HDAC2-IN-1

Cat. No.: HY-151248: FAQs
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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

CAS No. : 2919691-32-8

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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].

MedChemExpress (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].

MedChemExpress (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, K_p,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

CAS No.

2919691-32-8

SMILES

ClC1=CC([C@@H]2C[C@H](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

Handling Instructions (2659 KB)

References

[1]. Tamanini E, et al. Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor. ACS Medicinal Chemistry Letters, 2022.

HDAC2-IN-1 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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:

HDAC2-IN-12919691-32-8HDACHistone deacetylasesbrain penetrantorally activehistone H4K12histone H3K9Inhibitorinhibitorinhibit

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