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NKL 22

Cat. No. M13676
NKL 22 Structure
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Biological Activity

NKL 22 (compound 4b) is a potent and selective inhibitor of histone deacetylases (HDAC), with an IC50 of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 exhibits selectivity over HDAC2/4/5/7/8 (IC50≥1.59 μM). NKL 22 ameliorates the disease phenotype and transcriptional abnormalities in Huntington's disease transgenic mice.

Chemical Information
Molecular Weight 325.4
CAS Number 537034-15-4
Solubility (25°C) DMSO ≥ 29 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Stefan Nagel, et al. Int J Mol Sci. NKL Homeobox Genes NKX2-3 and NKX2-4 Deregulate Megakaryocytic-Erythroid Cell Differentiation in AML

[2] Stefan Nagel, et al. Int J Mol Sci. NKL Homeobox Gene VENTX Is Part of a Regulatory Network in Human Conventional Dendritic Cells

[3] Aurlie Ppin, et al. J Cell Biochem. TSC-22 Promotes Interleukin-2-Deprivation Induced Apoptosis in T-Lymphocytes

[4] Marta Gigli, et al. Circulation. Phenotypic Expression, Natural History, and Risk Stratification of Cardiomyopathy Caused by Filamin C Truncating Variants

[5] Yi Liu, et al. Curr Pharm Des. A Uniquely Modified DKL-based Peptide Probe for Positron Emission Tomography Imaging

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Keywords: NKL 22 supplier, HDAC, inhibitors, activators


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