1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK12-IN-E9

CDK12-IN-E9 

Cat. No.: HY-117203A
Handling Instructions

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.

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

CDK12-IN-E9 Chemical Structure

CDK12-IN-E9 Chemical Structure

CAS No. : 2020052-55-3

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM[1].

IC50 & Target[1]

CDK12

 

CDK9/cyclinT1

23.9 nM (IC50)

cdk2/cyclin A

932 nM (IC50)

CDK7/Cyclin H/MNAT1

1210 nM (IC50)

In Vitro

CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM[1].
CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression[1].
CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9[1].

Cell Proliferation Assay[1]

Cell Line: Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells
Concentration: 10 nM-10 μM
Incubation Time: 72 hours
Result: Showed potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM.

Western Blot Analysis[1]

Cell Line: Kelly, PC-9, and NCI-H82 cells
Concentration: 0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM
Incubation Time: 6 hours
Result: Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models.
Molecular Weight

434.53

Formula

C₂₄H₃₀N₆O₂

CAS No.

2020052-55-3

SMILES

C=CC(NC1=CC=CC(NC2=CC(N3[[email protected]](CCO)CCCC3)=NC4=C(CC)C=NN24)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

CDK12-IN-E9CDKCyclin dependent kinaseCDK9CDK12antiproliferativeABCpyrazollopyridinephosphorylatedRNAPIIMYCMCL1Cys1039Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
CDK12-IN-E9
Cat. No.:
HY-117203A
Quantity:
MCE Japan Authorized Agent: