SP-6-27
SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 1384170-58-4
- Formula: C24H24N4O
- Molecular Weight:384.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
|
Bax |
Caspase 3 |
Caspase-6 |
Caspase-9 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A 172 | IC50 |
7.4 nM
Compound: 4e
|
Antiproliferative activity against human A172 cells after 5 days by MTT assay
Antiproliferative activity against human A172 cells after 5 days by MTT assay
|
[PMID: 22608389] |
| A-375 | IC50 |
0.08 μM
Compound: 4e
|
Antiproliferative activity against human A375 cells after 48 hrs by SRB assay
Antiproliferative activity against human A375 cells after 48 hrs by SRB assay
|
[PMID: 22608389] |
| Astrocyte | IC50 |
2033 nM
Compound: 4e
|
Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay
Cytotoxicity against mouse primary astrocytes after 5 days by MTT assay
|
[PMID: 22608389] |
| LN-18 | IC50 |
13.3 nM
Compound: 4e
|
Antiproliferative activity against human LN18 cells after 5 days by MTT assay
Antiproliferative activity against human LN18 cells after 5 days by MTT assay
|
[PMID: 22608389] |
| LNCaP | IC50 |
0.14 μM
Compound: 4e
|
Antiproliferative activity against human LNCAP cells after 96 hrs by SRB assay
Antiproliferative activity against human LNCAP cells after 96 hrs by SRB assay
|
[PMID: 22608389] |
| PC-3 | IC50 |
0.22 μM
Compound: 4e
|
Antiproliferative activity against human PC3 cells after 96 hrs by SRB assay
Antiproliferative activity against human PC3 cells after 96 hrs by SRB assay
|
[PMID: 22608389] |
| T98G | IC50 |
12.5 nM
Compound: 4e
|
Antiproliferative activity against human T98G cells after 5 days by MTT assay
Antiproliferative activity against human T98G cells after 5 days by MTT assay
|
[PMID: 22608389] |
| U-87MG ATCC | IC50 |
20.6 nM
Compound: 4e
|
Antiproliferative activity against human U87 cells after 5 days by MTT assay
Antiproliferative activity against human U87 cells after 5 days by MTT assay
|
[PMID: 22608389] |
| WM164 | IC50 |
0.16 μM
Compound: 4e
|
Antiproliferative activity against human WM164 cells after 48 hrs by SRB assay
Antiproliferative activity against human WM164 cells after 48 hrs by SRB assay
|
[PMID: 22608389] |
SP-6-27 (0.001-10 μM; 72 h) potently inhibits proliferation in Cisplatin-sensitive and resistant ovarian cancer cells and exhibits minimal cytotoxicity to normal HOSEpiC cells (IC50 = 0.10-0.84 μM for OVCA cells, 83.35 μM for HOSEpiC cells)[1].
SP-6-27 (0.5 μM; 24 h) disrupts alpha-tubulin and beta-tubulin cytoskeletal structure, reducing microtubule density in ovarian cancer cells[1].
SP-6-27 (0.5 μM; 48 h) reduces migration in ovarian cancer cells (A2780)[1].
SP-6-27 (0.5 μM; 24 h) induces G2-M cell cycle arrest in Cisplatin-sensitive and resistant ovarian cancer cells[1].
SP-6-27 (0.5 μM; 24-48 h) induces apoptosis in Cisplatin-sensitive and resistant ovarian cancer cells[1].
SP-6-27 upregulates pro-apoptotic genes (Bax, PAF-1, caspase-9, caspase-6, Caspase-3) and GADD45A in ovarian cancer cells[1].
SP-6-27 (0.5 μM; 24-48 h) enhances cytotoxicity in Cisplatin-sensitive cells when treated simultaneously with Cisplatin and in Cisplatin-resistant cells when treated sequentially[1].
SP-6-27 (0.5-1 μM; 24 h) inhibits capillary tube formation by HUVECs, even in the presence of tumor conditioned media[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:cisplatin-sensitive OVCA (A2780, SKOV-3, TOV-112D), cisplatin-resistant OVCA (OVCAR-3, cis-A2780, cis-TOV-112D), HOSEpiC
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Concentration:0.001-10 μM
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Incubation Time:72 h
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Result:Exhibited potent cytotoxicity against Cisplatin-sensitive OVCA cells with a mean IC50 of 0.14 μM and against cisplatin-resistant OVCA cells with a mean IC50 of 0.36 μM; showed minimal cytotoxicity with an IC50 of 83.35 μM in normal HOSEpiC cells.
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Cell Line:A2780 OVCA cells
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Concentration:0.5 μM
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Incubation Time:48 h
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Result:Reduced migration compared to control cells when monitored over 48 h.
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Cell Line:Cisplatin-sensitive A2780 and Cisplatin-resistant cis-A2780 OVCA cells
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Concentration:0.5 μM
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Incubation Time:24 h
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Result:Caused a complete collapse of cells in G1 phase and a substantial increase in G2-M phase cells: 87.8% of A2780 cells were arrested in G2-M phase (vs. 16.40% in control) and 58.9% of cis-A2780 cells were arrested in G2-M phase (vs. 14.5% in control).
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Cell Line:Cisplatin-sensitive A2780 and Cisplatin-resistant cis-A2780 OVCA cells
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Concentration:0.5 μM
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Incubation Time:24 h (caspase-3 microscopy); 24, 48 h (Annexin V/7-AAD)
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Result:Caused a pronounced increase in Annexin-V positive cells (early/late apoptotic) in both cell types at 24 and 48 h; showed increased cleaved caspase-3 activity in A2780 cells compared to control cells.
Chemical Information
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CAS No. 1384170-58-4
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Molecular Weight 384.48
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Formula C24H24N4O
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SMILES
N#CC1=C(OC2=CC(=CC=C2C1C=3C=CC(=C4C=CC=CC43)N(C)C)N(C)C)N
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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)
- SP-6-27
- 1384170-58-4
- Microtubule/Tubulin
- Apoptosis
- Caspase
- Bcl-2 Family
- caspase-6
- intrinsic apoptosis
- cytoskeletal structure
- alpha-tubulin
- capillary tube formation
- Apaf-1
- ovarian cancer cell migration
- GADD45A
- HOSEpiC cells
- tumor conditioned media
- human cisplatin sensitive and resistant ovarian cancer cell lines
- cisplatin sensitive/resistant ovarian cancer cells
- Bax
- colchicine site
- human umbilical vein endothelial cells
- tubulin
- HUVECs
- caspase-3
- normal ovarian epithelia
- G2/M cell cycle arrest
- cisplatin
- beta-tubulin
- pro-apoptotic genes
- caspase-9
- microtubule density
- Inhibitor
- inhibitor
- inhibit