2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Survivin
  4. RO0505124

RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitotic entry, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer.

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

RO0505124

RO0505124 Chemical Structure

CAS No. : 443913-79-9

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RO0505124 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitotic entry, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer[1].

IC50 & Target[1]

CDK4

20 nM (IC50)

In Vitro

RO0505124 (30 min) potently and selectively inhibits recombinant human CDK4-cyclin D with an IC50 of 20 nM, showing >100-fold selectivity over CDK1 and CDK2, and relatively high selectivity across a panel of 128 kinases[1].
RO0505124 (48 h) inhibits proliferation of multiple human cancer cell lines with IC50 values ranging from 1.45 μM to 8.12 μM after 48 h of treatment[1].
RO0505124 (3.9-18.3 μM; 4-24 h) induces a G1 phase arrest and inhibits Rb phosphorylation in asynchronous HCT-116 cells[1].
RO0505124 (2 μM; 0-24 h) delays mitotic entry, prolongs mitotic duration, and induces aberrant mitosis[1].
RO0505124 (2 μM; 3-14 h) delays the accumulation of survivin and borealin proteins during G2/M phase in HeLa cells[1].

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

RO0505124 Related Antibodies

Western Blot Analysis[1]

Cell Line: asynchronous HCT-116 cells
Concentration: 3.9, 6.1, 18.3 μM
Incubation Time: 4, 24 h
Result: Reduced S phase to 50% of control levels and significantly decreased Rb phosphorylation at the IC50 concentration of 3.9 μM.
Further inhibited BrdUrd incorporation and Rb phosphorylation at higher doses.
Caused a G1 phase arrest with no reduction in G2/M phase cell proportion at higher doses.
Molecular Weight

451.55

Formula

C23H25N5O3S
CAS No.
SMILES

O=C(C1=CC=C2OCCOC2=C1)C=3SC(=NC3N)NC4=CC=C(C=C4)N5CCN(C)CC5
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Purity & Documentation
References
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RO0505124 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:

RO0505124443913-79-9RO 0505124RO-0505124CDKSurvivinCyclin dependent kinaseWee1ATM/ATRRb phosphorylationsurvivinborealinretinoblastoma proteinp38 MAPKCDK4-cyclin DCDK1CDK2Inhibitorinhibitorinhibit

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