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Chemical Structure| 314761-14-3 Chemical Structure| 314761-14-3

Structure of BTSA1
CAS No.: 314761-14-3

Chemical Structure| 314761-14-3

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

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Product Details of BTSA1

CAS No. :314761-14-3
Formula : C21H14N6OS2
M.W : 430.51
SMILES Code : O=C(N(C1=NC(C2=CC=CC=C2)=CS1)N=C/3C4=CC=CC=C4)C3=N\NC5=NC=CS5
MDL No. :MFCD01078360
InChI Key :CTRCXGFSYFTJIW-UHFFFAOYSA-N
Pubchem ID :3857348

Safety of BTSA1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Bax

In Vitro:

Cell Line
Concentration Treated Time Description References
Solid tumor cell lines (e.g., pancreatic cancer BxPC-3 and colon cancer SW480) 10 μM 4 hours Evaluate the ability of BTSA1.2 to induce BAX activation and translocation PMC8901805
OCI-AML3 cells 5 μM 6, 12, and 24 hours To assess the effect of BTSA1 on OCI-AML3 cell viability at different time points, results showed that BTSA1 significantly reduced cell viability within 6 hours PMC5793879
Human AML cell lines 1–4 μM 24 hours To evaluate the ability of BTSA1 to induce apoptosis in AML cell lines, results showed that BTSA1 significantly reduced cell viability and induced apoptosis PMC5793879
Human umbilical vein endothelial cells (HUVECs) 0.625 μmol/L 2.5 hours BTSA1, a Bax agonist, promotes Bax translocation to mitochondria without affecting its expression. In HUVECs, pretreatment with BTSA1 successfully abolished the inhibitory effect of L-cystathionine on Hcy-induced MPTP opening, caspase-9 and caspase-3 activation, and HUVEC apoptosis. PMC6899331

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice SW480 colon cancer xenograft model Oral gavage 200 mg/kg Once daily for 7 days Evaluate the efficacy of BTSA1.2 and Navitoclax combination therapy in colon cancer xenograft models PMC8901805
NOD-SCID IL2Rγ null (NSG) mice Human AML xenograft model Intraperitoneal injection 10 mg/kg Every 48 hours for 3 weeks To evaluate the anti-tumor activity and safety of BTSA1 in AML xenograft models, results showed that BTSA1 significantly suppressed leukemia growth and increased host survival without detectable toxicity PMC5793879
C57BL/6 mice Bleomycin-induced pulmonary fibrosis model Intraperitoneal injection 10 mg/kg Once every 2 days Evaluate the therapeutic effect of BTSA1 on pulmonary fibrosis, results showed BTSA1 significantly reduced the number of senescent myofibroblasts in lung tissue and alleviated both reversible and irreversible pulmonary fibrosis PMC11488301

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.61mL

2.32mL

1.16mL

23.23mL

4.65mL

2.32mL

References

 

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