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AZ82

Cat. No. M13687
AZ82 Structure
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Biological Activity

AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

Chemical Information
Molecular Weight 560.63
CAS Number 1449578-65-7
Solubility (25°C) DMSO 90 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] Anzana Parvin, et al. Gene. Corrigendum to "Inhibition of kinesin motor protein KIFC1 by AZ82 induces multipolar mitosis and apoptosis in prostate cancer cell" [Gene 760 (2020) 144989]

[2] Anzana Parvin, et al. Gene. Inhibition of kinesin motor protein KIFC1 by AZ82 induces multipolar mitosis and apoptosis in prostate cancer cell

[3] Masashi Yukawa, et al. Fungal Genet Biol. Fission yeast cells overproducing HSET/KIFC1 provides a useful tool for identification and evaluation of human kinesin-14 inhibitors

[4] Hee-Won Park, et al. Sci Rep. Structural basis of small molecule ATPase inhibition of a human mitotic kinesin motor protein

[5] Jiaquan Wu, et al. ACS Chem Biol. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1

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Keywords: AZ82 supplier, Kinesin, inhibitors, activators

 
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