1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. HDAC6-IN-13

HDAC6-IN-13 

Cat. No.: HY-151261
Handling Instructions

HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity.

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

HDAC6-IN-13 Chemical Structure

HDAC6-IN-13 Chemical Structure

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Description

HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity[1].

IC50 & Target[1]

HDAC6

0.019 μM (IC50)

HDAC3

1.03 μM (IC50)

HDAC1

1.53 μM (IC50)

HDAC2

2.06 μM (IC50)

In Vitro

HDAC6-IN-13 (Compound 35m) (0.1-1 μM; 24 h) is highly selective toward HDAC6 versus class I HDACs[1].
HDAC6-IN-13 is a slow-on and slow-off tight-binding HDAC6 inhibitor, while exhibits fast-on properties for HDAC1, 2, and 3[1].
HDAC6-IN-13 (5-20 μM; 8 h) shows anti-inflammatory activity in vitro[1].

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

Western Blot Analysis[1]

Cell Line: MV4−11 and J774A.1
Concentration: 0.1, 0.2, 0.5 and 1 μM
Incubation Time: 24 h
Result: Concentration-related accumulation of acetylated tubulin (Ac-Tubulin) was observed, while upregulation of acetylated histone H3 (AcHH3) and acetylated histone H4 (AcHH4) was not apparent even at the concentration of 1 μM.

Western Blot Analysis[1]

Cell Line: J774A.1 cells
Concentration: 5, 10 and 20 μM
Incubation Time: 8 h
Result: Inhibited the cleavage of pro-caspase 1 to p20 in a dose-dependent manner, inhibited the interaction between HDAC6 and dynein.
In Vivo

HDAC6-IN-13 (Compound 35m) (20 mg/kg; p.o. and i.p.; once) displays a remarkable inhibition in LPS-induced inflammation in mice[1].
HDAC6-IN-13 (20 mg/kg; p.o.; once) shows very high oral bioavailability (F% = 93.4%) and significant BBB permeability in mice[1].

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

Animal Model: Male C57BL/6 WT mice, LPS-induced endotoxic shock model[1]
Dosage: 20 mg/kg
Administration: PO and IP, immediately after the LPS injection
Result: Significantly decreased the serum IL-1β levels in LPS-induced mice via both ip and po administration.
Animal Model: Male CD-1 mice[1]
Dosage: 5 mg/kg or 20 mg/kg
Administration: IV (5 mg/kg) or PO (20 mg/kg) (Pharmacokinetic Study)
Result: Pharmacokinetics Characterization of HDAC6-IN-13 (Compound 35m) with iv and Oral Administrationa[1]
PK parameters HDAC6-IN-13 HDAC6-IN-13
administered dose (mg/kg) iv at 5 mg/kg oral at 20 mg/kg
Cmax (ng/mL) 4604 ± 551 5570 ± 551
t1/2 (h) 7.95 ± 0.370 6.80 ± 0.145
AUC0−inf (ng•h/mL) 2755 ± 395 10292 ± 1385
F% n/a 93.4 ± 12.6

aHDAC6-IN-13 was administrated via iv and po (n = 3). The blood sample was collected at different time points after dosing, and the plasma concentration of HDAC6-IN-13 was determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) was calculated using the linear trapezoidal method. The pharmacokinetic parameters were obtained using the noncompartmental method. Data are shown as mean ± SD.
Molecular Weight

370.45

Formula

C23H22N4O

SMILES

CCNNC(C1=CC=C(C=C1)CN2C3=CC=CC=C3C=CC4=C2C=NC=C4)=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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HDAC6-IN-13
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HY-151261
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