Synonym
KJ-Pyr-9; KJPyr-9; KJ Pyr-9; KJ-Pyr9; K JPyr 9; KJ Pyr9.
IUPAC/Chemical Name
4-[2-(2-Furanyl)-6-(4-nitrophenyl)-4-pyridinyl]benzamide
InChi Key
GTTDVYCKFQYVNN-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H15N3O4/c23-22(26)16-5-3-14(4-6-16)17-12-19(15-7-9-18(10-8-15)25(27)28)24-20(13-17)21-2-1-11-29-21/h1-13H,(H2,23,26)
SMILES Code
O=C(N)C1=CC=C(C2=CC(C3=CC=CO3)=NC(C4=CC=C([N+]([O-])=O)C=C4)=C2)C=C1
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
KJ Pyr 9 is an inhibitor of MYC with a Kd of 6.5 nM in in vitro assay.
In vitro activity:
Treatment with KJ-Pyr-9, a specific inhibitor of MYC/NMYC-myc-associated factor X interaction, decreased survival by the induction of apoptosis of both colorectal cancer cell lines.
Reference: Cancers (Basel). 2020 Sep 10;12(9):2582. https://pubmed.ncbi.nlm.nih.gov/32927768/
In vivo activity:
In vivo, KJ-Pyr-9 effectively blocks the growth of a mouse xenotransplant of MYC-amplified human cancer cells.
Reference: Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12556-61. https://pubmed.ncbi.nlm.nih.gov/25114221/
|
Solvent |
mg/mL |
mM |
Solubility |
DMF |
25.0 |
64.87 |
DMF:PBS (pH 7.2) (1:2) |
0.3 |
0.78 |
DMSO |
61.2 |
158.75 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
385.38
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Schulte Am Esch JSA, Windmöller BA, Hanewinkel J, Storm J, Förster C, Wilkens L, Krüger M, Kaltschmidt B, Kaltschmidt C. Isolation and Characterization of Two Novel Colorectal Cancer Cell Lines, Containing a Subpopulation with Potential Stem-Like Properties: Treatment Options by MYC/NMYC Inhibition. Cancers (Basel). 2020 Sep 10;12(9):2582. doi: 10.3390/cancers12092582. PMID: 32927768; PMCID: PMC7564713.
2. Tan Y, Sementino E, Chernoff J, Testa JR. Targeting MYC sensitizes malignant mesothelioma cells to PAK blockage-induced cytotoxicity. Am J Cancer Res. 2017 Aug 1;7(8):1724-1737. PMID: 28861328; PMCID: PMC5574944.
3. Hart JR, Garner AL, Yu J, Ito Y, Sun M, Ueno L, Rhee JK, Baksh MM, Stefan E, Hartl M, Bister K, Vogt PK, Janda KD. Inhibitor of MYC identified in a Kröhnke pyridine library. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12556-61. doi: 10.1073/pnas.1319488111. Epub 2014 Aug 11. PMID: 25114221; PMCID: PMC4151726.
In vitro protocol:
1. Schulte Am Esch JSA, Windmöller BA, Hanewinkel J, Storm J, Förster C, Wilkens L, Krüger M, Kaltschmidt B, Kaltschmidt C. Isolation and Characterization of Two Novel Colorectal Cancer Cell Lines, Containing a Subpopulation with Potential Stem-Like Properties: Treatment Options by MYC/NMYC Inhibition. Cancers (Basel). 2020 Sep 10;12(9):2582. doi: 10.3390/cancers12092582. PMID: 32927768; PMCID: PMC7564713.
2. Tan Y, Sementino E, Chernoff J, Testa JR. Targeting MYC sensitizes malignant mesothelioma cells to PAK blockage-induced cytotoxicity. Am J Cancer Res. 2017 Aug 1;7(8):1724-1737. PMID: 28861328; PMCID: PMC5574944.
In vivo protocol:
1. Hart JR, Garner AL, Yu J, Ito Y, Sun M, Ueno L, Rhee JK, Baksh MM, Stefan E, Hartl M, Bister K, Vogt PK, Janda KD. Inhibitor of MYC identified in a Kröhnke pyridine library. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12556-61. doi: 10.1073/pnas.1319488111. Epub 2014 Aug 11. PMID: 25114221; PMCID: PMC4151726.
1: Tan Y, Sementino E, Chernoff J, Testa JR. Targeting MYC sensitizes malignant
mesothelioma cells to PAK blockage-induced cytotoxicity. Am J Cancer Res. 2017
Aug 1;7(8):1724-1737. eCollection 2017. PubMed PMID: 28861328; PubMed Central
PMCID: PMC5574944.
2: Novel molecule hits key cancer target. Cancer Discov. 2014 Nov;4(11):OF8. doi:
10.1158/2159-8290.CD-NB2014-134. Epub 2014 Sep 4. PubMed PMID: 25367970.
3: Raffeiner P, Röck R, Schraffl A, Hartl M, Hart JR, Janda KD, Vogt PK, Stefan
E, Bister K. In vivo quantification and perturbation of Myc-Max interactions and
the impact on oncogenic potential. Oncotarget. 2014 Oct 15;5(19):8869-78. PubMed
PMID: 25326649; PubMed Central PMCID: PMC4253403.
4: Hart JR, Garner AL, Yu J, Ito Y, Sun M, Ueno L, Rhee JK, Baksh MM, Stefan E,
Hartl M, Bister K, Vogt PK, Janda KD. Inhibitor of MYC identified in a Kröhnke
pyridine library. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12556-61. doi:
10.1073/pnas.1319488111. Epub 2014 Aug 11. PubMed PMID: 25114221; PubMed Central
PMCID: PMC4151726.