2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Epigenetics JAK/STAT Signaling Stem Cell/Wnt
  3. HSP HDAC STAT
  4. 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.

Hsp110/HDAC6-IN-1

Hsp110/HDAC6-IN-1 Chemical Structure

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Hsp110/HDAC6-IN-1 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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Description

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[1].

IC50 & Target[1]

HDAC6

0.013 μM (IC50)

In Vitro

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.

Hsp110/HDAC6-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: hypoxia-treated human pulmonary arterial endothelial cells (HPAECs)
Concentration: 5; 10 μM
Incubation Time: 24 h
Result: Dose-dependently reduced the number of EdU-positive HPAECs under hypoxic conditions.

Cell Migration Assay [1]

Cell Line: hypoxia-treated human pulmonary arterial endothelial cells (HPAECs)
Concentration: 5; 10 μM
Incubation Time: 24 h
Result: Dose-dependently inhibited hypoxia-induced migration of HPAECs.
In Vivo

Hsp110/HDAC6-IN-1 (compound 15n) (15-30 mg/kg; i.g.; daily; 2 weeks) dose-dependently inhibits pulmonary vascular remodeling and improves PAH-related endpoints in hypoxia-induced PAH rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (SD) rats (male, 160-180 g) with hypoxia-induced PAH[1]
Dosage: 15; 30 mg/kg
Administration: i.g.; daily; 2 weeks
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.
Molecular Weight

623.70

Formula

C33H37N9O4
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Hsp110/HDAC6-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hsp110/HDAC6-IN-1HSPHDACSTATHeat shock proteinsHistone deacetylasesSTAT3 signaling pathwaySTAT3pulmonary arterial hypertensionHsp110human pulmonary arterial endothelial cellsHPAECspulmonary vascular remodelingHDAC6protein-protein interactionratsInhibitorinhibitorinhibit

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