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10058-F4 Myc inhibitor

Name: 10058-F4
Brand: Selleck Chemicals
SKU: S7153
Availability: InStock
Rating: 5 (110 reviews)

Cat.No.S7153

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

Chemical Structure

Molecular Weight: 249.35

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP (HSP90) PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	10074-G5 MYCi975 MYCi361 EN4 APTO-253

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	249.35	Formula	C₁₂H₁₁NOS₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	403811-55-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC1=CC=C(C=C1)C=C2C(=O)NC(=S)S2

Solubility

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.310mg/ml (1.24mM)	Taking the 1 mL working solution as an example, add 20 μL of 15.6 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	c-Myc ^[1] (Cell-free assay)
In vitro	10058-F4 inhibits growth of leukemic cells and dimerization of Myc and Max. This compound induces cell-cycle arrest and apoptosis of AML cells. It arrests AML cells at G0/G1 phase, downregulates c-Myc expression and upregulated CDK inhibitors, p21 and p27. Meanwhile, this chemical 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, it also induces myeloid differentiation, possibly through activation of multiple transcription factors. Similarly, this compound-induced apoptosis and differentiation could also be observed in primary AML cells. ^[1] It 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 this chemical also downregulates human telomerase reverse transcriptase (hTERT) at the transcriptional level. In addition to inhibiting the proliferation of HepG2 cells, it enhances sensitivity to conventional chemotherapeutic agents. ^[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 this compound are found in fat, lung, liver, and kidney. Peak tumor concentrations of this chemical are at least tenfold lower than peak plasma concentrations. Eight metabolites of this compound are identified in plasma, liver, and kidney. The terminal half-life of this chemical 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 this compound.^[3]
References	https://pubmed.ncbi.nlm.nih.gov/17046567/ https://pubmed.ncbi.nlm.nih.gov/17159602/ https://pubmed.ncbi.nlm.nih.gov/18509642/

Applications

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

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