GO-Y078
GO-Y078 is a curcumin (HY-N0005) analog. GO-Y078 activates p38/JNK1/2. GO-Y078 activates the MAPK pathway, Caspase 3/8/9, PARP, AP-1, DR5, and TP53, while inhibiting cIAP-1, XIAP, and NF-κB. GO-Y078 induces sub-G1/G2/M phase arrest and Apoptosis. GO-Y078 impairs angiogenesis. GO-Y078 can be used in research related to osteosarcoma, cervical cancer, oral squamous cell carcinoma, and peritoneal metastasis of gastric cancer.
For research use only. We do not sell to patients.
- CAS No.: 1217503-60-0
- Formula: C22H24O7
- Molecular Weight:400.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
cIAP-1 |
XIAP |
Caspase 3 |
Caspase 8 |
Caspase 9 |
JNK1 |
JNK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SiHa | IC50 |
7.76 μM
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Inhibition of cell viability against human cervical squamous cell carcinoma SiHa cells assessed via MTT-based colorimetric assay after 24 h incubation.
Inhibition of cell viability against human cervical squamous cell carcinoma SiHa cells assessed via MTT-based colorimetric assay after 24 h incubation.
|
42059340 |
| HeLa | IC50 |
11.94 μM
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Inhibition of cell viability against human cervical adenocarcinoma HeLa cells assessed via MTT-based colorimetric assay after 24 h incubation.
Inhibition of cell viability against human cervical adenocarcinoma HeLa cells assessed via MTT-based colorimetric assay after 24 h incubation.
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42059340 |
In Vitro
GO-Y078 (1-16 μM; 24 h) reduces the viability of osteosarcoma U2OS, MG-63, 143B and Saos-2 cells in a dose-dependent manner. After 24 h of treatment, the inhibitory effect is the strongest at the concentration of 16 μM (the viability of U2OS cells decreases by 54.7%, that of MG-63 cells by 79.6%, that of 143B cells by 58.9%, and that of Saos-2 cells by 71.6%)[1].
GO-Y078 (2.5-40 μM; 24 h) inhibits the viability of cervical squamous cell carcinoma SiHa cells and cervical adenocarcinoma HeLa cells, with an IC50 of 7.76 μM for the former and 11.94 μM for the latter[2].
GO-Y078 (0.5-4 μM; 24 h) potently inhibits the viability of SCC-9 and HSC-3 oral squamous cell carcinoma cells, with an IC50 of <4 μM, and exhibits stronger cytotoxic potency than DMC[3].
GO-Y078 (1-8 μM; 24 h) induces sub-G1 phase cell cycle arrest in osteosarcoma U2OS and 143B cells. After treatment with 8 μM for 24 h, the proportion of sub-G1 phase cells increases to 24.3% in U2OS cells and to 26.9% in 143B cells[1].
GO-Y078 (1-8 μM; 24 h) induces apoptosis in osteosarcoma U2OS and 143B cells in a dose-dependent manner. After 24 h of treatment, the proportion of Annexin V-positive cells increases to approximately 35% in U2OS cells and to approximately 50% in 143B cells at the concentration of 8 μM[1].
GO-Y078 (1-8 μM; 24 h) reduces the expression of anti-apoptotic proteins cIAP-1 and XIAP in osteosarcoma U2OS and 143B cells in a dose-dependent manner, while upregulating the level of pro-apoptotic activated caspase-3 in U2OS cells after 24 h of treatment[1].
GO-Y078 (1-8 μM; 24 h) activates the ERK1/2, JNK1/2 and p38 MAPK signaling pathways in osteosarcoma U2OS and 143B cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human osteosarcoma U2OS, MG-63, 143B, and Saos-2 cells
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Concentration:1-16 μM
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Incubation Time:24 h
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Result:Reduced cell viability in a dose-dependent manner across all four cell lines.
Reduced U2OS cell viability by 41.5% at 8 μM and 54.7% at 16 μM.
Reduced MG-63 cell viability by 39.9% at 8 μM and 79.6% at 16 μM.
Reduced 143B cell viability by 51.8% at 8 μM and 58.9% at 16 μM.
Reduced Saos-2 cell viability by 57.4% at 8 μM and 71.6% at 16 μM.
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Cell Line:human osteosarcoma U2OS and 143B cells
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Concentration:1-8 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent increase in the sub-G1 cell fraction in both cell lines.
Increased U2OS sub-G1 fraction from 4.7% (control) to 24.3% at 8 μM.
Increased 143B sub-G1 fraction from 5.2% (control) to 26.9% at 8 μM.
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Cell Line:human osteosarcoma U2OS and 143B cells
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Concentration:1-8 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent increase in total Annexin V-positive (early + late apoptotic) cells in both cell lines.
Increased U2OS Annexin V-positive cells to ~35% at 8 μM.
Increased 143B Annexin V-positive cells to ~50% at 8 μM.
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Cell Line:human osteosarcoma U2OS and 143B cells
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Concentration:8 μM (apoptosis array); 1-8 μM (Western blot)
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Incubation Time:24 h (apoptosis array); 24 h (Western blot)
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Result:Increased cleaved caspase-3 levels and decreased cIAP-1 and XIAP levels in U2OS cells at 8 μM (apoptosis array).
Caused dose-dependent reductions in cIAP-1 and XIAP expression in both U2OS and 143B cells.
Reduced U2OS cIAP-1 to near 0% and XIAP to near 10% of control levels at 8 μM.
Reduced 143B cIAP-1 to ~20% and XIAP to ~40% of control levels at 8 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KSN/Slc (nu/nu) (6-week-old male, peritoneal carcinomatosis model established by intraperitoneal inoculation of GCIY gastric cancer cells)[5]
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Dosage:133 mg/kg; 266 mg/kg
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Administration:i.p.
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Result:Suppressed ascites fluid accumulation completely, with average body weight of 29.1 g at 17 days after first treatment.
Increased median survival time to 30.5 days, representing an approximate 40% increase in survival time.
Extended survival time range to 25 to 109 days.
Chemical Information
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CAS No. 1217503-60-0
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Molecular Weight 400.43
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Formula C22H24O7
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SMILES
O(C)C1=C(OC)C(OC)=CC(/C=C/C(/C=C/C2=CC(OC)=C(O)C(OC)=C2)=O)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- GO-Y078
- 1217503-60-0
- Drug Derivative
- p38 MAPK
- JNK
- Caspase
- PARP
- AP-1
- TNF Receptor
- MDM-2/p53
- IAP
- NF-κB
- Apoptosis
- MAPK pathway
- oral squamous cell carcinoma
- human osteosarcoma U2OS cells
- human cervical squamous cell carcinoma SiHa cells
- osteosarcoma
- p38
- cell cycle arrest
- JNK1/2
- apoptosis
- cervical cancer
- Inhibitor
- inhibitor
- inhibit