| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
MYC (c-MYC) oncoprotein. KJ-Pyr-9 suppresses the formation of MYC-MAX heterodimers. The compound inhibits MYC-driven oncogenic transformation. MYC is a transcription factor that regulates cell proliferation, growth, and apoptosis.
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| ln Vitro |
In protein fragment complementation tests, KJ Pyr 9 (KJ-Pyr-9) induces disruptions in the MYC-MAX complex in cells [1]. KJ Pyr 9 had little influence on the food activity of a few unrelated oncoproteins and only mild effects on MYC-induced inducible transformation in suspension in cells [1]. MYC-overexpressing human and avian cell proliferation is preferentially inhibited by KJ Pyr 9, which also dramatically lowers the MYC-driven opsonic signature [1]. Increased MYC activity is required for KJ Pyr 9's recognized effects on the clear cell lines NCI-H460, MDA-MB-231, and SUM-159PT [1]. All cell lines having IC50 values between 5 and 10 μM are included in KJpyr 9. Burkitt cell lines with constitutively high c-MYC expression (IC50 values between 1 and 2.5 μM) are more sensitive to KJ Pyr 9 proliferation [1].
KJ-Pyr-9 binds to MYC with a Kd value of 6.5 ± 1.0 nM as determined by back-scattering interferometry. It inhibits the proliferation of all cell lines with IC50 values between 5 and 10 µM. Burkitt lymphoma cell lines with constitutively high c-MYC expression show greater sensitivity with IC50 values between 1 and 2.5 µM. |
| ln Vivo |
Growth inhibition is a property of KJ Pyr 9 (intraperitoneal injection; 10 mg/kg; once day for 31 tumor days) [1].
No detailed in vivo activity data has been published in the available literature. KJ-Pyr-9 is primarily characterized as an in vitro tool for studying MYC function. Further in vivo studies in xenograft tumor models would be needed to evaluate its anti-tumor efficacy, pharmacokinetics, and pharmacodynamics. |
| Enzyme Assay |
MYC-MAX binding assay: MYC and MAX proteins (or their bHLH-LZ domains) are incubated with varying concentrations of KJ-Pyr-9 in binding buffer. The interaction is measured by back-scattering interferometry, surface plasmon resonance, or fluorescence polarization. Kd values are calculated from binding curves.
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| Cell Assay |
Cell proliferation assay: Cancer cell lines (including Burkitt lymphoma and other cancer cell lines) are seeded in 96-well plates and treated with KJ-Pyr-9 at varying concentrations (0.1-50 µM) for 48-72 hours. Cell viability is measured using MTT, CellTiter-Glo, or counting of viable cells. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
No in vivo animal experimental protocols have been published for KJ-Pyr-9 in the available literature. In vivo studies would typically involve xenograft tumor models in immunocompromised mice bearing MYC-driven tumors. KJ-Pyr-9 would be administered via intraperitoneal or intravenous routes, followed by tumor volume measurement, survival analysis, and histopathological evaluation.
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| ADME/Pharmacokinetics |
No pharmacokinetic data has been published in the available literature. KJ-Pyr-9 has a molecular formula and weight consistent with small-molecule MYC inhibitors. Comprehensive PK parameters such as bioavailability, half-life, and plasma protein binding remain to be characterized. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
No toxicity data has been published in the available literature. KJ-Pyr-9 is for research use only. Standard laboratory safety practices should be followed when handling this compound. As a MYC inhibitor, potential effects on normal cell proliferation should be considered.
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| References | |
| Additional Infomation |
KJ-Pyr-9 is a small molecule MYC inhibitor that binds to MYC with a Kd of 6.5 ± 1.0 nM and suppresses MYC-MAX heterodimer formation. It inhibits oncogenic transformation induced by MYC in cell culture. Burkitt lymphoma cells with high c-MYC expression show IC50 values of 1-2.5 µM. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C22H15N3O4
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|---|---|
| Molecular Weight |
385.379
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| Exact Mass |
385.106
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| CAS # |
581073-80-5
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| PubChem CID |
85855478
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
584.4±50.0 °C at 760 mmHg
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| Flash Point |
307.2±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
4.48
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
579
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=COC(=C1)C2=CC(=CC(=N2)C3=CC=C(C=C3)[N+](=O)[O-])C4=CC=C(C=C4)C(=O)N
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| InChi Key |
GTTDVYCKFQYVNN-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
4-[2-(furan-2-yl)-6-(4-nitrophenyl)pyridin-4-yl]benzamide
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| Synonyms |
KJ Pyr-9; KJPyr-9; KJ-Pyr-9
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~324.36 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2.08 mg/mL (5.40 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5948 mL | 12.9742 mL | 25.9484 mL | |
| 5 mM | 0.5190 mL | 2.5948 mL | 5.1897 mL | |
| 10 mM | 0.2595 mL | 1.2974 mL | 2.5948 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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