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1-7a-B1

1-7a-B1 : Inhibitor of CDK9

Structure

Information

  • CDK9
  • Inhibitor
  • up to 1 uM

In Vitro Validations

Uniprot ID: P50750
Target Class: Kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 6.51 nM
Potency Assay: Biochemical assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Cyclin-dependent kinase 9, TAK, CDC2L4, CDK9, CDK9 ...

DOI Reference: 10.1021/acs.jmedchem.5c00472

Uniprot ID: P50750
Target Class: Kinase
Target SubClass: CMGC
Potency: Kd
Potency Value: 8868 nM
Potency Assay: SPR, binding affinity of 1-7a-B1 to CDK9/Cyclin T1
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Cyclin-dependent kinase 9, TAK, CDC2L4, CDK9, CDK9 ...

DOI Reference: 10.1021/acs.jmedchem.5c00472

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Inhibitory activity of 1-7a-B1 against several CDK subtypes (CDK1, CDK2, CDK4, and CDK6) was assessed showing that 1-7a-B1 possesses high inhibition selectivity toward CDK1/2/4/6, approximately 180-fold or more greater than that toward CDK9.
Potency assay (off target): The kinase selectivity profile of 1-7a-B1 was evaluated by determining the percent inhibition against a panel of 80 kinases at a single concentration of 100 nM.
Potency assay, off target (cells): GI50 values of a panel of 15 representative cell lines for different types of cancer and NCM460 (a normal colorectal cell line) were also determined. The GI50 values revealed that different types of cells could possess varying sensitivities to 1-7a-B1. The tested cells from pancreatic cancer (Panc-1), lung cancer (NCI-H226 and A549), liver cancer (HepG2), and normal colorectal (NCM460) cell lines showed low sensitivity to 1-7a-B1, which confirmed the low toxicity and selectivity of 1-7a-B1.
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