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PKC-theta inhibitor

Cat. No. M20591
PKC-theta inhibitor Structure
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Biological Activity

PKC-theta inhibitor inhibits PKC-θ with an IC50 of 12 nM.

Chemical Information
Molecular Weight 454.45
Formula C20H25F3N6O3
CAS Number 736048-65-0
Solubility (25°C) DMSO 91 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] Xin Chen, et al. Autophagy. Identification of HPCAL1 as a specific autophagy receptor involved in ferroptosis

[2] Simone C da Silva Rosa, et al. Autophagy. BNIP3L/Nix-induced mitochondrial fission, mitophagy, and impaired myocyte glucose uptake are abrogated by PRKA/PKA phosphorylation

[3] Kole T Roybal, et al. Sci Signal. Inhibiting the inhibitor of the inhibitor: blocking PKC-theta to enhance regulatory T cell function

[4] Roland G W Staal, et al. J Neurochem. PKC theta activity maintains normal quantal size in chromaffin cells

[5] Amnon Altman, et al. J Biochem. Protein kinase C-theta (PKC theta): a key enzyme in T cell life and death

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Keywords: PKC-theta inhibitor supplier, PKC, inhibitors, activators

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