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cdk9 in 2  (MedChemExpress)
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MedChemExpress cdk9 in 2
Thermo Fisher SelectScreen kinase assay results and modeling of UNC-721A within the <t>CDK9</t> active site. (A) The Thermo Fisher SelectScreen kinase assay was used to validate CDK9 as a target of UNC-721A. The kinase assay was performed as described in Methods and kinase inhibition plotted as a function of UNC-721A concentration. The IC50 value was determined to be 0.603 nM (n = 3). (B) Chemical structure of UNC-721A. The predicted fit of this molecule in the ATP binding site of CDK9 was determined by molecular modeling as described in Materials and Methods. This model indicates that the UNC-721A structure fits with high confidence within the CDK9 active site.
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Thermo Fisher SelectScreen kinase assay results and modeling of UNC-721A within the CDK9 active site. (A) The Thermo Fisher SelectScreen kinase assay was used to validate CDK9 as a target of UNC-721A. The kinase assay was performed as described in Methods and kinase inhibition plotted as a function of UNC-721A concentration. The IC50 value was determined to be 0.603 nM (n = 3). (B) Chemical structure of UNC-721A. The predicted fit of this molecule in the ATP binding site of CDK9 was determined by molecular modeling as described in Materials and Methods. This model indicates that the UNC-721A structure fits with high confidence within the CDK9 active site.

Journal: SLAS discovery : advancing life sciences R & D

Article Title: Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth

doi: 10.1177/2472555218773045

Figure Lengend Snippet: Thermo Fisher SelectScreen kinase assay results and modeling of UNC-721A within the CDK9 active site. (A) The Thermo Fisher SelectScreen kinase assay was used to validate CDK9 as a target of UNC-721A. The kinase assay was performed as described in Methods and kinase inhibition plotted as a function of UNC-721A concentration. The IC50 value was determined to be 0.603 nM (n = 3). (B) Chemical structure of UNC-721A. The predicted fit of this molecule in the ATP binding site of CDK9 was determined by molecular modeling as described in Materials and Methods. This model indicates that the UNC-721A structure fits with high confidence within the CDK9 active site.

Article Snippet: The inhibitors used were CDK9-IN-2 (MedChem Express, Monmouth Junction, NJ, cat. HY-16462), ML167 (Selleckchem, Houston, TX, cat. S7509), PF 670462 (Tocris, Minneapolis, MN, cat. 3316), and Alisertib (ApexBio, Hsinchu City, Taiwan, cat. A4110), respectively.

Techniques: Kinase Assay, Inhibition, Concentration Assay, Binding Assay

CDK-IN-2 2D and 3D cell viability responses. CDK-IN-2, a selective CDK9 inhibitor, was used to compare the effects on cell growth to that observed with UNC-721A. Cell viability assays were done in both 2D and 3D spheroid format as described above (CellTiter-Glo 3D). The cells consisted of a 1:1 ratio (5000:5000 cells/well) of MiaS or MiaR cells combined with GFP-CAF cells, and they were treated for 72 h and analyzed as above. (A) Results from the 2D analysis of this compound in triplicate. (B) Results from the 3D analysis of this compound in triplicate. Shown are representative figures for n = 3 independent experiments.

Journal: SLAS discovery : advancing life sciences R & D

Article Title: Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth

doi: 10.1177/2472555218773045

Figure Lengend Snippet: CDK-IN-2 2D and 3D cell viability responses. CDK-IN-2, a selective CDK9 inhibitor, was used to compare the effects on cell growth to that observed with UNC-721A. Cell viability assays were done in both 2D and 3D spheroid format as described above (CellTiter-Glo 3D). The cells consisted of a 1:1 ratio (5000:5000 cells/well) of MiaS or MiaR cells combined with GFP-CAF cells, and they were treated for 72 h and analyzed as above. (A) Results from the 2D analysis of this compound in triplicate. (B) Results from the 3D analysis of this compound in triplicate. Shown are representative figures for n = 3 independent experiments.

Article Snippet: The inhibitors used were CDK9-IN-2 (MedChem Express, Monmouth Junction, NJ, cat. HY-16462), ML167 (Selleckchem, Houston, TX, cat. S7509), PF 670462 (Tocris, Minneapolis, MN, cat. 3316), and Alisertib (ApexBio, Hsinchu City, Taiwan, cat. A4110), respectively.

Techniques: