10058-F4

Catalog No.S7153 Batch:S715303

Print

Technical Data

Formula

C12H11NOS2
Molecular Weight 249.35 CAS No. 403811-55-2
Solubility (25°C)* In vitro DMSO 50 mg/mL (200.52 mM)
Ethanol 11 mg/mL (44.11 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]
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 Assay:

[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 Study:

[3]
  • Animal Models

    PC-3 and DU145 xenografted SCID mice

  • Dosages

    20 or 30 mg/kg

  • Administration

    i.v.

Customer Product Validation

Data from [Data independently produced by , , Cancer Discov, 2015, 5(9): 944-59]

Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(3):659-673]

Data from [Data independently produced by , , Clin Cancer Res, 2018, 24(3):659-673]

Data from [Data independently produced by , , Theranostics, 2017, 7(7):2092-2107]

Selleck's 10058-F4 has been cited by 103 publications

An iron rheostat controls hematopoietic stem cell fate [ Cell Stem Cell, 2024, S1934-5909(24)00041-9] PubMed: 38402617
VAV2 orchestrates the interplay between regenerative proliferation and ribogenesis in both keratinocytes and oral squamous cell carcinoma [ Sci Rep, 2024, 14(1):4060] PubMed: 38374399
USP13 drives lung squamous cell carcinoma by switching lung club cell lineage plasticity [ Mol Cancer, 2023, 22(1):204] PubMed: 38093367
ESRRB Inhibits the TGFβ Signaling Pathway to Drive Cell Proliferation in Cervical Cancer [ Cancer Res, 2023, 83(18):3095-3114] PubMed: 37350664
Dose-dependent expression of GFI1 alters metabolism in the haematopoietic progenitors and MLL::AF9-induced leukaemic cells [ Br J Haematol, 2023, 10.1111/bjh.18939] PubMed: 37423893
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
The ABL-MYC axis controls WIPI1-enhanced autophagy in lifespan extension [ Commun Biol, 2023, 6(1):872] PubMed: 37620393
ATAD2 promotes glycolysis and tumor progression in clear cell renal cell carcinoma by regulating the transcriptional activity of c-Myc [ Discov Oncol, 2023, 14(1):79] PubMed: 37233956
Chemical-induced chromatin remodeling reprograms mouse ESCs to totipotent-like stem cells [ Cell Stem Cell, 2022, S1934-5909(22)00010-8] PubMed: 35143761

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.