2. Cell Cycle/DNA Damage
  3. CDK
  4. CGP-82996

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer.

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

CGP-82996 Chemical Structure

CGP-82996 Chemical Structure

CAS No. : 359886-84-3

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CGP-82996 Related Antibodies

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Description

GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer[1][2].

IC50 & Target[1]

Cdk4/cyclin D1

1.5 μM (IC50)

CDK6/cyclinD1

5.6 μM (IC50)

CDK5/p35

25 μM (IC50)

CDK2/cyclinA

>50 μM (IC50)

CDK1/cyclinB

>100 μM (IC50)

CDK2/cyclin E

>50 μM (IC50)

CDK4/cyclin D2

>50 μM (IC50)

Cdk6/cyclin D2

>50 μM (IC50)

V-abl

>10 μM (IC50)

c-met

>10 μM (IC50)

IGF-1R

>10 μM (IC50)

Insulin-R

>10 μM (IC50)

In Vitro

GP-82996 (5, 10 μM; 24 hours) induces G1 arrest and G0-G1/S ratio increase in U2OS (p16 negative) and MRC-5 (p16 positive) cells[1].
GP-82996 (5, 10 μM; 24 hours) reduces hyperphosphorylation of pRb, but has no changes in the levels of CDK4 in U2OS, MRC-5 cells[1].
GP-82996 (5, 10 μM; 48 hours) induces aooptosis in 83% of U2OS cells in concentration of 10μM[1].
GP-82996 (0.1-40 μM; 24,48, 72 hours) inhibits the cell proliferation of A549, H358, SKLU-1, H23, PC14 cells with IC50 values of 72 h are 4-7 μM[2].
GP-82996 (3, 5, 10 μM; 48 hours) induces G1 arrest in A549 and H23 cells[2].
GP-82996 ((1, 3, 5, 10 μM; 72 hours) enhances Paclitaxel sensitivity in KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23 cells) [2].
GP-82996 (10 μM; 72 hours) combined with Paclitaxel (3 nM; 72 hours) increases the apoptosis of A549 and H23 cells[2].

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

CGP-82996 Related Antibodies
In Vivo

GP-82996 (30 mg/kg, i.p. for 29 days) shows smaller final tumor volume compared with vehicle control in mouse xenograft models[1].

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

Animal Model: 19-21 g female BALB/c nu/nu mice xenograft model (HCT116 tumors volume=100 mm3)[1]
Dosage: 30 mg/kg
Administration: i.p. every 12 hours for 29 days
Result: Showed smaller final tumor volume compared with vehicle control in mouse xenograft models.
Molecular Weight

456.58

Formula

C27H32N6O
CAS No.
SMILES

O[C@H]1CC[C@H](NC2=NC(NC3=CC4=C(N(CC5=CC=CC=C5)C=C4)C=C3)=NC(NCC)=C2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    5% DMSO, 0.05% Tween 80, and 95% physiologic saline

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CGP-82996 Related Classifications

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:

CGP-82996359886-84-3CINK4CGP82996CGP 82996CINK 4CINK-4CDKCyclin dependent kinasecancerG1 arresthyperphosphorylation of pRbaooptosisKRAS mutationcellsInhibitorinhibitorinhibit

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