1. Apoptosis Cell Cycle/DNA Damage
  2. Apoptosis CDK
  3. CDK9-IN-33

CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity.

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CDK9-IN-33 Chemical Structure

CDK9-IN-33 Chemical Structure

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Description

CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity[1].

IC50 & Target[1]

CDK9

17.44 nM (IC50)

CDK7

160 nM (IC50)

CDK2

316.30 nM (IC50)

CDK4

1771.00 nM (IC50)

CDK6

>10000 nM (IC50)

In Vitro

CDK9-IN-33 (compound C35) (0, 0.01, 0.1, 1 µM; 24 h) decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1 and increases the expression of cleaved PARP[1].
CDK9-IN-33 (0, 0.01, 0.1, 1 µM) decreases the mRNA expression levels of the MCL1 gene[1].
. CDK9-IN-33 (0, 0.01, 0.1, 1 µM; 72 h) induces apoptosis in a dose-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells
Concentration:
Incubation Time: 4 days
Result: Showed antiproliferation potential for MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells with IC50 values of 5.9, 10.05, 5.61, 20.08, 8.98, 24.38 nM, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.01, 0.1, 1 µM
Incubation Time: 24 h
Result: Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.

RT-PCR[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.01, 0.1, 1 µM
Incubation Time: 24 h
Result: Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.

Apoptosis Analysis[1]

Cell Line: 4T1 cells
Concentration: 0, 0.01, 0.1, 1 µM
Incubation Time: 72 h
Result: Induced apoptosis in a dose-dependent manner.
In Vivo

CDK9-IN-33 (10 mg/kg; p.o.; daily for 10 days) shows anti-tumor activity in mice[1].
Pharmacokinetic Parameters (male ICR mice; p.o. 20.0 mg/kg, i.v. 5.0 mg/kg; )[1].

Cmpd T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (h·ng/mL) AUCt–∞ (h·ng/mL) CL (mL/min/kg) MRT0–∞ (h) Vss (mL/kg) F (%)
C35 (p.o.) 0.68 0.5 2867 4349 4350 - 1.43 - 68.9
C35 (i.v.) 0.36 - - 1578 1578 52.9 0.33 1033 -

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

Molecular Weight

437.54

Formula

C23H31N7O2

SMILES

CC(C1=C2N=C(N=C(N2N=C1)NCC3=CC=C(C=C3)NC(CC)=O)NC4CCOCC4)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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CDK9-IN-33
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HY-162619
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