Recombinant:Article Title: Discovery of 1(2H)-phthalazinone and 1(2H)-isoquinolinone derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Article Snippet: Although immune checkpoint inhibitors (ICIs) have been a revelation for treating several cancers, an unmet need remains to broaden ICI therapeutic scope and increase their response rates in clinical trials.. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of T cell activation and has previously been identified as a promising target for immunotherapy.. Herein, we report the discovery of a series of HPK1 inhibitors with novel 1(2H)-phthalazinone and 1(2H)-isoquinolinone scaffolds.
Article Title: Design, Synthesis, and Biological Evaluation of a Series of Spiro Analogues as Novel HPK1 Inhibitors
Article Snippet: .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature. .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature.
Concentration Assay:Article Title: Discovery of 1(2H)-phthalazinone and 1(2H)-isoquinolinone derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Article Snippet: Although immune checkpoint inhibitors (ICIs) have been a revelation for treating several cancers, an unmet need remains to broaden ICI therapeutic scope and increase their response rates in clinical trials.. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of T cell activation and has previously been identified as a promising target for immunotherapy.. Herein, we report the discovery of a series of HPK1 inhibitors with novel 1(2H)-phthalazinone and 1(2H)-isoquinolinone scaffolds.
Article Title: Design, Synthesis, and Biological Evaluation of a Series of Spiro Analogues as Novel HPK1 Inhibitors
Article Snippet: .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature. .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature.
In Vitro:Article Title: Design, Synthesis, and Biological Evaluation of a Series of Spiro Analogues as Novel HPK1 Inhibitors
Article Snippet: .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature. .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature.
Enzymatic Assay:Article Title: Design, Synthesis, and Biological Evaluation of a Series of Spiro Analogues as Novel HPK1 Inhibitors
Article Snippet: .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature. .. In vitro enzymatic assay (MAP4K1-MAP4K6) The recombinant human MAP4K1 protein (final concentration 0.5 nM, purchased from Carna Biosciences, Cat No, 07-410), recombinant human MAP4K2 protein(final concentration 1 nM, purchased from Carna Biosciences, Cat No, 07-111), recombinant human MAP4K3 protein (final concentration 1.5 nM, purchased from Invitrogen , Cat No, PV6350), recombinant human MAP4K4 protein (final concentration 2.5 nM, purchased from Carna Biosciences, Cat No, 07-137), recombinant human MAP4K5 (final concentration 0.25 nM, purchased from Invitrogen, Cat No, PR6671A), recombinant human MAP4K6 protein (final concentration 1.5 nM, purchased from Carna Biosciences, Cat No, 07-139) were preincubated with serially diluted ISM compounds (10000-0.50805 nM, 3-fold increments) in a reaction buffer [50mM HEPEs, pH 7.5; 10mM MgCl2; 4mM DTT; 0.01% Tween-20; 0.01% BSA] for 10 min at room temperature.
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