1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK9-IN-22

CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity.

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CDK9-IN-22 Chemical Structure

CDK9-IN-22 Chemical Structure

CAS No. : 2872677-61-5

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Description

CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity[1].

IC50 & Target[1]

CDK9/cyclinT1

10.4 nM (IC50)

cdk2/cyclin A

876.2 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
0.1 μM
Compound: 8d
Antiproliferative activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
A549 IC50
0.66 μM
Compound: 8d
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
HCT-116 IC50
0.09 μM
Compound: 8d
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
L02 IC50
1.43 μM
Compound: 8d
Antiproliferative activity against human L02 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human L02 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
NCI-H1975 IC50
0.43 μM
Compound: 8d
Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
PANC-1 IC50
0.08 μM
Compound: 8d
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
In Vitro

CDK9-IN-22 (compound 8 d) (0.1, 0.5, 2.5 µM; 24, 48 h) induces apoptosis and cell cycle arrests at G2/M phase in a concentration-dependent manner in PANC-1 cells[1].
CDK9-IN-22 (0.1, 0.5, 2.5 µM; 24 h) decreases the expression of p-RNAPII (S2) and CDK9 protein in PANC-1 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: A549, H1975, A431, PANC-1, HCT-116, LO2 cells
Concentration: 0-100 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.66, 0.43, 0.10, 0.08, 0.09, 1.43 μM for A549, H1975, A431, PANC-1, HCT-116, LO2 cells, respectively.

Apoptosis Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 0.5, 2.5 µM
Incubation Time: 48 h
Result: Induced apoptosis with the percentage of total apoptotic cells was 43.6, 54.1 and 65.8% at 0.1, 0.5 and 2.5 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 0.5, 2.5 µM
Incubation Time: 24 h
Result: Arrested the cell cycle at the G2/M phase in a dose-dependent manner (21.83% for 0.1 μM, 25.85% for 0.5 μM and 34.26% for 2.5 μM).

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 0.5, 2.5 µM
Incubation Time: 24 h
Result: Decreased the expression of p-RNAPII (S2) and CDK9 protein in a dose-dependent manner.
In Vivo

CDK9-IN-22 (5, 10, 20 mg/kg; i.p.; every other day for four weeks) inhibits tumor growth in xenograft murine model[1].

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

Animal Model: BALB/c nude mice (PANC-1 tumor xenograft murine model)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.p.; every other day for four weeks
Result: Inhibited the tumor growth with the tumor inhibition rate (TIR) was 6.2, 32.6 and 54.2% at the dose of 5, 10 and 20 mg/kg, respectively.
Molecular Weight

485.55

Formula

C28H28FN5O2

CAS No.
SMILES

CN(CCNC(C1=CC=C(C=C1)NC2=NC(C3=C(C=C(C=C3)F)OCC4=CC=CC=C4)=CC=N2)=O)C

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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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.

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Product Name:
CDK9-IN-22
Cat. No.:
HY-151984
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