1. Apoptosis
  2. c-Myc
    Apoptosis
  3. MYCMI-6

MYCMI-6 (Synonyms: NSC354961)

Cat. No.: HY-124675 Purity: 95.58%
Handling Instructions

MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.

For research use only. We do not sell to patients.

MYCMI-6 Chemical Structure

MYCMI-6 Chemical Structure

CAS No. : 681282-09-7

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Description

MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis[1].

In Vitro

MYCMI-6 (NSC354961) (6.25 μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy[1].
MYCMI-6 significantly inhibits growth of Burkitt’s lymphoma cells (Mutu, Daudi and ST486) - another classical example of a MYC-driven tumor, having translocations of MYC to one of the immunoglobulin loci - in a dose-dependent manner with an average GI50 of 0.5 μM. Treatment of MCF7 cells with the MYCMI-6 for 24 hours significantly decreased MYC:MAX isPLA signals to 7%. Titration showed an IC50 for inhibition of MYC:MAX of less than 1.5 μM for MYCMI-6 by isPLA. MYCMI-6 inhibits the MYC:MAX heterodimer formation with an IC50 of 3.8 μM. MYCMI-6 efficiently inhibits anchorage-independent growth of MYCN-amplified neuroblastoma cells with GI50 values of <0.4 μM[1].

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

Cell Viability Assay[1]

Cell Line: MYCN-amplified neuroblastoma cells (IMR-32, Kelly and SK-N-DZ), MYCN-non-amplified neuroblastoma cells (SK-N-F1, SK-N-AS and SK-N-RA)
Concentration: 6.25 μM
Incubation Time: 48 hours
Result: Reduced growth of the MYCN-amplified cell lines significantly stronger than the MYCN-non-amplified cell lines.
In Vivo

MYCMI-6 (20 mg/kg; i.p.; daily for 1-2 weeks) induces massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model[1].

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

Animal Model: 6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells)[1]
Dosage: 20 mg/kg body weight
Administration: I.p.; daily for 1-2 weeks
Result: A dramatic increase in the extension of apoptotic areas in the tumors and a significant increase in non-proliferative areas as determined by Ki67 staining in tumors.
Molecular Weight

373.41

Formula

C₂₀H₁₉N₇O

CAS No.

681282-09-7

SMILES

NC1=NC(N)=CC=C1/N=N/C2=CC3=NC4=CC=C(OCC)C=C4C(N)=C3C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (5.36 mM; ultrasonic and adjust pH to 2 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6780 mL 13.3901 mL 26.7802 mL
5 mM 0.5356 mL 2.6780 mL 5.3560 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 95.58%

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Keywords:

MYCMI-6NSC354961MYCMI6MYCMI 6NSC 354961NSC-354961c-MycApoptosisMycMCF7cellslymphomaMYC-driventumorneuroblastomacytotoxicathymicnudemiceInhibitorinhibitorinhibit

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