1. Metabolic Enzyme/Protease Epigenetics Cell Cycle/DNA Damage
  2. Epoxide Hydrolase HDAC
  3. sEH/HDAC6-IN-2

sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain.

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

sEH/HDAC6-IN-2 Chemical Structure

sEH/HDAC6-IN-2 Chemical Structure

CAS No. : 3009011-58-6

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Description

sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain[1].

IC50 & Target[1]

HDAC6

0.008 μM (IC50)

Human sEh

0.0009 μM (IC50)

Mouse sEh

0.0468 μM (IC50)

HDAC8

0.062 μM (IC50)

HDAC11

0.464 μM (IC50)

HDAC2

0.492 μM (IC50)

HDAC1

1.151 μM (IC50)

HDAC3

1.276 μM (IC50)

In Vitro

sEH/HDAC6-IN-2 has significant selectivity on the inhibitory activity of HDAC6 (selectivity Index: HDAC1/HDAC6 = 144, HDAC2/HDAC6 = 62, HDAC3/HDAC6 = 160, HDAC8/HDAC6 = 8, HDAC11/HDAC6 = 58)[1].
sEH/HDAC6-IN-2 (compound 28g; 1-2 μM; 24 h) induces an increase in acetylation of α-tubulin without affecting histone H3, indicating the selective inhibition of HDAC6[1].

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

Western Blot Analysis[1]

Cell Line: THP-1 cells
Concentration: 1 μM, 2 μM
Incubation Time: 24 h
Result: Induced acetylation of α-tubulin and histone H3.
In Vivo

sEH/HDAC6-IN-2 (compound 28g; 30 mg/kg; ip; once) relieves Formalin-induced inflammatory pain in mice[1].
Pharmacokinetics of sEH/HDAC6-IN-2 in SD rats Following Intravenous and Oral Administration[1].
1.19

parameter iv (10 mg/kg) ig (50 mg/kg)
Tmax (h) 0.08 0.50
Cmax (μM) 7.87 6.63
t1/2 (h) 5.43 3.55
CL (L/h) 0.16 0.82
Vz (L) 1.28 4.20
AUC0-12h (μM·h) 12.29 15.01
AUC0-∞ (μM·h) 21.16 21.22
F (%) 24.42 -

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

Animal Model: Kunming mice (male, weighing 20-22 g) injected with 5% Formalin solution[1].
Dosage: 30 mg/kg
Administration: ip; once
Result: Exhibited an effective analgesic activity.
Molecular Weight

580.02

Formula

C27H32ClF2N5O5

CAS No.
SMILES

O=C([C@@H]1CN(C(C2=CC=C(NC(NC3=CC=C(Cl)C(F)=C3)=O)C(F)=C2)=O)CCC1)NCCCCCCC(NO)=O

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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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  • 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.

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sEH/HDAC6-IN-2
Cat. No.:
HY-159171
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