KJ Pyr 9 是 MYC 的抑制剂。体外实验中, KJ Pyr 9 抑制 MYC 的 K_d 值为 6.5±1.0 nM。

KJ Pyr 9 is an inhibitor of MYC with a K d of 6.5 nM in in vitro assay.

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Kd: 6.5±1.0 nM (MYC)

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 IC50 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 (IC50 values between

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hart JR, et al. Inhibitor of MYC identified in a Kr?hnke pyridine library. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12556-61.

In Vitro: DMSO : 125 mg/mL (324.36 mM; Need ultrasonic)配制储备液