BTSA1 是一种有效的，高亲和力和口服活性的BAX激活剂，IC50为 250 nM，EC50为 144 nM。BTSA1 以高亲和力和特异性与 N 末端激活位点结合，并诱导BAX发生构象变化，从而导致BAX介导的细胞凋亡。
| 生物活性 | BTSA1 is a potent, high affinity and orally activeBAXactivator with anIC50of 250 nM and anEC50of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes toBAXleading toBAX-mediatedapoptosis[1]. |
| IC50& Target[1] | Bax 250 nM (IC50) | Bax 144 nM (EC50) |
|
体外研究
(In Vitro) | 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].
Cell Viability Assaysup>[1] | Cell Line: | Human AML cell lines< | | Concentration: | 5 μM | | Incubation Time: | 6 hours, 12 hours, 24 hours | | Result: | Reduced viability of all AML cell lines. Displayed substantial cell death activity within 6 hours. |
Western Blot Analysis[1] | Cell Line: | NB4 cells | | Concentration: | 2.5 μM, 5 μM, 10 μM | | Incubation Time: | 6 hours | | Result: | Significant BAX mitochondrial translocation was induced in a dose-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | OCI-AML3 cells | | Concentration: | 0.15625 μM, 0.3125 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM | | Incubation Time: | 4 hours, 6 hours, 8 hours, 12 hours, 24 hours | | 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. |
|
体内研究
(In Vivo) | BTSA1 (10 mg/kg; intraperitoneal injection; every two days; NOD-SCID IL2Rγ null (NSG) mice) treatment significantly increases survival when compared to vehicle-treated mice. BTSA1 treatment induces significant suppression of leukemia growth[1].
| Animal Model: | NOD-SCID IL2Rγ null (NSG) mice (6-8 weeks old) with THP-1 cells[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; every two days | | Result: | Significantly increased survival when compared to vehicle-treated mice. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(58.07 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3228 mL | 11.6141 mL | 23.2283 mL | | 5 mM | 0.4646 mL | 2.3228 mL | 4.6457 mL | | 10 mM | 0.2323 mL | 1.1614 mL | 2.3228 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
m.cnreagent.com