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MG149

Cat. No. M3645
MG149 Structure
Size Price Availability Quantity
2mg USD 100  USD100 In stock
5mg USD 150  USD150 In stock
10mg USD 240  USD240 In stock
50mg USD 720  USD720 In stock
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Quality Control
Biological Activity

MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149, at 200 μM, inhibites about 90% of Tip60 activity but has no inhibitory impact on p300 and PCAF. MG 149 is essentially competitive with Ac-CoA and noncompetitive with the histone substrate. MG149 inhibits acetyltransferase activity of nuclear extract from tissue samples from different brain regions in mice. MG149 inhibits the p53 and the NF-κB pathways.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 340.46
Formula C22H28O3
CAS Number 1243583-85-8
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

[1] Legartová S, et al. Epigenomics. Basic nuclear processes affected by histone acetyltransferases and histone deacetylase inhibitors.

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Keywords: MG149 supplier, Histone Acetyltransferase, inhibitors

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