2. Apoptosis
  3. Bcl-2 Family Apoptosis
  4. BTSA1

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.

For research use only. We do not sell to patients.

BTSA1 Chemical Structure

BTSA1 Chemical Structure

CAS No. : 314761-14-3

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Based on 1 publication(s) in Google Scholar

BTSA1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BTSA1

View All Bcl-2 Family Isoform Specific Products:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • Biological Activity

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Description

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)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BTSA1 Related Antibodies

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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

430.51

Formula

C21H14N6OS2
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(N(C1=NC(C2=CC=CC=C2)=CS1)N=C/3C4=CC=CC=C4)C3=N\NC5=NC=CS5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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, 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
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BTSA1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BTSA1314761-14-3BTSA 1BTSA-1Bcl-2 FamilyApoptosisBAXpharmacologicallyapoptosisFITC-BIMSAHBA2viabilityAMLmitochondrialtranslocationcaspase-3/7Inhibitorinhibitorinhibit

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