[CAS NO. 581073-80-5] KJPyr9
PRODUCTS SPECIFICATIONS [581073-80-5]
DESCRIPTION [581073-80-5]
Overview
| MDL | MFCD29081199 |
|---|---|
| Molecular Weight | 385.37 |
| Molecular Formula | C22H15N3O4 |
| SMILES | O=C(N)C1=CC=C(C2=CC(C3=CC=CO3)=NC(C4=CC=C([N+]([O-])=O)C=C4)=C2)C=C1 |
2 Publications Citing Use of MCE
Summary
KJ Pyr 9 is an inhibitor of MYC with a K d of 6.5 nM in in vitro assay.
IC50 & Target
Kd: 6.5±1.0 nM (MYC) [1]
In Vitro
KJ Pyr 9 (KJ-Pyr-9) interferes with MYC-MAX complex formation in the cell, as shown in a protein fragment complementation assay. KJ Pyr 9 specifically inhibits MYC-induced oncogenic transformation in cell culture; it has no or only weak effects on the oncogenic activity of several unrelated oncoproteins. KJ Pyr 9 preferentially interferes with the proliferation of MYC-overexpressing human and avian cells and specifically reduces the MYC-driven transcriptional signature. KJ Pyr 9 against three cell lines is tested known to be dependent on increased MYC activity: NCI-H460, MDA-MB-231, and SUM-159PT. The proliferation of all cell lines tested is inhibited, with IC 50 values between 5 and 10 μM. Additionally, the proliferation of Burkitt lymphoma cell lines, which show constitutively high expression of c-MYC, is more sensitive to KJ Pyr 9 (IC 50 values between 1 and 2.5 μM) [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
To test the in vivo effectiveness of KJ Pyr 9 (KJ-Pyr-9), nude mice receive a xenograft of MDA-MB-231 cells suspended in Matrigel and injected s.c. into the left and right flanks. When the tumors have reached an average volume of 100 mm 3 , mice are treated daily with 10 mg/kg KJ Pyr 9 or vehicle control by i.p. injection for 31 d. Inhibition of tumor growth by KJ Pyr 9 is noted after 8 d of treatment. By day 31, the tumor volume in the KJ Pyr 9-treated animals has not increased significantly. At the conclusion of the experiment the tumors are extracted and weighed. The weight measurements are in agreement with the volume determinations and confirmed the ability of KJ Pyr 9 to halt tumor growth [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 125 mg/mL ( 324.36 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5949 mL | 12.9745 mL | 25.9491 mL |
| 5 mM | 0.5190 mL | 2.5949 mL | 5.1898 mL |
| 10 mM | 0.2595 mL | 1.2975 mL | 2.5949 mL |