1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
    Autophagy
  2. HDAC
    Apoptosis
    Autophagy
  3. Quisinostat dihydrochloride

Quisinostat dihydrochloride (Synonyms: JNJ-26481585 dihydrochloride)

Cat. No.: HY-15433A
Handling Instructions

Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.

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

Quisinostat dihydrochloride Chemical Structure

Quisinostat dihydrochloride Chemical Structure

CAS No. : 875320-31-3

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Description

Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity[1].

IC50 & Target[1]

HDAC1

0.11 nM (IC50)

HDAC2

0.33 nM (IC50)

HDAC11

0.37 nM (IC50)

HDAC10

0.46 nM (IC50)

HDAC5

3.69 nM (IC50)

HDAC8

4.26 nM (IC50)

HDAC3

4.86 nM (IC50)

HDAC9

32.1 nM (IC50)

HDAC6

76.8 nM (IC50)

HDAC7

119 nM (IC50)

In Vitro

JNJ-26481585 inhibits HDAC isozymes in vitro[1].
JNJ-26481585 (30-1000 nM; 24 hours) is a potent pan-HDAC inhibitor in tumor cells[1].
JNJ-26481585 has broad spectrum antiproliferative activity against solid and hematologic cancer cell lines and induces apoptosis[1].

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

Western Blot Analysis[1]

Cell Line: Human A2780 ovarian carcinoma cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 24 hours
Result: Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM.
In Vivo

JNJ-26481585 (40 mg/kg; p.o.; once daily, for 3 days) as a potent HDAC1 inhibitor p21waf1,cip1 ZsGreen tumors in vivo[1].
JNJ-26481585 induces continuous H3 acetylation in tumor tissue in vivo[1].
JNJ-26481585 (10 mg/kg; once daily; i.p.; for 14 days) strongly inhibits the growth of large pre-established HCT116 colon xenografts[1].

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

Animal Model: NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, once daily, for 14 days
Result: Strongly inhibited the growth of large pre-established HCT116 colon xenografts.
Molecular Weight

467.39

Formula

C₂₁H₂₈Cl₂N₆O₂

CAS No.

875320-31-3

SMILES

[H]Cl.O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

QuisinostatJNJ-26481585JNJ26481585JNJ 26481585HDACApoptosisAutophagyHistone deacetylaseshistonedeacetylasehematologicmalignanciesInhibitorinhibitorinhibit

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Product Name:
Quisinostat dihydrochloride
Cat. No.:
HY-15433A
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