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KDM2A/7A-IN-1

Cat. No. M45100
KDM2A/7A-IN-1 Structure
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Biological Activity

KDM2A/7A-IN-1 is a first-in-class, selective, cell-permeable inhibitor of the histone lysine demethylase KDM2A/7A, with an IC50 value of 0.16 μM for KDM2A, 75-fold more selective than other JmjC lysine demethylases, and with no effect on methyltransferases or histone acetyltransferases. KDM2A was 75 times more selective than other JmjC lysine demethylases and had no effect on methyltransferases and histone acetyltransferases.

Chemical Information
Molecular Weight 506.68
Formula C33H38N4O
CAS Number 2169272-46-0
Form Solid
Solubility (25°C) DMSO >100 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] Zongyao Ren, et al. Neurosci Bull. The Role of KDM2A and H3K36me2 Demethylation in Modulating MAPK Signaling During Neurodevelopment

[2] Matthew Martin, et al. Biomolecules. KDM2A Deficiency in the Liver Promotes Abnormal Liver Function and Potential Liver Damage

[3] Chen Chen, et al. Cancer Res. Targeting KDM2A Enhances T-cell Infiltration in NSD1-Deficient Head and Neck Squamous Cell Carcinoma

[4] Jian Wang, et al. Biochem Biophys Res Commun. KDM2A plays a dual role in regulating the expression of malignancy-related genes in esophageal squamous cell carcinoma

[5] Bing Lu, et al. Cell Death Dis. Histone H3K36me2 demethylase KDM2A promotes bladder cancer progression through epigenetically silencing RARRES3

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Keywords: KDM2A/7A-IN-1 supplier, Histone demethylase, inhibitors, activators


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