NKL 22

Catalog No.S6548 Batch:S654801

Technical Data

Formula	C₁₉H₂₃N₃O₂
Molecular Weight	325.40	CAS No.	537034-15-4
Solubility (25°C)*	In vitro	DMSO	65 mg/mL (199.75 mM)
		Ethanol	3 mg/mL (9.21 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

NKL 22 is a selective inhibitor of HDAC with IC50 of 78 µM.

Targets

HDAC ^[1]
(Cell-free assay)

78 μM

In vitro

2.5 μM of NKL 22 increases frataxin protein concentrations in the FRDA ymphoid cell line. Incubation for 2 d in culture with NKL 22 increases the FXN mRNA level in lymphocytes from the affected individual to about 80% of that in lymphocytes from the unaffected individual. NKL 22 is highly active in increasing FXN mRNA levels in cells obtained from both carrier C and affected AC, bringing the FXN mRNA level in the FRDA lymphocytes to about 160% of that found in the untreated carrier lymphocytes.^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines human lymphocytes Concentrations 2.5 μM Incubation Time 48 h Method Blood is collected in heparinized Vacutainer tubes and lymphocytes are isolated by density centrifugation using Ficoll-Paque PLUS. Lymphocytes are maintained in the same culture medium and conditions as the established cell lines. HDAC inhibitors are dissolved in DMSO and added the solution to the culture medium at the concentrations, for the indicated times. The final DMSO concentration in the culture medium does not exceed 0.5% (v/v). Cells are treated with HDAC inhibitors after 16 h, and RNA is isolated after subsequent 48-h incubation.

Cell Assay:^{^[1]}

Cell lines
human lymphocytes
Concentrations
2.5 μM
Incubation Time
48 h
Method
Blood is collected in heparinized Vacutainer tubes and lymphocytes are isolated by density centrifugation using Ficoll-Paque PLUS. Lymphocytes are maintained in the same culture medium and conditions as the established cell lines. HDAC inhibitors are dissolved in DMSO and added the solution to the culture medium at the concentrations, for the indicated times. The final DMSO concentration in the culture medium does not exceed 0.5% (v/v). Cells are treated with HDAC inhibitors after 16 h, and RNA is isolated after subsequent 48-h incubation.

References

[1] Herman D, et al. Nat Chem Biol. 2006 ;2(10):551-8.

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SHIPPING AND STORAGE
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