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KJ Pyr 9

Catalog No. T15665 CAS 581073-80-5

KJ Pyr 9 is an MYC inhibitor (Kd: 6.5 nM in vitro assay).

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KJ Pyr 9, CAS 581073-80-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KJ Pyr 9 is an MYC inhibitor (Kd: 6.5 nM in vitro assay).
Targets&IC50	MYC:(kd)6.5±1.0 nM
In vitro	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 interferes with MYC-MAX complex formation in the cell, as shown in a protein fragment complementation assay. 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. KJ Pyr 9 preferentially interferes with the proliferation of MYC-overexpressing human and avian cells and specifically reduces the MYC-driven transcriptional signature. The proliferation of all cell lines tested is inhibited (IC50s: between 5 and 10 μM). The proliferation of Burkitt lymphoma cell lines, which show constitutively high expression of c-MYC, is more sensitive to KJ Pyr 9 (IC50s: between 1 and 2.5 μM).
In vivo	Nude mice receive a xenograft of MDA-MB-231 cells suspended in Matrigel and injected s.c. into the left and right flanks to test the in vivo effectiveness of KJ Pyr 9 (KJ-Pyr-9). The tumor volume in the KJ Pyr 9-treated animals has not increased significantly, by day 31. The tumors are extracted and weighed, at the conclusion of the experiment. When the tumors have reached an average volume of 100 mm3, 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. The weight measurements are in agreement with the volume determinations and confirmed the ability of KJ Pyr 9 to halt tumor growth.

Molecular Weight	385.37
Formula	C22H15N3O4
CAS No.	581073-80-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (259.49 mM), Need ultrasonic

H2O: < 0.1 mg/mL (insoluble)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KJ Pyr 9 581073-80-5 Autophagy Cell Cycle/Checkpoint c-Myc KJ Pyr9 inhibit Inhibitor Myc KJ Pyr-9 inhibitor

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