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

BTSA1 

Cat. No.: HY-123054
Handling Instructions

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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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].

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].

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.

314761-14-3

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BTSA1BTSA 1BTSA-1Bcl-2 FamilyApoptosisBAXpharmacologicallyapoptosisFITC-BIMSAHBA2viabilityAMLmitochondrialtranslocationcaspase-3/7Inhibitorinhibitorinhibit

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