2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK4-IN-5

CDK4-IN-5 is a potent, orally active and selective CDK4 inhibitor. CDK4-IN-5 suppresses CDK4 expression and downregulates the CDK4/CyclinD1 complex. CDK4-IN-5 induces G0/G1 phase cell cycle arrest in bladder cancer cells via CyclinD1 expression suppression. CDK4-IN-5 selectively exerts activity against bladder cancer cells. CDK4-IN-5 can be used for the research of bladder cancer.

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CDK4-IN-5

CDK4-IN-5 Chemical Structure

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CDK4-IN-5 Related Antibodies

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Description

CDK4-IN-5 is a potent, orally active and selective CDK4 inhibitor. CDK4-IN-5 suppresses CDK4 expression and downregulates the CDK4/CyclinD1 complex. CDK4-IN-5 induces G0/G1 phase cell cycle arrest in bladder cancer cells via CyclinD1 expression suppression. CDK4-IN-5 selectively exerts activity against bladder cancer cells. CDK4-IN-5 can be used for the research of bladder cancer[1].

IC50 & Target[1]

Cdk4/cyclin D1

 

In Vitro

CDK4-IN-5 (compound 2a) (0.016-50 μM; 72 h) potently inhibits the viability of T24 and 5637 bladder cancer cells with IC50 values of 0.44 μM and 0.49 μM, respectively, while demonstrating favorable selectivity over normal SV-HUC-1 cells (IC50 = 4.51 μM)[1].
CDK4-IN-5 (0.1 μM; 24-72 h) exerts a time-dependent inhibitory effect on the proliferation of T24 and 5637 bladder cancer cells[1].
CDK4-IN-5 (150-300 nM; 10-14 days) potently and durably suppresses colony formation of T24 and 5637 bladder cancer cells in a dose-dependent manner[1].
CDK4-IN-5 (600-1200 nM; 24 h) induces dose-dependent G0/G1 phase cell cycle arrest in T24 and 5637 bladder cancer cells[1].
CDK4-IN-5 (120-3000 nM; 48 h) dose-dependently downregulates CDK4 and CyclinD1 protein expression in T24 bladder cancer cells[1].
CDK4-IN-5 stably binds to the ATP-binding pocket of CDK4, with a most favorable binding energy of -10.1 kcal/mol at the CDK4 site[1].

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

CDK4-IN-5 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: T24, 5637 cells
Concentration: 150; 300 nM
Incubation Time: 10-14 days
Result: Inhibited colony formation of T24 and 5637 cells in a dose-dependent manner.
Showed a marked inhibitory effect in both T24 and 5637 cells.

Cell Proliferation Assay[1]

Cell Line: T24, 5637 cells
Concentration: 0.1 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Showed no significant inhibition at 24 h.
Decreased OD values by 37.41% in T24 cells and 50.90% in 5637 cells by 48 h.
Reduced OD values further to 45.47% in T24 cells and 51.89% in 5637 cells by 72 h.

Cell Cycle Analysis[1]

Cell Line: T24, 5637 cells
Concentration: 600; 1200 nM
Incubation Time: 24 h
Result: Induced accumulation of cells in the G0/G1 phase with concurrent reduction in S phase population.
Increased G0/G1 phase percentage from 57.16% to 81.22% in T24 cells and from 44.10% to 63.55% in 5637 cells at 600 nM.
Further increased G0/G1 phase percentage to 83.12% in T24 cells and 66.74% in 5637 cells at 1200 nM, with S phase fractions decreasing to 9.17% in T24 cells and 26.99% in 5637 cells.

Western Blot Analysis[1]

Cell Line: human bladder cancer T24 cells
Concentration: 120; 600; 3000 nM
Incubation Time: 48 h
Result: Significantly reduced CDK4 expression in a dose-dependent manner.
Decreased CyclinD1 levels in a dose-dependent manner.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t CL MRT0-t F
Rat[1] 5 mg/kg i.v. 1.85 h 12300 ng/mL 5537 ng·h/mL 16.67 mL/min/kg 0.39 h /
Rat[1] 50 mg/kg i.g. 13.2 h 2222 ng/mL 9073 ng·h/mL 86.67 mL/min/kg 7.63 h 16.4 %
Molecular Weight

472.61

Formula

C28H40O6
SMILES

C[C@@]1(CCC([C@@H](CCC2[C@H]3C)C)[C@]42OO1)O[C@H]4O[C@H]3OC(C(C)C5=CC=C(C=C5)CC(C)C)=O
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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CDK4-IN-5 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:

CDK4-IN-5CDKCyclin dependent kinaseratsATP-binding pocketCyclinD1CDK4/CyclinD1 complexCDK4G0/G1 phaseSV-HUC-15637bladder cancer cellsT24Inhibitorinhibitorinhibit

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