1. Apoptosis
  2. c-Myc
  3. MYC-IN-4

MYC-IN-4 is a MYC inhibitor. MYC-IN-4 impairs MYC/MAX protein-protein interaction (IC50 = 3.06 μM). MYC-IN-4 inhibits MYC-aberrant PC-3 prostate cancer cells with an IC50 of 0.440 μM. MYC-IN-4 demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts. MYC-IN-4 can be used for the study of prostate cancer.

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MYC-IN-4

MYC-IN-4 Chemical Structure

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Description

MYC-IN-4 is a MYC inhibitor. MYC-IN-4 impairs MYC/MAX protein-protein interaction (IC50 = 3.06 μM). MYC-IN-4 inhibits MYC-aberrant PC-3 prostate cancer cells with an IC50 of 0.440 μM. MYC-IN-4 demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts. MYC-IN-4 can be used for the study of prostate cancer[1].

In Vitro

MYC-IN-4 (Compound 15) exhibits potent antiproliferative activity against PC-3 cells (MYC-aberrant prostate cancer cells), with an IC50 value of 0.440 μM[1].
MYC-IN-4 (68 h) shows broad-spectrum antiproliferative activity against 14 other neoplastic cell lines, including MDA-MB-231, HCT-116, Myc-CaP, LN-CaP, NCI-H1581, A549, SK-N-BE, SK-OV-3, HepG-2, A-204, A-431, MG-63, LP-1, and MV4-11 cells, with IC50 values ranging from 0.331 μM to 2.60 μM[1].
MYC-IN-4 (10 μM, 1 h) significantly impairs MYC/MAX protein-protein interaction (PPI) in PC-3 cells via Co-IP assay[1].
MYC-IN-4 (0.1-100 μM, 2 h) inhibits MYC/MAX PPI in a cell-free AlphaLISA assay, with an IC50 value of 3.06 μM[1].
MYC-IN-4 (10 μM, 1 h) reduces the thermal stability of endogenous MYC in PC-3 cells[1].
MYC-IN-4 (1-10 μM, 24 h) induces concentration-dependent MYC degradation in PC-3 cells[1].
MYC-IN-4 suppresses MYC transcriptional activity in HEK293T cells transfected with E-box luciferase reporter plasmid, with an IC50 value of 0.739 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MYC-IN-4 (Compound 15) (10-50 mg/kg, i.p., every other day, for 16 days) demonstrates potent antitumor efficacy in FVB mice bearing Myc-CaP prostate tumor allografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Myc-CaP cells (1 × 106 in 100 µL total volume) were subcutaneously implanted into the right flanks of 6-week-old male FVB mice to establish MYC-driven prostate tumor allograft models [1]
Dosage: 10, 30, 50 mg/kg
Administration: i.p., QOD for 16 days
Result: Achieved tumor growth inhibition (TGI) rates of 57% and 70% at doses of 30 mg/kg and 50 mg/kg.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Combined with INCB086550 (HY-134884) increased the infiltration of CD8⁺ T cells and CD45⁺ leukocytes in the tumor microenvironment.
Molecular Weight

396.29

Formula

C19H10F6N2O

SMILES

FC(F)(F)C(C=C1)=CC=C1C(O2)=CC3=C2C=CC(C4=CC(C(F)(F)F)=NN4)=C3

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MYC-IN-4
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HY-178045
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