Sino-C
Sino-C is a Sinomenine (HY-15122) derivative with anticancer activity. Sino-C broadly disrupts cholesterol homeostasis by upregulating key genes such as SREBF2 and HMGCS1, leading to intracellular cholesterol accumulation and lipid droplet formation. Sino-C-induced metabolic dysregulation further triggers lipid peroxidation and endoplasmic reticulum (ER) stress, initiating a unique form of hybrid cell death including apoptotic (cleaved PARP) and necrotic-like features. Sino-C thus serves as a useful compound for research in colorectal cancer, lung cancer and breast cancer.
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- Formule: C25H25Cl2NO4S
- Masse moléculaire:506.44
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Sino-C (0-20 μM, 48 h) exhibits broad-spectrum anticancer activity in CRC (HCT116, RKO, and MC38), lung cancer (A549 and NCI-H1299), and breast cancer (MDA-MB-231 and 4T1) cells[1].
Sino-C (0-20 μM, 24 h) exhibits significant anti-CRC effect in HCT116 and RKO cells[1].
Sino-C (0-20 μM, 24 h) induces HCT116 and RKO cell death, characterized by PARP cleavage without caspase-3 activation, causes severe morphological alterations (widened perinuclear spaces, extensive ER dilation with ribosome detachment, mitochondrial swelling) along with significant LDH leakage and membrane injury, suggesting a non-apoptotic mechanism[1].
Sino-C (24 h) elicits a unique form of cell death: the morphological features do not match those of classical apoptosis, paraptosis, pyroptosis, or ferroptosis, but instead represent a hybrid mode combining both apoptotic and necrotic-like characteristics in HCT116 cells[1].
Sino-C (0-20 μM, 24 h) upregulates cholesterol homeostasis-related genes, elevates intracellular cholesterol levels, and induces lipid droplet accumulation in HCT116 cells[1].
Sino-C (0-20 μM, 24 h) induces cholesterol dysregulation, which leads to lipid peroxidation and subsequently triggers endoplasmic reticulum (ER) stress, ultimately contributing to CRC cell death[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, RKO, MC38, A549, NCI-H1299, MDA-MB-231, 4T1
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Concentration:1.25, 2.5, 5, 10 and 20 μM
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Incubation Time:48 h
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Result:Significantly reduced cell viability in all tested cell lines in a dose-dependent manner, with IC50 values predominantly below 10 μM.
Showed greater potency against CRC cell lines, with IC50 values of 5.15 μM (HCT116), 9.72 μM (RKO), and 4.58 μM (MC38).
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Cell Line:HCT116 and RKO cells
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Concentration:0, 5, 10 and 20 μM
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Incubation Time:24 h
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Result:Remarkably inhibited the colony formation of HCT116 and RKO cells.
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Cell Line:HCT116 and RKO cells
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Concentration:0, 5, 10 and 20 μM
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Incubation Time:24 h
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Result:Revealed a dose-dependent increase in apoptosis: from 5.81% (control) to 26.80% (20 μM) in HCT116 cells from 5.39% to 22.34% in RKO cells.
Had minimal Annexin V+ staining in both cell lines, indicating a limited externalization of phosphatidylserine on the plasma membrane.
Increased in PI+ stained cells upon Sino-C treatment, suggesting that apoptosis may not be the only cell death mode.
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Cell Line:HCT116 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Upregulated key genes involved in cholesterol homeostasis, including the master transcriptional Regulator of cholesterol biosynthesis, SREBF2, as well as rate-limiting enzymes and a key Receptor in the pathway, such as HMGCS1, SQLE, and LDLR.
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Cell Line:HCT116 cells
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Concentration:5, 10 and 20 μM
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Incubation Time:24 h
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Result:Markedly elevated intracellular cholesterol levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 cells (1 × 106, s.c.) induce- BALB/c nude mice[1]
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Dosage:30 and 50 mg/kg
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Administration:i.t., every other day from day 14 to day 22 (30 mg/kg) then i.t., every other day from day 24 to day 28 (50 mg/kg)
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Result:Significantly reduced tumor size and average tumor weight by approximately 43.24%.
Suppressed tumor growth over the two-week study period.
Caused no significant changes in mouse body weight, indicating minimal systemic toxicity.
Chemical Information
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Masse moléculaire 506.44
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Formule C25H25Cl2NO4S
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SMILES
O=C1C[C@@]2(CCN3C)C4=C(O)C(O)=CC=C4[C@@H](SCC5=CC=C(Cl)C=C5Cl)[C@@]3([H])C2C=C1OC
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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
Références
[1]. Zhang YM, et al. Sino-C, a novel sinomenine derivative, induces cell death bya novel sinomenine derivative, induces cell death by disrupting cholesterol homeostasis in colorectal cancer cells. Acta Pharmacol Sin. 2025 Nov 3. doi: 10.1038/s41401-025-01683-8. Epub ahead of print. PMID: 41184618. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sino-C Related Classifications
HY-179526 Related Classifications
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