1. Cell Cycle/DNA Damage
  2. CDK
  3. PHA-767491

PHA-767491 (Synonyms: CAY10572)

Cat. No.: HY-13461
Handling Instructions

PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.

For research use only. We do not sell to patients.

PHA-767491 Chemical Structure

PHA-767491 Chemical Structure

CAS No. : 845714-00-3

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Description

PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.

IC50 & Target[4]

CDK9

34 nM (IC50)

CDK2

240 nM (IC50)

CDK1

250 nM (IC50)

CDK5

460 nM (IC50)

GSK3-β

220 nM (IC50)

Mk2

470 nM (IC50)

Plk1

980 nM (IC50)

Chk2

1100 nM (IC50)

In Vitro

PHA-767491 inhibits proliferation in both cell lines with an IC50 of 0.64 µM in HCC1954 cells and 1.3 µM in Colo-205 cells. PHA-767491 is effective DDK inhibitors in vitro, with IC50 values of 18.6 nM. PHA-767491 (2 µM) completely abolishes Mcm2 phosphorylation by 24 hours in HCC1954 cells[1]. PHA-767491 in combination with 5-FU exhibits much stronger cytotoxicity and induces significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracts the 5-FU-induced phosphorylation of Chk1 and decreases the expression of the anti-apoptotic protein myeloid leukemia cell 1ine[2]. PHA-767491 (0-10 µM) decreases glioblastoma cell viability in a time- and dose-dependent fashion, with IC50 of approximately 2.5 µM for U87-MG and U251-MG cells. PHA-767491 hydrochloride induces apoptosis in glioblastoma cells, suppresses glioblastoma cell proliferation, cell migration and cell invasion[3].

In Vivo

PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts[2].

Molecular Weight

213.24

Formula

C₁₂H₁₁N₃O

CAS No.

845714-00-3

SMILES

O=C1C2=C(NC(C3=CC=NC=C3)=C2)CCN1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Kinase Assay
[1]

20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 µCi (γ)-32P ATP and 1.5 µM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

PHA-767491CAY10572PHA767491PHA 767491CAY 10572CAY-10572CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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PHA-767491
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HY-13461
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