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Chemical Structure| 403811-55-2 Chemical Structure| 403811-55-2

Structure of 10058-F4
CAS No.: 403811-55-2

Chemical Structure| 403811-55-2

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10058-F4 is a c-Myc inhibitor that disrupts c-Myc-Max dimerization and the transactivation of c-Myc target genes.

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Product Details of 10058-F4

CAS No. :403811-55-2
Formula : C12H11NOS2
M.W : 249.35
SMILES Code : O=C1N=C(S)SC1=CC2=CC=C(CC)C=C2
MDL No. :MFCD04969046

Safety of 10058-F4

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of 10058-F4

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
TMR cells 10 μM Reduced expression of HOXB7, HER2, and ER target genes PMC4560624
BT474 cells 1, 5, 10, 50 μM 48 h Combined with trastuzumab, significantly reduced cell viability PMC4560624
H1299 cells 10 µM 24 h Inhibited MYC expression and increased p21 protein levels PMC8363664
human mammary epithelial cells (hMECs) 10μM To investigate the effect of MYC inhibitor 10058-F4 on miR-18a expression, results showed that 10058-F4 significantly reduced miR-18a expression in hMECs cultured on stiff substrates. PMC3981899
Jurkat cells 5 nM 12 h Inhibited c-Myc expression, reduced GLS1 and GLUD expression, impaired T cell activation and proliferation PMC10131875
intestinal organoids 20 μM or 40 μM 24 h increased the secretion of total GLP-1 and active GLP-1 in response to glucose, along with elevated Gcg mRNA levels PMC9944847
intestinal organoids 40 μM 48 h reduced ceramide production and secretion PMC9944847
DU145 100 nM 48 h To evaluate the effect of MYC inhibitor 10058-F4 on the radiosensitivity of DU145 cells, results showed that 10058-F4 significantly increased the radiosensitivity of DU145 cells. PMC8315064
LNCaP 100 nM 48 h To evaluate the effect of MYC inhibitor 10058-F4 on the radiosensitivity of LNCaP cells, results showed that 10058-F4 had a minor effect on the radiosensitivity of LNCaP cells. PMC8315064
intestinal organoids 20 μM or 40 μM 24 h or 48 h Treatment with 10058-F4 increased Gcg mRNA levels in intestinal organoids and promoted the secretion of total GLP-1 and active GLP-1. PMC9944847

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice BT474 cell xenograft model intraperitoneal injection 30 mg/kg daily, for the duration of the treatment Combined with trastuzumab, significantly inhibited tumor growth PMC4560624
nude mice MDA-MB-231/ADR xenograft model intraperitoneal injection 20 mg/kg every 3 days for 3 weeks The combination of 10058-F4 and DOX significantly slowed down the tumor growth rate in nude mice and reduced the tumor size and weight. PMC9005717
Nile tilapia Bacterial infection model Intraperitoneal injection 10 mg/kg Administered on day 1, 3, 5, and 6 post-infection Inhibited c-Myc expression, reduced GLS1 and GLUD expression, impaired T cell proliferation and cytotoxicity, increased infection mortality PMC10131875
Mice TPO-Cre/LSL-BrafV600E mice Gastric gavage and intraperitoneal injection 30 mg/kg Once daily for 2 weeks To investigate the effect of 10058-F4 on PRC2 components and H3K27me3 levels in BrafV600E-induced thyroid cancer mouse model, the results showed that 10058-F4 significantly reduced tumor volume and weight, and decreased the levels of PRC2 components and H3K27me3 PMC5485424
mice HFD-induced obesity and hepatic steatosis model oral 50 mg/kg daily for 8 weeks improved HFD-induced obesity, insulin resistance, hepatic steatosis and fibrosis, accompanied by increased GLP-1 and decreased ceramide levels in serum PMC9944847
mice high-fat diet-induced obesity and hepatic steatosis model oral 50 mg/kg daily for 8 weeks 10058-F4 treatment reduced and liver weight gain, improved insulin resistance, and reduced hepatic steatosis. PMC9944847

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.01mL

0.80mL

0.40mL

20.05mL

4.01mL

2.01mL

40.10mL

8.02mL

4.01mL

References

 

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