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in vitro PHARMACOLOGY 2011 CATALOG - Cerep

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150 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />

❚ prote<strong>in</strong>-SERINE/THREONINE k<strong>in</strong>ases [TKL]<br />

IRAK4<br />

Ref. 2933<br />

Q 3 weeks<br />

Included <strong>in</strong>:<br />

ExpresS Diversity k<strong>in</strong>ase profile<br />

Organ safety profile<br />

Comprehensive k<strong>in</strong>ase profile<br />

Source<br />

human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />

Substrate ATP + Ulight-FLGFTYVAP<br />

(50 nM)<br />

Measured product phospho-Ulight-FLGFTYVAP<br />

Detection method LANCE<br />

Reference staurospor<strong>in</strong>e (IC 50 : 32 nM)<br />

Li, S. et al. (2002) Proc. Natl. Acad. Sci. U S A., 99: 5567-5572.<br />

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LIMK1<br />

Ref. 2934<br />

Q 3 weeks<br />

Included <strong>in</strong>:<br />

Comprehensive k<strong>in</strong>ase profile<br />

Source<br />

human recomb<strong>in</strong>ant (Sf21 cells)<br />

Substrate ATP + Ulight-RRRSLLE<br />

(50 nM)<br />

Measured product phospho-Ulight-RRRSLLE<br />

Detection method LANCE<br />

Reference<br />

staurospor<strong>in</strong>e (IC 50 : 59 nM)<br />

Scott, R.W. and Olson, M.F. (2007) J. Mol. Med., 85: 555-568.<br />

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LRRK2<br />

Ref. 3177<br />

Q 3 weeks<br />

Source<br />

human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />

Substrate ATP + Ulight-RRRSLLE<br />

(50 nM)<br />

Measured product phospho-Ulight-RRRSLLE<br />

Detection method LANCE<br />

Reference<br />

H-89 (IC 50 : 30 nM)<br />

Greggio, E. et al. (2008) J. Biol. Chem., 283: 16906-16914.<br />

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MLK1<br />

Ref. 2935<br />

Q 3 weeks<br />

Included <strong>in</strong>:<br />

Comprehensive k<strong>in</strong>ase profile<br />

Source<br />

human recomb<strong>in</strong>ant<br />

Substrate ATP + Ulight-FLGFTYVAP<br />

(400 nM)<br />

Measured product phospho-Ulight-FLGFTYVAP<br />

Detection method LANCE<br />

Reference<br />

staurospor<strong>in</strong>e (IC 50 : 21.5 nM)<br />

Maroney, A.C. et al. (2001) Biochem. J., 276: 25302-25308.<br />

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MLK2 (MAP3K10)<br />

Ref. 2326<br />

Q 3 weeks<br />

Included <strong>in</strong>:<br />

Comprehensive k<strong>in</strong>ase profile<br />

Source<br />

human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />

Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG<br />

(25 nM)<br />

Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL<br />

AGCG<br />

Detection method LANCE<br />

Reference<br />

staurospor<strong>in</strong>e (IC 50 : 79 nM)<br />

Liu, Y.F. et al. (2000) J. Biol. Chem., 275: 19035-19040.<br />

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RAF-1 k<strong>in</strong>ase<br />

Ref. 2936<br />

Q 3 weeks<br />

Included <strong>in</strong>:<br />

ExpresS Diversity k<strong>in</strong>ase profile<br />

Organ safety profile<br />

Comprehensive k<strong>in</strong>ase profile<br />

Source<br />

human recomb<strong>in</strong>ant<br />

Substrate ATP + Ulight-ARTKQTARKSTGGKAPRKQLAGCG<br />

(50 nM)<br />

Measured product phospho-Ulight-ARTKQTARKSTGGKAPRKQL<br />

AGCG<br />

Detection method LANCE<br />

Reference staurospor<strong>in</strong>e (IC 50 : 94 nM)<br />

Force, T. et al. (1994) Proc. Natl. Acad. Sci. USA., 91: 1270-1274.

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