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

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In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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YK-4-279 (Synonyms: YK 4-279)

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