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GNA002

Cat. No. M11278
GNA002  Structure
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Biological Activity

GNA002 is a potent, selective, covalent EZH2 inhibitor with an IC50 of 1.1 μM against EZH2. GNA002 can specifically and covalently bind Cys668 in the EZH2-SET domain to induce EZH2 degradation through COOH terminal of ubiquitination mediated by Hsp70 interacting protein (CHIP). GNA002 effectively reduced EZH2-mediated H3K27 trimethylation and reactivated tumor suppressor genes silenced by Polycomb repressor complex 2 (PRC2).

Chemical Information
Molecular Weight 701.9
Formula C42H55NO8
CAS Number 1385035-79-9
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage -20°C , dry , sealed
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] Fan Li, et al. J Nanobiotechnology. Multifunctional nanoplatforms as cascade-responsive drug-delivery carriers for effective synergistic chemo-photodynamic cancer treatment

[2] Fan Li, et al. Nanoscale. Nuclear-targeted nanocarriers based on pH-sensitive amphiphiles for enhanced GNA002 delivery and chemotherapy

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Keywords: GNA002 supplier, Histone Methyltransferase, inhibitors, activators

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