BTSA1
Based on 2 publication(s) in Google Scholar
BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.77%
- CAS 番号: 314761-14-3
- 分子式: C21H14N6OS2
- 分子量:430.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 BTSA1
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生物活性
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Bax 250 nM (IC50) |
Bax 144 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>20 μM
Compound: 2; BTSA1
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Antiproliferative activity against siRNA-induced BAX knock down human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against siRNA-induced BAX knock down human HeLa cells after 48 hrs by MTT assay
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[PMID: 33021789] |
| HeLa | IC50 |
0.81 μM
Compound: 2; BTSA1
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Synergistic antiproliferative activity against human HeLa cells assessed as assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay
Synergistic antiproliferative activity against human HeLa cells assessed as assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay
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[PMID: 33021789] |
| HeLa | IC50 |
11.47 μM
Compound: 2; BTSA1
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Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 33021789] |
| L02 | IC50 |
54.2 μM
Compound: 2; BTSA1
|
Cytotoxicity against human L02 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 33021789] |
BTSA1 (5 μM; 6-24 hours; human AML cell lines) treatment reduced viability of all AML cell lines and displays substantial cell death activity within 6 hours[1].
BTSA1 (2.5-10 μM; 6 hours; NB4 cells) treatment induces BAX translocation coincided with the release of cytochrome c from the mitochondria to the cytosol. Significant BAX mitochondrial translocation is induced in a BTSA1 dose-dependent manner[1].
BTSA1 (0.15625-10 μM; 4-24 hours; OCI-AML3 cells) treatment induces dose-dependent caspase-3/7 activation in OCI-AML3 cells. Caspase-3/7 activation is monitored within 4-24 hours and maximal caspase-3/7 activation is detected in 4 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human AML cell lines<
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Concentration:5 μM
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Incubation Time:6 hours, 12 hours, 24 hours
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Result:Reduced viability of all AML cell lines. Displayed substantial cell death activity within 6 hours.
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Cell Line:NB4 cells
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:6 hours
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Result:Significant BAX mitochondrial translocation was induced in a dose-dependent manner.
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Cell Line:OCI-AML3 cells
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Concentration:0.15625 μM, 0.3125 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:4 hours, 6 hours, 8 hours, 12 hours, 24 hours
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Result:Induced dose-dependent caspase-3/7 activation in OCI-AML3 cells. Caspase-3/7 activation was monitored within 4-24 hr and maximal caspase-3/7 activation was detected in 4 hr.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID IL2Rγ null (NSG) mice (6-8 weeks old) with THP-1 cells[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; every two days
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Result:Significantly increased survival when compared to vehicle-treated mice.
化学情報
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CAS 番号 314761-14-3
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性状 Solid
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分子量 430.51
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分子式 C21H14N6OS2
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Color Brown to reddish brown
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SMILES
O=C(N(C1=NC(C2=CC=CC=C2)=CS1)N=C/3C4=CC=CC=C4)C3=N\NC5=NC=CS5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Characterization of mitochondrial dysfunction induced by BAX trigger site activator 1 in the ARPE-19 retinal pigment epithelial cell model. [Abstract]2026 Jun 15:1027:178975. PMID: 42134759 -
Int J Mol Sci
Mitochondrial Trafficking of MLKL, Bak/Bax, and Drp1 Is Mediated by RIP1 and ROS which Leads to Decreased Mitochondrial Membrane Integrity during the Hyperglycemic Shift to Necroptosis. [Abstract]2023 May 11;24(10):8609. PMID: 37239951
溶剤 & 溶解度
DMSO : 25 mg/mL (58.07 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3228 mL | 11.6141 mL | 23.2283 mL | 58.0707 mL |
| 5 mM | 0.4646 mL | 2.3228 mL | 4.6457 mL | 11.6141 mL | |
| 10 mM | 0.2323 mL | 1.1614 mL | 2.3228 mL | 5.8071 mL | |
| 15 mM | 0.1549 mL | 0.7743 mL | 1.5486 mL | 3.8714 mL | |
| 20 mM | 0.1161 mL | 0.5807 mL | 1.1614 mL | 2.9035 mL | |
| 25 mM | 0.0929 mL | 0.4646 mL | 0.9291 mL | 2.3228 mL | |
| 30 mM | 0.0774 mL | 0.3871 mL | 0.7743 mL | 1.9357 mL | |
| 40 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | 1.4518 mL | |
| 50 mM | 0.0465 mL | 0.2323 mL | 0.4646 mL | 1.1614 mL |