ZAK-IN-1
Based on 1 Customer Validation
ZAK-IN-1 is an orally active and selective selective leucine-zipper and sterile‑α motif kinase (ZAK) inhibitor with IC50 of 4 nM and KD of 8 nM. ZAK-IN-1 exhibits excellent selectivity against a panel of 403 wild-type kinases. ZAK-IN-1 blocks p38/GATA-4 and JNK/c-Jun signaling and shows promising anti antihypertrophic cardiomyopathy (HCM) efficacy. ZAK-IN-1 can be used for the study of HCM.
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- Reinheit: 98.43%
- CAS. Nr.: 2362525-64-0
- Formel: C27H19F2N7O3S
- Molecular Weight:559.55
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
4 nM
Compound: 6p
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Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay
Inhibition of N-terminal GST-tagged recombinant human full-length ZAK expressed in baculovirus infected Sf9 insect cells using MBP as substrate after 30 mins by ADP-Glo assay
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[PMID: 31244114] |
ZAK-IN-1 (Compound 6p) (0-10 μg/mL, 24 h) could effectively suppress hypertrophy induced by ZAKα overexpression by blocking p38/GATA-4 and JNK/c-Jun signaling in H9c2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H9c2 cells
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Concentration:0, 2.5, 5, 10 μg/mL
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Incubation Time:24 h
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Result:Dose dependently inhibited the phosphorylated ZAKα but had no detectable impact on the ZAKα expression level.
Blocked the cardiac hypertrophy induced by AngII and Doxycycline (HY-N0565) .
Dose dependently decreased the expression of brain natriuretic peptide (BNP).
Suppressed the elevation of p-JNK and p-p38 and hypertrophic transcription factors p-GATA-4 and p-c-Jun.
| Species | Dose | Route | Cmax | T1/2 | AUC0-t | AUC0-∞ | Bioavailability | CL |
|---|---|---|---|---|---|---|---|---|
| Rat | 10 mg/kg | p.o. | 16372.2 μg/L | 1.7 h | 71572.6 μg/L·h | 71790.9 μg/L·h | 65.3 % | / |
| Rat | 2.5 mg/kg | i.v. | 34151.6 μg/L | 1.6 h | 27424.4 μg/L·h | 27866.1 μg/L·h | / | 91.9 L/h/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spontaneous hypertensive rats (SHR) model established by SD male rats (180-220 g)[1]
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Dosage:0, 2.5, and 10 mg/kg
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Administration:Oral administration (p.o.), once daily for 8 weeks
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Result:Suppressed the whole heart and the left ventricle mass elevation and rescued the hypertrophic symptoms in a dose-dependent manner.
Suppressed the phosphorylation of ZAK down-stream signaling JNK, p38, c-Jun, p-GATA-4, and protein levels of hypertrophic markers BNP and ANP in a dose-dependent manner.
Chemical Information
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CAS. Nr. 2362525-64-0
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Appearance Solid
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Molecular Weight 559.55
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Formel C27H19F2N7O3S
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Color White to off-white
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SMILES
FC1=CC=C(NS(C2=CC=CC(C3=CC=CC=C3)=C2)(=O)=O)C(F)=C1N4N=NC(C5=CN=C(NN=C6OC)C6=C5)=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (178.72 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7872 mL | 8.9358 mL | 17.8715 mL | 44.6788 mL |
| 5 mM | 0.3574 mL | 1.7872 mL | 3.5743 mL | 8.9358 mL | |
| 10 mM | 0.1787 mL | 0.8936 mL | 1.7872 mL | 4.4679 mL | |
| 15 mM | 0.1191 mL | 0.5957 mL | 1.1914 mL | 2.9786 mL | |
| 20 mM | 0.0894 mL | 0.4468 mL | 0.8936 mL | 2.2339 mL | |
| 25 mM | 0.0715 mL | 0.3574 mL | 0.7149 mL | 1.7872 mL | |
| 30 mM | 0.0596 mL | 0.2979 mL | 0.5957 mL | 1.4893 mL | |
| 40 mM | 0.0447 mL | 0.2234 mL | 0.4468 mL | 1.1170 mL | |
| 50 mM | 0.0357 mL | 0.1787 mL | 0.3574 mL | 0.8936 mL | |
| 60 mM | 0.0298 mL | 0.1489 mL | 0.2979 mL | 0.7446 mL | |
| 80 mM | 0.0223 mL | 0.1117 mL | 0.2234 mL | 0.5585 mL | |
| 100 mM | 0.0179 mL | 0.0894 mL | 0.1787 mL | 0.4468 mL |
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