COG449
COG449 (OP449) is a cell-penetrating peptide that binds to SET, prevents the formation of the SET-PP2A complex, and restores PP2A phosphatase activity. COG449 decreases the phosphorylation levels of AKT308, ERK1/2, NFkB p65, and c-MYC S62, and reduces c-MYC stability and target gene expression. COG449 induces apoptosis, autophagy, and histone H3 hyperacetylation, and decreases the levels of SET, CIP2A, SETBP1, and Mcl-1. COG449 reduces cancer cell viability and decreases tumor mass in xenograft models. COG449 can be used for research on various cancers such as oral squamous cell carcinoma, T-cell acute lymphoblastic leukemia, B-CLL, non-Hodgkin lymphoma, and breast cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C418H712N146O82S4
- Molecular Weight:9223.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
ERK1 |
ERK2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| WSU-HN13 | IC50 |
5.94 μM
|
Reduction in cell viability of human HN13 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
Reduction in cell viability of human HN13 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
|
32569675 |
| HN12 | IC50 |
5.11 μM
|
Reduction in cell viability of human HN12 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
Reduction in cell viability of human HN12 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
|
32569675 |
| HN-6 | IC50 |
9.17 μM
|
Reduction in cell viability of human HN6 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
Reduction in cell viability of human HN6 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
|
32569675 |
| CAL-27 | IC50 |
8.86 μM
|
Reduction in cell viability of human Cal27 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
Reduction in cell viability of human Cal27 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
|
32569675 |
| SCC-9 | IC50 |
6.26 μM
|
Reduction in cell viability of human SCC9 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
Reduction in cell viability of human SCC9 head and neck squamous cell carcinoma cells assessed after incubation for 72 hrs by resazurin assay.
|
32569675 |
| Jurkat | IC50 |
1.25 μM
|
Inhibition of cell viability in human JURKAT T-ALL cells assessed by MTS assay after 72 hrs incubation.
Inhibition of cell viability in human JURKAT T-ALL cells assessed by MTS assay after 72 hrs incubation.
|
27705940 |
| LOUCY | IC50 |
1.25 μM
|
Inhibition of cell viability in human LOUCY T-ALL cells assessed by MTS assay after 72 hrs incubation.
Inhibition of cell viability in human LOUCY T-ALL cells assessed by MTS assay after 72 hrs incubation.
|
27705940 |
| RPMI 8402 | IC50 |
1.25 μM
|
Inhibition of cell viability in human RPMI-8402 T-ALL cells assessed by MTS assay after 72 hrs incubation.
Inhibition of cell viability in human RPMI-8402 T-ALL cells assessed by MTS assay after 72 hrs incubation.
|
27705940 |
| MOLT-4 | IC50 |
1.25 μM
|
Inhibition of cell viability in human MOLT-4 T-ALL cells assessed by MTS assay after 72 hrs incubation.
Inhibition of cell viability in human MOLT-4 T-ALL cells assessed by MTS assay after 72 hrs incubation.
|
27705940 |
| K562 | IC50 |
2.5 μM
|
Cytotoxicity against human K562 CML cells assessed as reduction in proliferation and increased apoptosis.
Cytotoxicity against human K562 CML cells assessed as reduction in proliferation and increased apoptosis.
|
blood.V118.21.3757.3757 |
| BaF3 | IC50 |
0.89 μM
|
Inhibition of proliferation of murine Ba/F3 cells expressing wild-type BCR-ABL1 incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
Inhibition of proliferation of murine Ba/F3 cells expressing wild-type BCR-ABL1 incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
|
24436473 |
| BaF3 | IC50 |
1.62 μM
|
Inhibition of proliferation of murine Ba/F3 cells expressing imatinib-insensitive BCR-ABL1T315I point mutant incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
Inhibition of proliferation of murine Ba/F3 cells expressing imatinib-insensitive BCR-ABL1T315I point mutant incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
|
24436473 |
| BaF3 | IC50 |
1.97 μM
|
Inhibition of proliferation of murine Ba/F3 cells expressing BCR-ABL1E255V/T315I compound mutant incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
Inhibition of proliferation of murine Ba/F3 cells expressing BCR-ABL1E255V/T315I compound mutant incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
|
24436473 |
| K562 | IC50 |
0.60 μM
|
Inhibition of proliferation of human CML K562 cells incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
Inhibition of proliferation of human CML K562 cells incubated for 72 hrs by Cell Titer 96 Aqueous One solution assay.
|
24436473 |
| MOLM-14 | IC50 |
0.59 μM
|
Inhibition of proliferation of human AML MOLM-14 cells harboring FLT3-ITD incubated for 72 hrs by cell viability assay.
Inhibition of proliferation of human AML MOLM-14 cells harboring FLT3-ITD incubated for 72 hrs by cell viability assay.
|
24436473 |
| GDM-1 | IC50 |
0.82 μM
|
Inhibition of proliferation of human AML GDM-1 cells with CSF1R overexpression incubated for 72 hrs by cell viability assay.
Inhibition of proliferation of human AML GDM-1 cells with CSF1R overexpression incubated for 72 hrs by cell viability assay.
|
24436473 |
| HL-60 | IC50 |
0.94 μM
|
Inhibition of proliferation of human AML HL-60 cells harboring NRASQ61L incubated for 72 hrs by cell viability assay.
Inhibition of proliferation of human AML HL-60 cells harboring NRASQ61L incubated for 72 hrs by cell viability assay.
|
24436473 |
| CMK | IC50 |
1.73 μM
|
Inhibition of proliferation of human AML CMK cells harboring JAK3A572V incubated for 72 hrs by cell viability assay.
Inhibition of proliferation of human AML CMK cells harboring JAK3A572V incubated for 72 hrs by cell viability assay.
|
24436473 |
| UT7 | IC50 |
1.78 μM
|
Inhibition of proliferation of human AML UT7 cells incubated for 72 hrs by cell viability assay.
Inhibition of proliferation of human AML UT7 cells incubated for 72 hrs by cell viability assay.
|
24436473 |
In Vitro
COG449 (0-7.0 μM; 72 h) reduces cell viability in HN13, HN12, HN6, Cal27, and SCC9 OSCC cell lines with IC50 values of 5.94 μM, 5.11 μM, 9.17 μM, 8.86 μM, and 6.26 μM, respectively, and reduces viability in NOK-SI and NOK-SI/SET cells with IC50 values of 8.95 μM and 9.16 μM, respectively[1].
COG449 (72 h) inhibits the growth of NOTCH-dependent and -independent T-ALL cells with an IC50 of 1.25 μM at 72 h[2].
COG449 (1 μM) reduces total c-MYC and phospho-S62 c-MYC levels in RPMI-8402 and JURKAT T-ALL cells[2].
COG449 (1 μM) reduces the phosphorylation of ERK1/2 and AKT in RPMI-8402 and JURKAT cells[2].
COG449 (1 μM) negatively affects c-MYC transcriptional activity and reduces the levels of SET, CIP2A, and SETBP1 in T-ALL cells[2].
COG449 (1 μM) reduces tyrosine phosphorylation of PP2Ac in T-ALL cells[2].
COG449 (24 h) induces dose-dependent cytotoxicity in breast cancer cell lines and immortalized MCF10A cells[4].
COG449 significantly reduces the anchorage-independent growth of MDA-MB-231, HCC38, SKBR3, MDA-MB-436, and MDA-MB-468 breast cancer cells[4].
COG449 (1-2 μM; 4 h) reduces pS62-MYC levels in MDA-MB-231, HCC38, MDA-MB-436, and MDA-MB-468 breast cancer cells[4].
COG449 (1 µM) increases PP2A activity by 45% in K562 and 32Dp210 CML cells[5].
COG449 is cytotoxic to K562 and LAMA CML cells, with IC50 values of 2.5 µM and 1.25 µM, respectively[5].
COG449 exhibits selective cytotoxicity against BCR-ABL-positive CML cells[5].
COG449 is cytotoxic to the TKI-resistant 32Dp210T315I mutant cell line, with an IC50 of 2.5 µM[5].
COG449 (2.5-5 µM) inhibits colony formation in primary CML CD34+ cells without affecting normal human CD34+ cells[5].
COG449 (72 h) selectively inhibits the growth of Ba/F3 cells expressing wild-type and mutant BCR-ABL1, as well as K562 and LAMA CML cell lines, with IC50 values ranging from 0.60 to 1.97 μM, while showing no effect on parental Ba/F3 cells[6].
COG449 (2.5 μM) effectively inhibits the growth of primary CML blast crisis cells harboring wild-type BCR-ABL1 (90% inhibition) and BCR-ABL1T315I (35% inhibition)[6].
COG449 (10-20 μM; 2-6 h) alters multiple SET targets in HN12 and SCC9 cells and activates apoptosis and autophagy markers[1].
COG449 (10-20 μM; 2-6 h) modulates SET targets in NOK-SI and NOK-SI/SET cells and induces apoptosis and autophagy markers, with dose-dependent effects on histone H3 acetylation[1].
COG449 (0.62-1.25 μM) increases PP2A activity in a dose-dependent manner in JURKAT, LOUCY, RPMI-8402, and MOLT-4 T-ALL cell lines[2].
COG449 (1 μM) reduces the binding of SET to PP2Ac in T-ALL cell lines[2].
COG449 (1 μM) reduces the binding of phospho-S62 c-Myc to PP2Ac in T-ALL cells[2].
COG449 is a SET-targeting agent that activates PP2A and reduces Mcl-1 levels by disrupting the SET-PP2A complex, and has shown activity in B-CLL and non-Hodgkin lymphoma[3].
COG449 (48 h) induces apoptosis in mouse and human CML cell lines[6].
COG449 (6 h) induces apoptosis in MDA-MB-231 breast cancer cells[4].
COG449 (6 h) reduces CIP2a levels in CD34+ CML and K562 cells and inhibits BCR-ABL downstream signaling[5].
COG449 (24 h) attenuates BCR-ABL1 kinase signaling and leads to BCR-ABL1 degradation in K562 cells[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HN13, HN12, HN6, Cal27, SCC9
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Concentration:0, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 7.0 μM
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Incubation Time:72 h
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Result:Decreased cell viability in HN13, HN12, HN6, Cal27, and SCC9 cell lines in a dose-dependent manner.
Achieved IC50 values of 5.94 μM for HN13, 5.11 μM for HN12, 9.17 μM for HN6, 8.86 μM for Cal27, and 6.26 μM for SCC9.
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Cell Line:NOK-SI, NOK-SI/SET
-
Concentration:0, 0.5, 1.0, 2.0, 3.0, 4.0, 5.0, 7.0 μM
-
Incubation Time:72 h
-
Result:Decreased cell viability in NOK-SI and NOK-SI/SET cells.
Achieved IC50 values of 8.95 μM for NOK-SI and 9.16 μM for NOK-SI/SET.
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Cell Line:HN12, SCC9
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Concentration:10, 20 μM
-
Incubation Time:2, 4, 6 h
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Result:Induced a marked increase of p21 and reduction of pAKT308, pNFκB, and NFκB levels in HN12 cells.
Showed reduction of pNFκB, NFκB, and AKT, a decrease in ERK1/2 levels, and an increase of acetyl histone H3 levels in SCC9 cells.
Decreased PARP (full length) levels and increased LC3 lipidation (LC3-II) in both HN12 and SCC9 cells.
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Cell Line:NOK-SI, NOK-SI/SET
-
Concentration:10, 20 μM
-
Incubation Time:2, 4, 6 h
-
Result:Decreased the levels of pNFκB, NFκB, pAKT308, SET, and p53, and increased the levels of pERK and acetyl histone H3.
Increased the levels of acetyl-H3 histones at 10 μM, while 20 μM promoted a drastic reduction in these levels.
Reduced PARP (full length) in both cell lines.
Confirmed increased LC3 lipidation (LC3-II).
Observed an increase of LC3-II/LC3-I ratio in NOK-SI/SET cells.
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Cell Line:MDA-MB-231, HCC38, MDA-MB-436, and MDA-MB-468 cells
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Concentration:1, 2 μM (MDA-MB-231); 0.5, 1 μM (HCC38); 1, 2 μM (MDA-MB-436); 1, 2 μM (MDA-MB-468)
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Incubation Time:4 h
-
Result:Decreased pS62-MYC/GAPDH ratios from 1.0 to 0.72 (1 μM) and 0.50 (2 μM) in MDA-MB-231; from 1.0 to 0.64 (0.5 μM) and 0.54 (1 μM) in HCC38; from 1.0 to 0.70 (1 μM) and 0.42 (2 μM) in MDA-MB-436; from 1.0 to 0.60 (1 μM) and 0.39 (2 μM) in MDA-MB-468.
MYC/GAPDH ratios were 1.0, 1.13 (1 μM), and 1.08 (2 μM) in MDA-MB-231; 1.0, 1.05 (0.5 μM), and 1.17 (1 μM) in HCC38; 1.0, 0.78 (1 μM), and 0.56 (2 μM) in MDA-MB-436; 1.0, 0.68 (1 μM), and 0.38 (2 μM) in MDA-MB-468.
In Vivo
COG449 (5 mg/kg; i.p.; once every 3 days) significantly inhibits AML tumor growth in mice, reducing tumor burden by more than 2-fold compared with the vehicle control group[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:NOD/SCID/γ-chain null (NSG) (female, orthotopic xenografts of MDA-MB-231, MDA-MB-436, and MDA-MB-468 cells into the fourth mammary gland)[4]
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Dosage:5 mg/kg
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Administration:i.p.; three times per week; up to 40 days
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Result:Slowed tumor growth in MDA-MB-231, MDA-MB-436, and MDA-MB-468 xenografts compared with controls.
Increased the number of apoptotic cells in MDA-MB-231 tumors as measured by TUNEL assay.
Decreased the number of proliferating cells in MDA-MB-231 tumors as measured by Ki67 staining.
Was specifically detected in the tumors of treated mice.
Significantly increased PP2A activity in treated tumors compared with PBS-treated tumors.
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Animal Model:RAG2−/− γc−/− mice (20 g)[6]
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Dosage:5 mg/kg
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Administration:i.p.; every 3 days; starting 7 days post-implantation
-
Result:Inhibited tumor growth measured over time.
Reduced tumor burden by more than 2-fold compared with vehicle-treated controls, with final tumor mass of 0.45 g versus 1.14 g for vehicle.
Chemical Information
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Molecular Weight 9223.31
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Formel C418H712N146O82S4
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SMILES
O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCCCN)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC1=CNC2=CC=CC=C12)C(N[C@@H](CC3=CC=CC=C3)C(N[C@@H](CCC(N)=O)C(N[C@@H](CC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCSC)C(N[C@@H](CCCCN)C(N[C@@H](CC4=CNC5=CC=CC=C45)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CSC(C6=O)CC(N6CCN7C(CC(SC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)CCC(N)=O)=O)[C@H](CC)C)=O)CCCCN)=O)[C@H](CC)C)=O)CC8=CNC9=CC=CC=C98)=O)CC%10=CC=CC=C%10)=O)CCC(N)=O)=O)CC(N)=O)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCSC)=O)CCCCN)=O)CC%11=CNC%12=CC=CC=C%12%11)=O)CCCCN)=O)CCCCN)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N)=O)CCCCN)=O)CCCNC(N)=N)=O)CC(C)C)=O)CCCCN)=O)CCCNC(N)=N)=O)CC(C)C)=O)CC%13=CNC=N%13)=O)CO)=O)C)=O)CC(C)C)=O)CCCNC(N)=N)=O)C(C)C)=O)CCCNC(N)=N)=O)CC(C)C)=O)C7=O)=O)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(N[C@@H](CO)C(N[C@@H](CC%14=CNC=N%14)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)C
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Synonyms
OP449
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Sequence
Ac-Arg-Gln-Ile-Lys-Ile-Trp-Phe-Gln-Asn-Arg-Arg-Met-Lys-Trp-Lys-Lys-Cys-Leu-Arg-Val-Arg-Leu-Ala-Ser-His-Leu-Arg-Lys-Leu-Arg-Lys-Arg-Leu-Leu-NH2 (BMOE-linked Cys17 dimer)
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Sequence Shortening
Ac-RQIKIWFQNRRMKWKKCLRVRLASHLRKLRKRLL-NH2 (BMOE-linked Cys17 dimer)
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- COG449
- OP449
- COG 449
- COG-449
- OP 449
- OP-449
- Phosphatase
- Akt
- ERK
- NF-κB
- c-Myc
- Apoptosis
- Autophagy
- Histone Acetyltransferase
- SET antagonist
- SET-PP2A complex
- chronic myeloid leukemia
- histone H3 hyperacetylation
- T-cell acute lymphoblastic leukemia
- oral squamous cell carcinoma
- apoptosis
- autophagy
- PP2A phosphatase activity
- PP2A activator
- Inhibitor
- inhibitor
- inhibit