1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. HDAC2-IN-1

HDAC2-IN-1 

Cat. No.: HY-151248
Handling Instructions

HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively.

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

HDAC2-IN-1 Chemical Structure

HDAC2-IN-1 Chemical Structure

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Description

HDAC2-IN-1 (Compound 17) is a brain penetrant, orally active, competitive HDAC2 inhibitor with an IC50 of 0.5 μM[1]. HDAC2-IN-1 also inhibits HDAC1 and HDAC8 with IC50s of 1.61 μM and 0.98 μM, respectively[1].

IC50 & Target[1]

HDAC2

0.5 μM (IC50)

HDAC8

0.98 μM (IC50)

HDAC1

1.61 μM (IC50)

In Vitro

HDAC2-IN-1 (Compound 17) (3 and 10 μM; 48 h) increases histone H4K12 and H3K9 acetylation levels in SKNSH cells in a dose-dependent manner[1].

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

In Vivo

HDAC2-IN-1 (Compound 17) (30 or 100 mg/kg; p.o.; once) shows good plasma and brain exposure, and shows promising brain penetration[1].

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

Animal Model: Male C57BL/6 mice[1]
Dosage: 30 or 100 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Showed good plasma and brain exposure, also showed promising brain penetration, Kp,uu = 0.36. Significantly increased histone H4K12 acetylation in mouse brain 4 h after oral dosing at 100 mg/kg.
Molecular Weight

426.96

Formula

C22H23ClN4OS

SMILES

ClC1=CC([[email protected]@H]2C[[email protected]](C(N3CCN(CC3)C4=NC=CC5=C4SC=C5)=O)NC2)=CC=C1

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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Product Name:
HDAC2-IN-1
Cat. No.:
HY-151248
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