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TPCK

Cat. No. M30043
TPCK Structure
Synonym:

L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

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Biological Activity

TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium.

Chemical Information
Molecular Weight 351.85
Formula C17H18ClNO3S
CAS Number 402-71-1
Form Solid
Solubility (25°C) DMSO ≥ 100 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] Jay Trivedi, et al. Biochem Biophys Res Commun. N-p-Tosyl-L-phenylalanine chloromethyl ketone (TPCK) inhibits HIV-1 by suppressing the activity of viral protease

[2] Rana Anjum, et al. FEBS Lett. TPCK inhibits AGC kinases by direct activation loop adduction at phenylalanine-directed cysteine residues

[3] Z Fabian, et al. Biochem Biophys Res Commun. TPCK targets elements of mitotic spindle and induces cell cycle arrest in prometaphase

[4] Z Fabian, et al. Apoptosis. TPCK-induced apoptosis and labelling of the largest subunit of RNA polymerase II in Jurkat cells

[5] E Schmitt, et al. Biochem Cell Biol. The Bcl-xL and Bax-alpha control points: modulation of apoptosis induced by cancer chemotherapy and relation to TPCK-sensitive protease and caspase activation

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Keywords: TPCK, L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK supplier, Serine/Threonine Protease, inhibitors, activators


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