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TP-064

Cat. No. M11055
TP-064  Structure
Size Price Availability Quantity
25mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

TP-064 is a potent and selective PRMT4 small molecule inhibitor with ic50 < 10 nM, which is more than 100 times more selective for PRMT4 than other PRMT.

Chemical Information
Molecular Weight 458.6
Formula C28H34N4O2
CAS Number 2080306-20-1
Solubility (25°C) DMSO ≥ 60 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] Futaba Inoue, et al. Biochem Biophys Res Commun. Histone arginine methyltransferase CARM1 selective inhibitor TP-064 induces apoptosis in endometrial cancer

[2] Yiheng Zhang, et al. Atherosclerosis. PRMT4 inhibitor TP-064 impacts both inflammatory and metabolic processes without changing the susceptibility for early atherosclerotic lesions in male apolipoprotein E knockout mice

[3] Yiheng Zhang, et al. Biochim Biophys Acta Mol Basis Dis. PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo

[4] Kazuhide Nakayama, et al. Oncotarget. TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma

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