BCS12
Based on 1 Customer Validation
BCS12 is a CAIX inhibitor. BCS12 inhibits the viability of cancer cells under hypoxic conditions. BCS12 elevates ROS levels and suppresses the expression of HIF-1α and CA9. BCS12 downregulates Bcl-2, activates caspase-9, caspase-3, caspase-7 and Bax, and induces PARP cleavage and apoptosis. BCS12 reduces tumor burden, increases the number of apoptotic nuclei and restores tissue structure in rats bearing breast tumors. BCS12 can be used in research related to triple-negative breast cancer.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 329719-71-3
- Formula: C17H16ClNO2S
- Molecular Weight:333.83
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
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CA IX |
Caspase 9 |
Bax |
Caspase 3 |
Caspase-7 |
Bcl-2 |
HIF-1α |
BCS12 (96 h) selectively inhibits the viability of triple-negative breast cancer cells MDA-MB-231 and MDA-MB-468 under hypoxic conditions (IC50 = 15.49 µM and 18.81 µM), while showing extremely low toxicity toward non-tumorigenic MCF-10A cells (IC50 = 121.6 µM)[1].
BCS12 (5-10 µM; 14 days) dose-dependently inhibits the clonogenic survival capacity of MDA-MB-231 and MDA-MB-468 cells[1].
BCS12 (20 µM) inhibits hypoxia-induced expression of HIF-1α and CAIX proteins in MDA-MB-231 and MDA-MB-468 cells[1].
BCS12 (2-20 µM; 24 h) dose-dependently increases the ROS level in MDA-MB-231 cells, with the strongest effect observed at 20 µM[1].
BCS12 (5-20 µM; 24 h) dose-dependently regulates the expression of apoptotic proteins in MDA-MB-231 cells, downregulates the anti-apoptotic protein Bcl-2, activates the pro-apoptotic caspase-9 and caspase-3, and induces PARP cleavage. It also induces apoptosis in MDA-MB-231 cells under hypoxic conditions, upregulates the expression of pro-apoptotic genes Bax, caspase-9, caspase-3 and caspase-7, and downregulates the anti-apoptotic gene Bcl-2 as well as hypoxia-related CA9 and HIF-1α[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-468 triple-negative breast cancer cells
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Concentration:0, 5, 10 µM
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Incubation Time:14 days
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Result:Caused a dose-dependent decrease in colony formation in both cell lines, with MDA-MB-231 showing significantly reduced clonogenic survival at 10 µM compared to controls.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:5, 10, 20 µM
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Incubation Time:24 h
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Result:Caused a dose-dependent reduction in anti-apoptotic Bcl-2 protein levels.
Increased cleaved caspase-9, cleaved caspase-3, and cleaved PARP protein levels, indicating activation of the intrinsic apoptotic cascade.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells (hypoxic conditions)
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Concentration:1, 2, 5, 10, 20 µM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in total apoptosis (Annexin V+/PI+ cells): 1 µM (4.43%, ns vs control), 2 µM (10.0%), 5 µM (16.9%), 10 µM (20.5%), and 20 µM (37.0%,).
Produced a 19-fold increase in apoptosis at 20 µM compared to DMSO-treated controls.
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Cell Line:MDA-MB-231 triple-negative breast cancer cells
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Concentration:10, 20 µM
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Incubation Time:24 h
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Result:Caused a dose-dependent increase in Bax, caspase-9, and caspase-7 fluorescence intensity, indicating upregulation and activation of these pro-apoptotic proteins.
Significantly reduced Bcl-2 fluorescence intensity.
Induced nuclear condensation and fragmentation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (female nulliparous, virgin, 50-60 days old, 120-150 grams, acclimatized for 1 week before study, DMBA-induced breast cancer)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:i.p.; daily; 28 days
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Result:Suppressed DMBA-induced body weight loss in a dose-dependent manner.
Produced a significant, dose-dependent reduction in tumor volume, with the 40 mg/kg group showing the greatest reduction over the 28-day treatment period.
Increased apoptotic nuclei in a dose-dependent manner: reached 22.8 TUNEL-positive cells/field at 20 mg/kg, and 44.7 TUNEL-positive cells/field at 40 mg/kg.
Increased contrast index (CI) values significantly in both treated groups compared to the DMBA-only group, with the highest CI in the 40 mg/kg group.
Restored tissue architecture in treated tumor sections.
Chemical Information
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CAS No. 329719-71-3
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Appearance Solid
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Molecular Weight 333.83
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Formula C17H16ClNO2S
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Color White to off-white
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SMILES
O=C1N(C(C2=CC=C(C=C2)Cl)SC1)C3=CC=C(C=C3)OCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (299.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.49 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9955 mL | 14.9777 mL | 29.9554 mL | 74.8884 mL |
| 5 mM | 0.5991 mL | 2.9955 mL | 5.9911 mL | 14.9777 mL | |
| 10 mM | 0.2996 mL | 1.4978 mL | 2.9955 mL | 7.4888 mL | |
| 15 mM | 0.1997 mL | 0.9985 mL | 1.9970 mL | 4.9926 mL | |
| 20 mM | 0.1498 mL | 0.7489 mL | 1.4978 mL | 3.7444 mL | |
| 25 mM | 0.1198 mL | 0.5991 mL | 1.1982 mL | 2.9955 mL | |
| 30 mM | 0.0999 mL | 0.4993 mL | 0.9985 mL | 2.4963 mL | |
| 40 mM | 0.0749 mL | 0.3744 mL | 0.7489 mL | 1.8722 mL | |
| 50 mM | 0.0599 mL | 0.2996 mL | 0.5991 mL | 1.4978 mL | |
| 60 mM | 0.0499 mL | 0.2496 mL | 0.4993 mL | 1.2481 mL | |
| 80 mM | 0.0374 mL | 0.1872 mL | 0.3744 mL | 0.9361 mL | |
| 100 mM | 0.0300 mL | 0.1498 mL | 0.2996 mL | 0.7489 mL |
BCS12 Related Classifications
HY-186248 Related Classifications
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- BCS12
- 329719-71-3
- BCS 12
- BCS-12
- Carbonic Anhydrase
- HIF/HIF Prolyl-Hydroxylase
- Bcl-2 Family
- Caspase
- PARP
- Apoptosis
- Reactive Oxygen Species (ROS)
- HIF-1α
- MDA-MB-468
- MCF-10A
- DMBA-induced breast tumor-bearing rats
- MDA-MB-231
- PARP cleavage
- triple-negative breast cancer
- Carbonic Anhydrase IX
- mitochondrial apoptosis
- caspase cascade
- Inhibitor
- inhibitor
- inhibit