| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
YZ129 targets heat shock protein 90 (HSP90), a molecular chaperone involved in the folding and stabilization of numerous client proteins, including those in the calcineurin-NFAT signaling pathway. By binding to HSP90, YZ129 disrupts the HSP90-calcineurin-NFAT pathway, inhibiting NFAT nuclear translocation with an IC₅0 of 820 nM.
|
|---|---|
| ln Vitro |
YZ129 demonstrates potent in vitro activity against glioblastoma. It induces GBM cell cycle arrest at the G2/M phase, promotes apoptosis, and inhibits tumor cell growth/proliferation and migration. The compound directly binds to HSP90 and inhibits NFAT nuclear translocation with an IC₅0 of 820 nM. Purity is typically >99%.
|
| ln Vivo |
In vivo, YZ129 is used as a research tool to explore HSP90-NFAT signaling in glioblastoma, benchmarking combination treatments with radiotherapy or kinase inhibitors, and evaluating pathway vulnerability in other NFAT- or HSP90-addicted cancers as well as inflammation, angiogenesis, and immune modulation in tumors.
|
| Enzyme Assay |
In vitro binding assays for YZ129 typically employ purified HSP90 protein and assess binding affinity using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or fluorescence polarization. NFAT nuclear translocation inhibition is assessed in cell-based assays using NFAT-GFP reporter constructs or immunofluorescence staining for NFAT localization.
|
| Cell Assay |
In vitro cellular assays for YZ129 involve treating glioblastoma cell lines (e.g., U87, U251) with varying concentrations of the compound (typically 0.01-100 microM range) for 24-72 hours. Readouts include cell viability measured by MTT or CellTiter-Glo, assessment of cell cycle distribution by flow cytometry, evaluation of apoptosis by annexin V/PI staining, and assessment of NFAT nuclear translocation by immunofluorescence or cell fractionation.
|
| Animal Protocol |
In vivo animal studies for YZ129 would typically employ orthotopic or subcutaneous xenograft mouse models bearing glioblastoma tumors. Tumor-bearing mice would be administered YZ129 via appropriate routes at various doses, potentially in combination with radiotherapy or kinase inhibitors. Tumor growth inhibition would be monitored over 2-4 weeks. Endpoints would include tumor volume, survival, and pharmacodynamic biomarkers.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of YZ129 are characteristic of small molecule HSP90 inhibitors. With a molecular weight of 300.31, the compound is a small molecule. PK parameters including half-life, Cmax, Tmax, and AUC would be determined via LC-MS/MS analysis following administration in appropriate animal models.
|
| Toxicity/Toxicokinetics |
YZ129 is a research-grade compound for laboratory use only. As with all research chemicals, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. The compound is not intended for human therapeutic use. Comprehensive toxicology data is not publicly available.
|
| References | |
| Additional Infomation |
YZ129 (CAS# 1643120-60-8) is an HSP90-calcineurin-NFAT pathway inhibitor against glioblastoma. It induces G2/M cell cycle arrest, promotes apoptosis, and inhibits tumor cell proliferation and migration. The compound is not approved for clinical use and is for research purposes only.
|
| Molecular Formula |
C19H12N2O2
|
|---|---|
| Molecular Weight |
300.310784339905
|
| Exact Mass |
300.089
|
| CAS # |
1643120-60-8
|
| PubChem CID |
137628683
|
| Appearance |
Brown to red solid powder
|
| LogP |
2.9
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
23
|
| Complexity |
528
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1C(C=C(C2C=CC=CC=21)NC1C=CC2C=NC=CC=2C=1)=O
|
| InChi Key |
NYDMVPHEEBVAHT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H12N2O2/c22-18-10-17(15-3-1-2-4-16(15)19(18)23)21-14-6-5-13-11-20-8-7-12(13)9-14/h1-11,21H
|
| Chemical Name |
4-(isoquinolin-6-ylamino)naphthalene-1,2-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~5.6 mg/mL (~18.65 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3299 mL | 16.6495 mL | 33.2989 mL | |
| 5 mM | 0.6660 mL | 3.3299 mL | 6.6598 mL | |
| 10 mM | 0.3330 mL | 1.6649 mL | 3.3299 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
