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cell-free kinase assay

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-123597
    NSC 109555

    DDUG; NCI C04808

    		 Autophagy Checkpoint Kinase (Chk) Cancer
    NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
    NSC 109555
  • HY-116153
    HUHS2002

    		Cholinesterase (ChE) Neurological Disease
    HUHS2002 is a free fatty acid derivative with the ability to enhance α7 cholinergic receptor activity. HUHS2002 enhances whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner. The effects of HUHS2002 were blocked in the presence of the Ca2 /calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. HUHS2002 activated CaMKII in cultured rodent hippocampal neurons, and this activation was abolished by KN-93. HUHS2002 also partially inhibited the activity of protein phosphatase 1 (PP1) in a cell-free PP1 activity assay .
    HUHS2002
  • HY-183534
    CDK2-IN-58

    		CDK Cancer
    CDK2-IN-58 is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with an IC50 of 0.21 μM. CDK2-IN-58 can be used for cancer research .
    CDK2-IN-58
  • HY-179400
    LDN-193688

    		Anaplastic lymphoma kinase (ALK) TGF-beta/Smad Others
    LDN-193688 (Compound 26) is a ALK2 inhibitor, with IC₅₀ values of 104, 18, 235, 1530, and 1080 nM against ALK1, ALK2, ALK3, ALK4, and ALK5, respectively. LDN-193688 inhibits bone morphogenetic protein 4 (BMP4)-induced phosphorylation of SMAD1/5/8, with an IC₅₀ of 2.6 μM .
    LDN-193688

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