Schisanlactone B
Schisanlactone B is a glutathione S-transferase (GST) inhibitor with an IC50 of 5 μM. Schisanlactone B binds to GST and inhibits its enzymatic activity. Schisanlactone B induces apoptosis and cell cycle arrest. Schisanlactone B can be used in research related to various cancers such as hepatocellular carcinoma, leukemia, melanoma, lung cancer, gastric cancer, and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 87164-32-7
- Formula: C30H42O4
- Molecular Weight:466.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
GST 5 μM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
34.72 μM
|
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human HL-60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
16557460 |
| Bel-7402 | IC50 |
100 μM
|
Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
16557460 |
| CCRF-CEM | IC50 |
4.66 μg/mL
|
Cytotoxic activity against murine leukemia CCRF-CEM cells assessed as reduction in cell viability incubated for 24 hrs by crystal violet protein staining method.
Cytotoxic activity against murine leukemia CCRF-CEM cells assessed as reduction in cell viability incubated for 24 hrs by crystal violet protein staining method.
|
14661856 |
| HeLa | IC50 |
46.6 μg/mL
|
Cytotoxic activity against human Hela cells assessed as reduction in cell viability incubated for 24 hrs by crystal violet protein staining method.
Cytotoxic activity against human Hela cells assessed as reduction in cell viability incubated for 24 hrs by crystal violet protein staining method.
|
14661856 |
| NCI-H23 | GI50 |
1.28 μM
|
Antiproliferative activity against human NCI-H23 lung cancer cells assessed as reduction in cell growth by SRB assay.
Antiproliferative activity against human NCI-H23 lung cancer cells assessed as reduction in cell growth by SRB assay.
|
34075849 |
| NUGC-3 | GI50 |
1.80 μM
|
Antiproliferative activity against human NUGC-3 stomach cancer cells assessed as reduction in cell growth by SRB assay.
Antiproliferative activity against human NUGC-3 stomach cancer cells assessed as reduction in cell growth by SRB assay.
|
34075849 |
| PC-3 | GI50 |
2.33 μM
|
Antiproliferative activity against human PC-3 prostate cancer cells assessed as reduction in cell growth by SRB assay.
Antiproliferative activity against human PC-3 prostate cancer cells assessed as reduction in cell growth by SRB assay.
|
34075849 |
| MDA-MB-231 | GI50 |
2.38 μM
|
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell growth by SRB assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as reduction in cell growth by SRB assay.
|
34075849 |
| ACHN | GI50 |
2.63 μM
|
Antiproliferative activity against human ACHN renal cancer cells assessed as reduction in cell growth by SRB assay.
Antiproliferative activity against human ACHN renal cancer cells assessed as reduction in cell growth by SRB assay.
|
34075849 |
| HCT-15 | GI50 |
2.67 μM
|
Antiproliferative activity against human HCT-15 colon cancer cells assessed as reduction in cell growth by SRB assay.
Antiproliferative activity against human HCT-15 colon cancer cells assessed as reduction in cell growth by SRB assay.
|
34075849 |
| A549 | GI50 |
17.47 μM
|
Cytotoxicity against human lung carcinoma A549 cells assessed as growth inhibition incubated for 72 hrs by sulforhodamine B colorimetric assay.
Cytotoxicity against human lung carcinoma A549 cells assessed as growth inhibition incubated for 72 hrs by sulforhodamine B colorimetric assay.
|
23883077 |
| PC-3 | GI50 |
18.09 μM
|
Cytotoxicity against human prostate carcinoma PC-3 cells assessed as growth inhibition incubated for 72 hrs by sulforhodamine B colorimetric assay.
Cytotoxicity against human prostate carcinoma PC-3 cells assessed as growth inhibition incubated for 72 hrs by sulforhodamine B colorimetric assay.
|
23883077 |
| KB | GI50 |
15.02 μM
|
Cytotoxicity against human epidermoid carcinoma of the nasopharynx KB cells assessed as growth inhibition incubated for 72 hrs by sulforhodamine B colorimetric assay.
Cytotoxicity against human epidermoid carcinoma of the nasopharynx KB cells assessed as growth inhibition incubated for 72 hrs by sulforhodamine B colorimetric assay.
|
23883077 |
In Vitro
Schisanlactone B (C1) (5-10 μM; 24 h) down-regulates intracellular GST protein levels in a concentration-dependent manner in both HepG2 and HepG2/DDP cells[1].
Schisanlactone B (10 μM; 6 h), in combination with Cisplatin, increases ROS levels in both HepG2 and HepG2/DDP cells[1].
Schisanlactone B (20 μM; 30 min) is a natural GST inhibitor that inhibits purified GST activity with an IC50 of 5 μM, binding to GST via Van der Waals interactions at PRO A:73 and GLU A:85[1].
Schisanlactone B (C1) (5 μM; 24 h) effectively reduces intracellular GST levels in both HepG2/DDP and HepG2 cells, as demonstrated by decreased fluorescence imaging signals[1].
Schisanlactone B (2.5-20 μM; 48 h) decreases cell viability in a concentration-dependent manner in HepG2 (IC50 = 17.2 μM) and HepG2/DDP (IC50 = 14.3 μM) cells[1].
Schisanlactone B (Compound 13) (1 nM-100 μM; 48 h) exhibits cytotoxic activity against HL-60 cells with an IC50 of 34.72 μM, and shows no activity against Bel-7402, BGC-823, and MCF-7 cell lines[2].
Schisanlactone B (Compound 2) (0.5-100 µg/mL; 24 h) exhibits moderate cytotoxic activity against murine leukemia (CCRF-CEM) cells with an IC50 of 4.66 µg/mL and against Hela cells with an IC50 of 46.6 µg/mL[3].
Schisanlactone B (compound 6) exhibits potent antiproliferative activity against NCI-H23, HCT-15, NUGC-3, ACHN, PC-3, and MDA-MB-231 human cancer cell lines with GI50 values in the low micromolar range[4].
Schisanlactone B (up to 20 mg/mL; 72 h) exhibits moderate cytotoxicity against A549, PC-3, KB and KBvin human cancer cell lines with GI50 values ranging from 15.02 to 18.09 μM[6].
Schisanlactone B (7.5 μM; 48 h) induces apoptosis in a concentration-dependent manner in HepG2 and HepG2/DDP cells[1].
Schisanlactone B (5-10 μM; 24 h) modulates apoptosis-related protein expression by increasing C-caspase-3 and Bax and decreasing P-caspase 3 and Bcl-2 in HepG2/DDP cells[1].
Schisanlactone B (10 μM; 48 h), in combination with Cisplatin (HY-17394), induces cell cycle arrest at G2 phase in HepG2 cells and G1 phase in HepG2/DDP cells[1].
Schisanlactone B (10 μM; 24 h), in combination with Cisplatin, induces mitochondrial membrane damage, with stronger effects in HepG2/DDP cells compared to HepG2 cells[1].
Schisanlactone B (10 μM; 24 h) regulates mitochondrial apoptosis-related proteins (caspase 3, Bax, Bcl-2, Cyt C) and down-regulates GST expression in both HepG2 and HepG2/DDP cells[1].
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:HepG2/DDP and HepG2
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Concentration:5 μM; 10 μM
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Incubation Time:24 h
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Result:Down-regulated GST protein levels in a concentration-dependent manner in both HepG2 and HepG2/DDP cells.
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Cell Line:HepG2/DDP and HepG2
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Concentration:5 μM
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Incubation Time:24 h (C1); 30 min (NEM); 20 min (staining)
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Result:Reduced intracellular GST levels in both HepG2/DDP and HepG2 cells, as demonstrated by decreased fluorescence imaging signals.
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Cell Line:HepG2 and HepG2/DDP
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Concentration:2.5 μM; 5 μM; 7.5 μM; 10 μM; 15 μM; 20 μM
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Incubation Time:48 h (C1); 4 h (MTT)
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Result:Decreased cell viability in a concentration-dependent manner in HepG2 and HepG2/DDP cells with an IC50 of 17.2 μM in HepG2 and an IC50 of 14.3 μM in HepG2/DDP cells.
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Cell Line:HepG2 and HepG2/DDP
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Concentration:7.5 μM
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Incubation Time:48 h
-
Result:Induced apoptosis in a concentration-dependent manner in both HepG2 and HepG2/DDP cells.
Exhibited a higher apoptotic rate in HepG2/DDP cells (18.9%) compared to HepG2 cells (13.8%) at 7.5 μM.
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Cell Line:HepG2/DDP and HepG2
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Concentration:5 μM; 7.5 μM; 10 μM
-
Incubation Time:24 h
-
Result:Increased the levels of cleaved caspase-3 (C-caspase-3) and Bax, but decreased the expression of P-caspase 3 and Bcl-2 in HepG2/DDP cells.
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Cell Line:HepG2 and HepG2/DDP
-
Concentration:10 μM
-
Incubation Time:48 h
-
Result:Induced cell cycle arrest at G2 phase in HepG2 cells and G1 phase in HepG2/DDP cells in combination with Cisplatin.
-
Cell Line:HepG2 and HepG2/DDP
-
Concentration:10 μM
-
Incubation Time:24 h
-
Result:Induced mitochondrial membrane damage in combination with Cisplatin, with stronger effects in HepG2/DDP cells compared to HepG2 cells.
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Cell Line:HepG2 and HepG2/DDP
-
Concentration:10 μM
-
Incubation Time:24 h
-
Result:Regulated mitochondrial apoptosis-related proteins (caspase 3, Bax, Bcl-2, Cyt C) and down-regulated GST expression in both HepG2 and HepG2/DDP cells.
In Vivo
C1 (10 mg/kg; i.p.; once every 2 days; 16 days) achieves a tumor inhibition rate of 19.4% in HepG2/DDP tumor-bearing mice, and C1 (5 mg/kg) combined with Cisplatin (2.5 mg/kg) achieves a tumor inhibition rate of 71.7%, demonstrating effective sensitization of Cisplatin-resistant HCC to Cisplatin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/C nude mice (female, 6-8 weeks, 18-20 g)[1]
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Dosage:5 mg/kg
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Administration:in situ injection; single dose
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Result:Down-regulated GST levels in vivo in both Cisplatin-resistant (HepG2/DDP) and Cisplatin-sensitive (HepG2) hepatocellular carcinoma mouse models.
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Animal Model:BALB/C nude mice (female)[1]
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Dosage:10 mg/kg (monotherapy); 5 mg/kg (combination with Cisplatin)
-
Administration:i.p.; once every 2 days; 16 days
-
Result:Achieved a tumor inhibition rate of 19.4% as a single agent.
Achieved a tumor inhibition rate of 71.7% in combination with Cisplatin (2.5 mg/kg).
Induced extensive cell death and mitochondrial apoptosis by up-regulating Bax, C-caspase 3, and Cyt C and down-regulating Bcl-2 and GST.
Chemical Information
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CAS No. 87164-32-7
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Molecular Weight 466.66
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Formula C30H42O4
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SMILES
C[C@]12[C@]3([C@]4([C@]5(C4)[C@@](CC3)(C(C)(C)OC(=O)C=C5)[H])CC[C@]1(C)[C@@]([C@H](C)[C@]6(OC(=O)C(C)=CC6)[H])(CC2)[H])[H]
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Structure Classification
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Initial Source
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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.
Protocols
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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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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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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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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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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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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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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.
Purity & Documentation
References
[2]. Wang W, et al. New triterpenoids from Kadsura heteroclita and their cytotoxic activity. Planta medica. 2006 Apr;72(5):450-7. [Content Brief]
[6]. Lu Y, et al. Cytotoxic and potential anticancer constituents from the stems of Schisandra pubescens. Pharmaceutical biology. 2013 Sep;51(9):1204-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)