MYCMI-6

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.

Product information

CAS Number: 681282-09-7

Molecular Weight: 373.41

Formula: C20H19N7O

Synonym:

NSC354961

Chemical Name: 3-[(E)-2-(9-amino-7-ethoxyacridin-3-yl)diazen-1-yl]pyridine-2, 6-diamine

Smiles: CCOC1=CC2=C(C=C1)N=C1C=C(C=CC1=C2N)/N=N/C1=CC=C(N)N=C1N

InChiKey: QNWGRUNKGVWOTA-CYYJNZCTSA-N

InChi: InChI=1S/C20H19N7O/c1-2-28-12-4-6-15-14(10-12)19(22)13-5-3-11(9-17(13)24-15)26-27-16-7-8-18(21)25-20(16)23/h3-10H,2H2,1H3,(H2,22,24)(H4,21,23,25)/b27-26+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 2.4 mg/mL (6.43 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

MYCMI-6 (NSC354961) (6.25 μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy. 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.

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.

References:

1. Castell A, et al. A selective high affinity MYC-binding compound inhibits MYC:MAX interaction and MYC-dependent tumor cell proliferation. Sci Rep. 2018 Jul 3;8(1):10064.

Products are for research use only. Not for human use.