Hsp110/HDAC6-IN-1
Hsp110/HDAC6-IN-1 is an orally active Hsp110/HDAC6 dual inhibitor. Hsp110/HDAC6-IN-1 disrupts Hsp110-STAT3 protein-protein interaction, suppresses HDAC6 enzymatic activity, and suppresses STAT3 signaling pathway. Hsp110/HDAC6-IN-1 inhibits abnormal proliferation and migration of human pulmonary arterial endothelial cells, and suppresses pulmonary vascular remodeling in rats. Hsp110/HDAC6-IN-1 can be used for the research of pulmonary arterial hypertension.
For research use only. We do not sell to patients.
- Formula: C33H37N9O4
- Molecular Weight:623.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC6 0.013 μM (IC50) |
Hsp110/HDAC6-IN-1 (compound 15n) (10 μM; 1 h) inhibits purified Hsp110 protein with an 82.55% inhibition rate at 10 μM[1].
Hsp110/HDAC6-IN-1 potently and selectively inhibits recombinant HDAC6 protein with an IC50 of 0.013 μM[1].
Hsp110/HDAC6-IN-1 (1.5625-12.5 μM; 90 s) binds directly to purified Hsp110 protein with a Kd of 2.77 μM[1].
Hsp110/HDAC6-IN-1 (0-1.4 μM; 1 h) inhibits the interaction between probe C and purified Hsp110 protein with an IC50 of 5.26 μM[1].
Hsp110/HDAC6-IN-1 (2 h) binds directly to endogenous Hsp110 in HPAECs, increasing its stability against protease digestion[1].
Hsp110/HDAC6-IN-1 (48 h) potently inhibits hypoxia-induced proliferation of HPAECs with an IC50 of 8.99 μM[1].
Hsp110/HDAC6-IN-1 (5-10 μM; 24 h) dose-dependently inhibits migration, and hypoxia-induced proliferation of HPAECs[1].
Hsp110/HDAC6-IN-1 (5 μM) disrupts the Hsp110-STAT3 protein-protein interaction in HPAECs when treated at 5 μM[1].
Hsp110/HDAC6-IN-1 (5-10 μM) dose-dependently inhibits HDAC6 activity and suppresses the STAT3 signaling pathway in hypoxia-treated HPAECs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hypoxia-treated human pulmonary arterial endothelial cells (HPAECs)
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Concentration:5; 10 μM
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Incubation Time:24 h
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Result:Dose-dependently reduced the number of EdU-positive HPAECs under hypoxic conditions.
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Cell Line:hypoxia-treated human pulmonary arterial endothelial cells (HPAECs)
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Concentration:5; 10 μM
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Incubation Time:24 h
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Result:Dose-dependently inhibited hypoxia-induced migration of HPAECs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats (male, 160-180 g) with hypoxia-induced PAH[1]
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Dosage:15; 30 mg/kg
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Administration:i.g.; daily; 2 weeks
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Result:Reduced right ventricular systolic pressure (RVSP).
Reduced right ventricular weight/tibia length ratio, reduced right ventricular weight/(left ventricular + interventricular septum) ratio, reduced pulmonary artery medial thickness percentage.
Increased pulmonary artery Ac-α-tubulin levels, reduced pulmonary artery p-STAT3, c-Myc, Cyclin D1, Fibronectin I, Collagen I, p-Smad3, and α-SMA levels.
Produced greater improvements in right ventricular hypertrophy indices compared to the 15 mg/kg dose, produced greater increases in pulmonary artery Ac-α-tubulin levels and greater reductions in pulmonary artery p-STAT3, Cyclin D1, p-Smad3, and α-SMA levels compared to the combination therapy group.
Did not cause significant decreases in rat body weight.
Chemical Information
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Molecular Weight 623.70
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Formula C33H37N9O4
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SMILES
O=C(NO)CCCCCCNC(C1=CC=CC(N2N=C(C)C3=CC(C4=NC(N)=CC(N)=N4)=C(OCC5=CC=CC(C)=C5)N=C32)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hsp110/HDAC6-IN-1 Related Classifications
HY-183985 Related Classifications
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