10058-F4

Catalog No.S7153

10058-F4 Chemical Structure

Molecular Weight(MW): 249.35

10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression.

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USD 170 In stock
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Cited by 12 Publications

7 Customer Reviews

  • Immunoblot analysis of HER2, P-AKT, and HOXB7 in BT474 cells after treatment with 10 µM 10058-F4, 100 µg/ml of trastuzumab, or a combination of 10058-F4 and trastuzumab.

    Cancer Discov, 2015, 5(9): 944-59. 10058-F4 purchased from Selleck.

    E, qPCR analysis and Western blotting of ABCG2 expression in CNE2 cells stably expressing RARS-MAD1L1 or pBabe (vector) after treatment with 10058-F4 or DMSO.

    Clin Cancer Res, 2018, 24(3):659-673. 10058-F4 purchased from Selleck.

  • qPCR analysis and Western blotting of ABCG2 expression in CNE2 cells stably expressing RARS-MAD1L1 or pBabe (vector) after treatment with 10058-F4 or DMSO.

    Clin Cancer Res, 2018, 24(3):659-673. 10058-F4 purchased from Selleck.

    Comparison of the levels of Ncl, Ezh2, Suz12, Jarid2 and H3K27me3 (C) between BrafV600E mice treated with 10058-F4 (n=3) and vehicle (n=3), respectively. DMSO was used as the vehicle control. The insert shows the magnified image of the area indicated by the red square. Scale bars, 200 μm.

    Theranostics, 2017, 7(7):2092-2107. 10058-F4 purchased from Selleck.

  • Schematic diagram represented the regulatory region of PCYT1A promoter (upper panel). The activity of MYC binding to the PCYT1A promoter was measured by chromatin immunoprecipitation assay in DB cells either treated with 10058-F4 (40 μm) for 48 h or transfected with MYC siRNA. DNA–protein complexes from DB cells were precipitated with anti-MYC antibody and amplified with primers amplifying MYC binding sites on PCYT1A promoter using PCR and quantitative real-time PCR (lower panel). Antibody against RNA Polymerase II was referred as positive control. Nonspecific IgG was referred as negative control.

    Blood Cancer J, 2017, doi:10.1038/bcj.2017.61. 10058-F4 purchased from Selleck.

    B-lymphoma cell line DB was either treated with 10058-F4 (40 μM) for 48 h or transfected with MYC siRNA. Expression of Choline, PC(16:0/22:6), LPC(16:0) and LPC(18:0) were detected by UPLC-triple quadrupole mass spectrometry.

    Blood Cancer J, 2017, doi:10.1038/bcj.2017.61. 10058-F4 purchased from Selleck.

  • NHEJ assay in MOLM14 cells treated with either DMSO or 30 µmol/L c-MYC inhibitor 10058-F4 (MYCi). Top, representative agarose gel of PCR products of plasmid DNA isolated from DMSO- or 10058-F4 (MYCi)-treated cells. Bottom, graphical representation of the size of deletions determined by sequencing of the repair junctions in individual plasmid DNAs represented by symbols.

    Mol Cancer Res, 2015, 13(4): 699-712 . 10058-F4 purchased from Selleck.

Purity & Quality Control

Choose Selective c-Myc Inhibitors

Biological Activity

Description 10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression.
Targets
c-Myc [1]
(Cell-free assay)
In vitro

10058-F4 inhibits growth of leukemic cells and dimerization of Myc and Max. 10058-F4 induces cell-cycle arrest and apoptosis of AML cells. 10058-F4 arrests AML cells at G0/G1 phase, downregulates c-Myc expression and upregulated CDK inhibitors, p21 and p27. Meanwhile, 10058-F4 induces apoptosis through activation of mitochondrial pathway shown by downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, and cleavage of caspase 3, 7, and 9. Furthermore, 10058-F4 also induces myeloid differentiation, possibly through activation of multiple transcription factors. Similarly, 10058-F4-induced apoptosis and differentiation could also be observed in primary AML cells. [1] 10058-F4 decreases c-Myc protein levels, inhibites proliferation of HepG2 cells likely through upregulation of cyclin-dependent kinase (cdk) inhibitor, p21WAF1 and lowers intracellular levels of [alpha]-fetoprotein (AFP). Treatment with 10058-F4 also downregulates human telomerase reverse transcriptase (hTERT) at the transcriptional level. In addition to inhibiting the proliferation of HepG2 cells, 10058-F4 enhances sensitivity to conventional chemotherapeutic agents, doxorubicin, 5-fluorouracil (5-FU) and cisplatin. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
REH MVfGeY5kfGmxbjDhd5NigQ>? MkPlNE01ODEkgJpCuW0> NX60[FVEPDhiaB?= MWLy[YR2[2WmIITo[UBu\XSjYn;sbYMh[WO2aY\peJktKEmFNUC9OFAxKM7:TR?= MnHTN|A6PTd{N{O=
Nalm-6 MUXGeY5kfGmxbjDhd5NigQ>? MUWwMVQxOOLCidM1US=> M4[yXVQ5KGh? NUT0V4ZGemWmdXPl[EB1cGVibXX0ZYJwdGmlIHHjeIl3cXS7LDDJR|UxRTR|MDFOwG0> NXTXfWNKOzB7NUeyO|M>
Jurkat MofTSpVv[3Srb36gZZN{[Xl? NVTZdVFpPjBizszN M33HSVI1KGh? MXPjMW16[yCneIDy[ZN{cW:wIHzleoVteyC2cnXheIVlKHerdHigWnBCKChyLDCwMlgh[W6mIEGuOkBuVSliY3;tZolv\WRid3n0bEA3OCEQvF2gNVAxPThvRkSg[IVkemWjc3XkJIZ2enSqZYKgZ49ueGG{ZXSge4l1cCC2aHWgZ49zemW|cH;u[Ilv\yClb370do9tew>? MXeyOVEzODd{Mx?=
CCRF-CEM NH;6cXZHfW6ldHnvckBie3OjeR?= MXe2NEDPxE1? NX3Nd3FvOjRiaB?= MVvjMW16[yCneIDy[ZN{cW:wIHzleoVteyC2cnXheIVlKHerdHigWnBCKChyLDCwMlgh[W6mIEGuOkBuVSliY3;tZolv\WRid3n0bEA3OCEQvF2gNVAxPThvRkSg[IVkemWjc3XkJIZ2enSqZYKgZ49ueGG{ZXSge4l1cCC2aHWgZ49zemW|cH;u[Ilv\yClb370do9tew>? NFfwWVgzPTF{MEeyNy=>
HL-60 MX7GeY5kfGmxbjDhd5NigQ>? NV\5ZoFLPjBiYX7kJFExOCEQvF2= NWPhNm1rOjRiaH;1dpM> MUjk[YNz\WG|ZXSgcIV3\Wy|IH;mJIMuVXmlIIDyc5RmcW6| MoruNVcxPDZ3Nke=
U937 M13yOGZ2dmO2aX;uJIF{e2G7 NETFTHo3OCCjbnSgNVAxKM7:TR?= NFTxPJIzPCCqb4Xydy=> Mne4[IVkemWjc3XkJIxmfmWuczDv[kBkNU27YzDwdo91\Wmwcx?= M1W0VlE4ODR4NU[3
NB4 MVzGeY5kfGmxbjDhd5NigQ>? M3v5cFYxKGGwZDCxNFAh|ryP M1XFeFI1KGixdYLz NWDTWmtw\GWlcnXhd4VlKGyndnXsd{Bw\iClLV35Z{Bxem:2ZXnudy=> NXixcolvOTdyNE[1Olc>

... Click to View More Cell Line Experimental Data

In vivo Peak plasma 10058-F4 concentrations of approximately 300 μM are seen at 5 min and declined to below the detection limit at 360 min following a single iv dose. Plasma concentration versus time data are best approximated by a two-compartment, open, linear model. The highest tissue concentrations of 10058-F4 are found in fat, lung, liver, and kidney. Peak tumor concentrations of 10058-F4 are at least tenfold lower than peak plasma concentrations. Eight metabolites of 10058-F4 are identified in plasma, liver, and kidney. The terminal half-life of 10058-F4 is approximately 1 h, and the volume of distribution is >200 ml/kg. No significant inhibition of tumor growth is seen after i.v. treatment of mice with either 20 or 30 mg/kg 10058-F4.[3]

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HL-60, U937, and NB-4 cells
  • Concentrations: 0, 30, 60, 90, 120, 150 μM
  • Incubation Time: 72 h
  • Method:

    Cells, plated in 96-well plates (105/mL for cell lines and 5 × 105/mL for primary leukemic cells), are treated in triplicate with indicated concentrations of 10058-F4. At various time points, 20 μL 5 mg/mL MTT is added to each well. After incubation at 37°C for 3 hours, the MTT medium is removed and 100 μL DMSO lysis buffer is added. The number of viable cells is assessed by the percentage of absorbance of treated cells relative to that of solvent controls, using 570-nm wavelength on a spectrophotometer.


    (Only for Reference)
Animal Research:

[3]

+ Expand
  • Animal Models: PC-3 and DU145 xenografted SCID mice
  • Formulation: --
  • Dosages: 20 or 30 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 49 mg/mL (196.51 mM)
Ethanol 4 mg/mL (16.04 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+corn oil
For best results, use promptly after mixing.
10mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 249.35
Formula

C12H11NOS2

CAS No. 403811-55-2
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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c-Myc Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID