1. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Apoptosis
  2. HDAC HSP Apoptosis
  3. HDAC6/HSP90-IN-2

HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer.

For research use only. We do not sell to patients.

HDAC6/HSP90-IN-2 Chemical Structure

HDAC6/HSP90-IN-2 Chemical Structure

CAS No. : 2803866-22-8

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Description

HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer[1].

IC50 & Target

HDAC6

106 nM (IC50)

HDAC1

654.5 nM (IC50)

HDAC3

1539 nM (IC50)

HDAC7

1691 nM (IC50)

In Vitro

HDAC6/HSP90-IN-2 (compound 6e) (0.05-2 μM; 24 h) effects HSP90, HDAC6 and signaling pathways regulated by Hsp90 dose-dependently[1].
HDAC6/HSP90-IN-2 (compound 6e) (2 μM; 24 h) promotes the acetylation of HSP90[1].
HDAC6/HSP90-IN-2 (compound 6e) (0-100 μM; 24-72 h) inhibits the growth of H1975 non-small cell lung cancer cells[1].
HDAC6/HSP90-IN-2 (compound 6e) (0-2 μM; 24 h) induces apoptosis of H1975 cells[1].

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

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 0.05, 0.1, 0.5, 1 and 2 μM
Incubation Time: 24 hours
Result: Showed inhibitory effect to Hsp90 and HDACs dose-dependently and increased the expression levels of Hsp70 and Hsp90 probably by activates HSF1.

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 2 μM
Incubation Time: 24 hours
Result: Promoted the acetylation of Hsp90 by inhibiting HDAC6, and increased the acetylation at K294 residue of Hsp90.

Apoptosis Analysis[1]

Cell Line: H1975 cells
Concentration: 0, 0.5, 1 and 2 μM
Incubation Time: 24 hours
Result: Induced early and late apoptosis of H1975 cells dose-dependently.

Cell Viability Assay[1]

Cell Line: H1975 cells
Concentration: 0-100 μM
Incubation Time: 24, 48 and 72 h
Result: Inhibited the growth of H1975 non-small cell lung cancer cells with a GI50 value of 1.7 μM.
In Vivo

HDAC6/HSP90-IN-2 (25-50 mg/kg; i.p. every weekdays for 6 weeks) exhibits antitumor activity of in NOD-scid IL2Rgammanull (NSG) mice with xenotransplantation of H1975 cells[1].

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

Animal Model: NOD-scid IL2Rgammanull (NSG) mouse with H1975 cells xenograft[1]
Dosage: 25-50 mg/kg
Administration: Intraperitoneal injection; 25-50 mg/kg for every weekdays; for 6 weeks
Result: Delayed tumor growth after 2 weeks and reduced the growth rates of tumors in mice.
Molecular Weight

358.39

Formula

C19H22N2O5

CAS No.
SMILES

OC1=C(C(C)C)C=C(C(N(C)CC2=CC=C(C=C2)C(NO)=O)=O)C(O)=C1

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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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HDAC6/HSP90-IN-2
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