2. Cell Cycle/DNA Damage Apoptosis PROTAC
  3. CDK Apoptosis DNA/RNA Synthesis Molecular Glues
  4. CDK-IN-9

CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.

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CDK-IN-9

CDK-IN-9 Chemical Structure

CAS No. : 3031561-92-6

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Based on 1 publication(s) in Google Scholar

CDK-IN-9 Related Antibodies

Top Publications Citing Use of Products

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II[1].

IC50 & Target[1]

RNA Polymerase

 

CDK2/E

4 nM (IC50)

Cdk5/p25

39 nM (IC50)

CDK9/T1

20 nM (IC50)

CDK12/K

64 nM (IC50)

CDK13/K

22 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
DB GI50
0.02 μM
Compound: 24
Antiproliferative activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
NU-DUL-1 GI50
0.015 μM
Compound: 24
Antiproliferative activity against human NU-DUL-1 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human NU-DUL-1 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
OCI-LY19 GI50
0.465 μM
Compound: 24
Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
SUD4 GI50
0.028 μM
Compound: 24
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
U2932 GI50
0.055 μM
Compound: 24
Antiproliferative activity against human U2932 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human U2932 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
In Vitro

CDK-IN-9 (compound 24) (0.005, 0.05, 0.5, or 5 μM; 2 h) potently decreases the level of cyclin K in MINO cells at 5 nM, and makes cyclin K disappear completely at 50 nM[1].
CDK-IN-9 makes siRNA silencing of DDB1 effectively stabilizes cyclin K at the protein level in treated MINO cells[1].
CDK-IN-9 (2.5-40 nM; 24 h) activates caspases 3/7/9 and decreases anti-apoptotic proteins Mcl-1 and XIAP in MINO cells[1].

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

CDK-IN-9 Related Antibodies
In Vivo

CDK-IN-9 (0.1-10 mg/kg; IP, single dosage) causes the decrease in cyclin K and CDK12 levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

420.53

Formula

C21H24N8S
CAS No.
SMILES

NCCSC1=NC2=C(NN=C2C(NCC3=CC=C(C=C3)N4C=CC=N4)=N1)C5CCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CDK-IN-9 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK-IN-93031561-92-6CDKApoptosisDNA/RNA SynthesisMolecular GluesCyclin dependent kinasecyclin KCDK12DDB1dephosphorylationretinoblastomaMINO cellsInhibitorinhibitorinhibit

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