Product Feature - Kinase Inhibitors

A protein kinase is an enzyme that chemically modifies proteins by the addition of a phosphate group. This modification results in a change in the protein activity, cellular localisation or association with other proteins.

The human genome consists of roughly 500 protein kinase genes; about 2% of all eukaryotic genes. 30% of all proteins can be modified by kinases and kinases regulate the majority of cellular pathways. Disregulation of kinase activity has been implicated in diseases such as cancer and kinase inhibitors are being developed as potential therapeutics.

Selective inhibitor of TGF-β RI
2718 l LY 364947
IC₅₀ = 59 nM. Displays > 40-fold selectivity over TGF-β RII and MLK-7K.
TGF-β RI Related Products: SB 431542

Potent and selective cMET inhibitor
2693 l PHA 665752
IC₅₀ = 9 nM. Displays > 7-fold selectivity over cMET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src.
cMET Related Products: EGFR Reagents VEGFR Reagents

Potent and selective inhibitor of MEK1/2
2605 l PD 198306
Inhibits the isolated enzyme at a concentration of 8 nM.
MEK 1/2 Related Products: PD 98059 SL 327 U0126

Selective inhibitor of IKK
2539 l IKK 16
IC₅₀ values are 40, 70 and 200 nM for IKK-2, IKK complex and IKK-1 respectively.
IKK Related Products: TPCA-1 IMD 0354

Cell Cycle Kinase Inhibitors

ATM and ATR protein kinases are key regulators of the cell cycle checkpoint pathways in response to DNA damage. ATM responds to double stranded DNA breaks (DSBs) whilst ATR only plays a small role in DSBs and primarily responds to damage induced by UV light. Activated ATM and ATR phosphorylate and activate Chk1 and Chk2 respectively.

Selective Chk1 Inhibitor
2560 l SB 218078
IC₅₀ = 15 nM. Displays > 16-fold selectivity over cdc2 and PKC.
Chk1 Related Products: PD 407824 Cell Cycle Reagents

Selective inhibitor of ATR and ATM kinases
2639 l CGK 733
IC₅₀ ~ 200 nM. Displays no effect on DNA-PK, PIKK and mTOR.
ATR/ATM Related Products: PD 407824 Cell Cycle Reagents

Cdk 4 inhibitor
2609 l Ryuvidine
IC₅₀ = 6.0 μM at cdk4/cyclin D1 and displays > 33-fold selectivity over cdk2.
Cdk 4 Related Products: NSC 625987

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