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BTSA1

Catalog No. T5104   CAS 314761-14-3

BTSA1 is a BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.

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BTSA1 Chemical Structure
BTSA1, CAS 314761-14-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 38.00
5 mg In stock $ 64.00
10 mg In stock $ 122.00
25 mg In stock $ 198.00
50 mg In stock $ 372.00
100 mg In stock $ 556.00
500 mg In stock $ 1,220.00
1 mL * 10 mM (in DMSO) In stock $ 70.00
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Purity: 99.15%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BTSA1 is a BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
Targets&IC50 Bax:250 nM (IC50), Bax:144 nM (EC50)
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[1].
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[1].
Molecular Weight 430.51
Formula C21H14N6OS2
CAS No. 314761-14-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/mL (139.37 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compounds Library Max Anti-Aging Compound Library Cuproptosis Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library Apoptosis Compound Library PPI Inhibitor Library Mitochondria-Targeted Compound Library Orally Active Compound Library Bioactive Compound Library

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Keywords

BTSA1 314761-14-3 Apoptosis BCL inhibit FITC-BIM caspase-3/7 translocation BTSA 1 Bcl-2 Family BTSA-1 viability Inhibitor mitochondrial pharmacologically BAX AML SAHBA2 inhibitor

 

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