MYCi361

For research use only.

Catalog No.S8905 Synonyms: NUCC-0196361

1 publication

MYCi361 Chemical Structure

CAS No. 2289690-31-7

MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.

Selleck's MYCi361 has been cited by 1 publication

Purity & Quality Control

Choose Selective Myc Inhibitors

Biological Activity

Description MYCi361 is a MYC inhibitor that engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 binds to MYC with Kd of 3.2 μM. MYCi361 suppresses in vivo tumor growth, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.
Targets
MYC [1]
(Cell-free assay)
3.2 μM(Kd)
In vitro

MYCi361 engages MYC inside cells, disrupts MYC/MAX dimers, and impairs MYC-driven gene expression. MYCi361 enhances MYC phosphorylation on threonine-58, consequently increasing proteasome-mediated MYC degradation.[1]

In vivo

MYCi361 suppresses in vivo tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: MycCaP, PC3, LNCaP, PC12, MV411, SK-N-BE (2), 293T, P493-6 B cells, LLC1, TGR-1, HO15.19 Rat-1 cells
  • Concentrations: 4 μM
  • Incubation Time: 72 h
  • Method:

    Immunogenic Cell Death Assays: MycCaP cells are treated with 4 μM MYCi361 for 72 hr, and supernatants are collected. Cell counts are performed for quantifying secreted ATP and high mobility group protein B1 (HMGB1). For detection of surface Calreticulin, cells are incubated with rabbit anti-Calreticulin for 60 min and then incubated with Alexa Flour 488 anti-rabbit secondary antibody, and analyzed by flow cytometry.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 6-8 week old FVB mice, prostate PDX model, NSG mice, C57BL/6 mice, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1 mice
  • Dosages: 55 mg/kg, 50 mg/kg
  • Administration: IP, Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (168.1 mM)
Ethanol 14 mg/mL (23.53 mM)
Water 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.

Chemical Information

Molecular Weight 594.86
Formula

C26H16ClF9N2O2

CAS No. 2289690-31-7
Storage powder
in solvent
Synonyms NUCC-0196361
Smiles CN1C(=CC(=N1)C(F)(F)F)C2=C(C(=C(C=C2)OCC3=CC=C(C=C3)Cl)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)O

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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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Myc Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID