BTSA1

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BTSA1  纯度: 99.74%

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。

BTSA1

BTSA1 Chemical Structure

CAS No. : 314761-14-3

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BTSA1 相关产品

•相关化合物库:

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  • Apoptosis Compound Library
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  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library
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生物活性

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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

430.51

Formula

C21H14N6OS2
CAS 号

314761-14-3
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Reyna DE, et al. Direct Activation of BAX by BTSA1 Overcomes Apoptosis Resistance in Acute Myeloid Leukemia. Cancer Cell. 2017 Oct 9;32(4):490-505.e10.

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