10058-F4

Catalog No.S7153

For research use only.

10058-F4 is a c-Myc inhibitor that specificallly inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.

10058-F4 Chemical Structure

CAS No. 403811-55-2

Selleck's 10058-F4 has been cited by 80 publications

Purity & Quality Control

Choose Selective 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. 10058-F4 promotes a caspase-3-dependent apoptosis and modulates autophagy.
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 MV3GeY5kfGmxbjDhd5NigQ>? M2j4U|AuPDBy4pEJxtVO MYC0PEBp Ml76doVlfWOnZDD0bIUhdWW2YXLvcIlkKGGldHn2bZR6NCCLQ{WwQVQxOCEQvF2= M2rSTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUW3Nlc{Lz5|MEm1O|I4OzxxYU6=
Nalm-6 M3foXmZ2dmO2aX;uJIF{e2G7 MXOwMVQxOOLCidM1US=> NVfKbIlxPDhiaB?= M{K3TZJm\HWlZXSgeIhmKG2ndHHic4xq[yCjY4Tpeol1gSxiSVO1NF01OzBizszN MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl3N{K3N{c,OzB7NUeyO|M9N2F-
Jurkat MoHVSpVv[3Srb36gZZN{[Xl? M3vPW|YxKM7:TR?= NWr6bYlPOjRiaB?= MWDjMW16[yCneIDy[ZN{cW:wIHzleoVteyC2cnXheIVlKHerdHigWnBCKChyLDCwMlgh[W6mIEGuOkBuVSliY3;tZolv\WRid3n0bEA3OCEQvF2gNVAxPThvRkSg[IVkemWjc3XkJIZ2enSqZYKgZ49ueGG{ZXSge4l1cCC2aHWgZ49zemW|cH;u[Ilv\yClb370do9tew>? NYfIVIhjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWxNlA4OjNpPkK1NVIxPzJ|PD;hQi=>
CCRF-CEM NFm5b2RHfW6ldHnvckBie3OjeR?= NF7pSlQ3OCEQvF2= MVqyOEBp M{PPW4MuVXmlIHX4dJJme3Orb36gcIV3\Wy|IITy[YF1\WRid3n0bEBXWEFiKECsJFAvQCCjbnSgNU43KG2PKTDjc41jcW6nZDD3bZRpKDZyIN88UUAyODB3OD3GOEBl\WO{ZXHz[YQh\nW{dHjldkBkd22yYYLl[EB4cXSqIITo[UBkd3K{ZYPwc45lcW6pIHPvcpRzd2y| M1jFO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MUKwO|I{Lz5{NUGyNFczOzxxYU6=
HL-60 M{PBT2Z2dmO2aX;uJIF{e2G7 NHrUboo3OCCjbnSgNVAxKM7:TR?= MU[yOEBpd3W{cx?= NU[wSm4z\GWlcnXhd4VlKGyndnXsd{Bw\iClLV35Z{Bxem:2ZXnudy=> NFLnfow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{C0OlU3Pyd-MUewOFY2Pjd:L3G+
U937 NH;QepdHfW6ldHnvckBie3OjeR?= MoPLOlAh[W6mIEGwNEDPxE1? Ml;WNlQhcG:3coO= NUXySo9z\GWlcnXhd4VlKGyndnXsd{Bw\iClLV35Z{Bxem:2ZXnudy=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzB2NkW2O{c,OTdyNE[1Olc9N2F-
NB4 NHf1doJHfW6ldHnvckBie3OjeR?= MWS2NEBidmRiMUCwJO69VQ>? MkLLNlQhcG:3coO= Moji[IVkemWjc3XkJIxmfmWuczDv[kBkNU27YzDwdo91\Wmwcx?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzB2NkW2O{c,OTdyNE[1Olc9N2F-
NB1643 MVLxTHRUKGG|c3H5 M1rKSJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NVXQV2xuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-EGFR / HIF-1α / c-Myc / Glut-1 ; Cyclin D2 / Cyclin D3 / p-21 / c-Myc / p-AKT / AKT ; PARP / Caspase-3 / Myc 30967777 28861328 25793663
Growth inhibition assay Cell viability 28861328
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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[3]

  • Animal Models: PC-3 and DU145 xenografted SCID mice
  • Dosages: 20 or 30 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

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.

0.312mg/mL

Chemical Information

Molecular Weight 249.35
Formula

C12H11NOS2

CAS No. 403811-55-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=CC=C(C=C1)C=C2C(=O)NC(=S)S2

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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.

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Molarity Calculator

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Tech Support

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.

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