CG0009
CG0009 is a GSK3 inhibitor. CG0009 activates p53 transcriptional activity, depletes Cyclin D1, induces Caspase-dependent Apoptosis, and activates Wnt/β-catenin target genes. CG0009 does not induce epithelial-mesenchymal transition, does not increase Vimentin/N-cadherin, and does not decrease E-cadherin. CG0009 exhibits anticancer activity against breast cancer and colorectal cancer.
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- CAS No.: 944744-57-4
- Formule: C26H31N7O
- Masse moléculaire:457.58
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
CG0009 is a GSK3 inhibitor. CG0009 activates p53 transcriptional activity, depletes Cyclin D1, induces Caspase-dependent Apoptosis, and activates Wnt/β-catenin target genes. CG0009 does not induce epithelial-mesenchymal transition, does not increase Vimentin/N-cadherin, and does not decrease E-cadherin. CG0009 exhibits anticancer activity against breast cancer and colorectal cancer[1][2][3][4].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.49 μM
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Cytotoxicity against human MCF7 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human MCF7 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
|
23565238 |
| Hs-578T | IC50 |
1 μM
|
Cytotoxicity against human HS578T breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human HS578T breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
|
23565238 |
| MDA-MB-435 | IC50 |
4.3 μM
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Cytotoxicity against human MDA-MB-435 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human MDA-MB-435 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
|
23565238 |
| MDA-MB-231 | IC50 |
4.9 μM
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Cytotoxicity against human MDA-MB-231 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human MDA-MB-231 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
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23565238 |
| NCI/ADR-RES | IC50 |
11 μM
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Cytotoxicity against human NCI/ADR-RES breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human NCI/ADR-RES breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
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23565238 |
| BT-549 | IC50 |
11 μM
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Cytotoxicity against human BT549 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human BT549 breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
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23565238 |
| T47D | IC50 |
>100 μM
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Cytotoxicity against human T47D breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human T47D breast cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
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23565238 |
| HCT-116 | IC50 |
0.22 μM
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Cytotoxicity against human HCT116 colon cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
Cytotoxicity against human HCT116 colon cancer cells assessed as viability reduction after 48 hrs exposure by CellTiter-Glo luminescent assay.
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23565238 |
In Vitro
Anti-cancerCell Cycle RegulationApoptosisOthers
Anti-cancer
CG0009 (0.001-100 μM; 48 h) reduces viability most potently in HCT116 (IC50 0.22 μM) and MCF7 (0.49 μM), while T47D remains resistant (>100 μM)[1].
Anti-cancer
Cell Cycle Regulation
CG0009 (1 μM; 0-48 h) depletes cyclin D1 in ERα-negative HS578T, MDA-MB-435, MDA-MB-231, and NCI/ADR-RES cells, with complete loss by 40 h in moderately sensitive lines[1].
CG0009 decreases proliferation and survival in different breast cancer cell lines, reduces cyclin D1 expression, and activates p53[2].
CG0009 decreases proliferation and survival in different breast cancer cell lines, reduces cyclin D1 expression, and activates p53[2].
Apoptosis
Cell Cycle Regulation
Others
CG0009 (1 μM; 0-24 h) inactivates GSK3α/β in HCT116, MCF7, and T47D by increasing Ser21/Ser9 phosphorylation and decreasing Tyr216 phosphorylation[1].
CG0009 (1 μM; 0-24 h) does not sustain AKT Ser473 phosphorylation in MCF7 cells[1].
CG0009 (1 μM; 0-48 h) does not increase AKT kinase activity in MCF7 lysates[1].
CG0009 (1 μM; 0-24 h) induces p53 and p21 protein in MCF7 but not T47D[1].
CG0009 (1 μM; 0-24 h) does not sustain AKT Ser473 phosphorylation in MCF7 cells[1].
CG0009 (1 μM; 0-48 h) does not increase AKT kinase activity in MCF7 lysates[1].
CG0009 (1 μM; 0-24 h) induces p53 and p21 protein in MCF7 but not T47D[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
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Cell Line:human breast cancer cell lines (MCF7, HS578T, MDA-MB-435, MDA-MB-231, NCI/ADR-RES, BT549, T47D) and HCT116 colon cancer cells
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Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:48 h (after 24 h seeding)
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Result:IC50 values were 0.49 μM in MCF7, 1 μM in HS578T, 4.3 μM in MDA-MB-435, 4.9 μM in MDA-MB-231, 11 μM in NCI/ADR-RES, 11 μM in BT549, >100 μM in T47D, and 0.22 μM in HCT116.
Growth was suppressed across the panel, with HCT116 and MCF7 most sensitive and T47D resistant.
Western Blot Analysis[1]
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Cell Line:HCT116, MCF7, and T47D cells
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Concentration:1 μM
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Incubation Time:0, 8, 16, 24 h
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Result:Inactivating phosphorylation of GSK3α Ser21 and GSK3β Ser9 was enhanced, activating phosphorylation of GSK3β Tyr216 was suppressed in all three cell lines, and total GSK3α/β was slightly decreased.
Western Blot Analysis[1]
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Cell Line:MCF7 and T47D cells
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Concentration:1 μM
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Incubation Time:0, 8, 16, 24, 32 h
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Result:In MCF7, caspase-9 and PARP were activated after 8 h.
In T47D, PARP activation was delayed until 32 h, and caspase-9 activation was not detectable.
Western Blot Analysis[1]
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Cell Line:MCF7 cells
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Concentration:1 μM
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Incubation Time:0, 8, 16, 24 h
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Result:Normalized pAKT Ser473 values were 1, 0.9, 1, and 0.8 at 0, 8, 16, and 24 h, respectively.
Real Time qPCR[1]
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Cell Line:MCF7 and T47D cells
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Concentration:1 μM
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Incubation Time:0, 8, 16, 24, 32, 40, 48 h
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Result:In MCF7, ERα and cyclin D1 transcripts were significantly reduced approximately 5-fold up to 48 h.
In T47D, ERα initially decreased at 8 h, increased to approximately 8-fold at 24 h, and decreased again at 48 h; cyclin D1 showed a decrease followed by a subsequent increase.
T47D expressed approximately 10-fold higher cyclin D1 transcripts than MCF7.
Western Blot Analysis[1]
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Cell Line:MCF7 and T47D cells
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Concentration:1 μM
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Incubation Time:0, 8, 16, 24, 32, 40, 48 h
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Result:Complete ablation of ERα and cyclin D1 proteins occurred in MCF7, but not in T47D.
Chemical Information
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CAS No. 944744-57-4
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Masse moléculaire 457.58
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Formule C26H31N7O
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SMILES
O=C(NC=1C=NC=CC1C)C=2C=CN=C3N=C(NC32)C=4C=CC(=CC4)N(C)CCN(CC)CC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Select Batch:
Pureté:
99.98%
Assay:
99.98%
ee.:
99.98%
Références
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CG0009 Related Classifications
HY-111045 Related Classifications
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Keywords
- CG0009
- 944744-57-4
- CG 0009
- CG-0009
- GSK-3
- MDM-2/p53
- CDK
- Caspase
- Apoptosis
- Wnt
- β-catenin
- Glycogen synthase kinase-3
- Glycogen synthase kinase 3
- Cyclin dependent kinase
- Beta catenin
- AKT
- Bax
- GSK3α/β
- Wnt/β-catenin
- breast cancer
- caspase-dependent apoptosis
- cyclin D1
- epithelial-to-mesenchymal transition
- estrogen receptor
- p53
- Inhibitor
- inhibitor
- inhibit