Home Cell Cycle Myc inhibitor - Apoptosis related activator - Autophagy modulator 10058-F4 For research use only.

10058-F4

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

10058-F4 Chemical Structure

CAS No. 403811-55-2

Purity & Quality Control

10058-F4 Related Products

Signaling Pathway

Myc Signaling Pathways

Myc Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
REH Function assay 0-400 µM 48 h reduced the metabolic activity, IC50=400 μM 30957273
Nalm-6 Function assay 0-400 µM 48 h reduced the metabolic activity, IC50=430 μM 30957273
Jurkat Function assay 60 μM 24 h c-Myc expression levels treated with VPA (0, 0.8 and 1.6 mM) combined with 60 μM 10058-F4 decreased further compared with the corresponding controls 25120723
CCRF-CEM Function assay 60 μM 24 h c-Myc expression levels treated with VPA (0, 0.8 and 1.6 mM) combined with 60 μM 10058-F4 decreased further compared with the corresponding controls 25120723
HL-60 Function assay 60 and 100 μM 24 hours decreased levels of c-Myc proteins 17046567
U937 Function assay 60 and 100 μM 24 hours decreased levels of c-Myc proteins 17046567
NB4 Function assay 60 and 100 μM 24 hours decreased levels of c-Myc proteins 17046567
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
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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
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. [2]
Cell Research 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.
Experimental Result Images Methods Biomarkers Images 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
Growth inhibition assay Cell viability 28861328
In Vivo
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]
Animal Research Animal Models PC-3 and DU145 xenografted SCID mice
Dosages 20 or 30 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 249.35 Formula

C12H11NOS2
CAS No. 403811-55-2 SDF Download 10058-F4 SDF
Smiles CCC1=CC=C(C=C1)C=C2C(=O)NC(=S)S2
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 50 mg/mL ( (200.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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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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