BTSA1

SKU: orb1302087

Description

BTSA1 is a high-affinity, specific small molecule activator of BAX that binds its N-terminal site, inducing pro-apoptotic conformational changes. It is a valuable research tool for studying BAX-dependent apoptosis mechanisms in both cellular (in vitro) and animal (in vivo) models of cancer and related diseases.

Research Area

Cell Biology

Key Properties

• CAS Number: 314761-14-3
• MW: 430.51
• Purity: 99.71% (May vary between batches)
• Formula: C₂₁H₁₄N₆OS₂
• SMILES: O=C1N(N=C(\C1=N/Nc1nccs1)c1ccccc1)c1nc(cs1)-c1ccccc1
• Target: Bcl-2 Family,Apoptosis
• Solubility: DMSO:60 mg/mL (139.37 mM)

Bioactivity

• Target IC50:
  Bax:144 nM (EC50)|Bax:250 nM (IC50)
• In Vivo:
  BTSA1 potently suppresses human acute myeloid leukemia (AML) xenografts and increases host survival without toxicity. It is well-tolerated in mice with no toxic effects on healthy hematopoiesis, including healthy stem cell-enriched (LSK) cells, common myeloid progenitors, granulocyte-monocyte progenitors, and megakaryocyte-erythrocyte progenitors. BTSA1 has a substantial half-life in mouse plasma (T1/2 = 15 hr) and oral bioavailability (%F = 51), while a 10 mg/kg dose reaches sufficient levels (~15 μM) of BTSA1 to induce BAX activation and apoptosis in leukemia cells. Thus, BTSA1 is orally bioavailable with excellent pharmacokinetics, has significant anti-tumor activity in leukemia xenografts by promoting apoptosis, and at therapeutically effective doses it does not show any detectable toxicity in the hematopoietic system or other tissues.
• In Vitro:
  BTSA1 has no capacity to directly activate the pro-apoptotic homolog BAK. BTSA1 treatment potently and dose-responsively induces membrane translocation of recombinant soluble BAX to the mitochondrial membrane, which is followed by induction of BAX oligomerization. BTSA1-induced BAX activation promotes apoptosis in cancer cells. BTSA1 reduces the viability of all AML cell lines in a dose-dependent manner with IC50 values ranged between 1 and 4 μM, which leads to complete effect within 24 hr treatment. It induces dose-dependent caspase-3/7 activation in all five AML cell lines.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AML, Apoptosis, Bax, BAX, Bcl-2 Family, caspase-3/7, BTSA 1, BTSA1, BTSA-1, inhibit, mitochondrial, Inhibitor, FITC-BIM, translocation, SAHBA2, pharmacologically, viability

Compound Identifiers

PubChem CID

3857348