| Identification | Back Directory | [Name]
BTSA 1 | [CAS]
314761-14-3 | [Synonyms]
BTSA 1
CS-2853
BTSA 1;BTSA-1
BTSA1 >=98% (HPLC)
5-Phenyl-2-(4-phenyl-thiazol-2-yl)-4-(thiazol-2-yl-hydrazono)-2,4-dihydro-pyrazol-3-one
1H-Pyrazole-4,5-dione, 3-phenyl-1-(4-phenyl-2-thiazolyl)-, 4-[2-(2-thiazolyl)hydrazone] | [Molecular Formula]
C21H14N6OS2 | [MOL File]
314761-14-3.mol | [Molecular Weight]
430.51 |
| Chemical Properties | Back Directory | [Boiling point ]
625.2±48.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:53.0(Max Conc. mg/mL);123.11(Max Conc. mM) | [form ]
Solid | [pka]
6.52±0.40(Predicted) | [color ]
Brown to reddish brown | [InChI]
InChI=1S/C21H14N6OS2/c28-19-18(24-25-20-22-11-12-29-20)17(15-9-5-2-6-10-15)26-27(19)21-23-16(13-30-21)14-7-3-1-4-8-14/h1-13H,(H,22,25) | [InChIKey]
KYVZVVOQWWCVPP-UHFFFAOYSA-N | [SMILES]
N1(C2=NC(C3=CC=CC=C3)=CS2)C(=O)C(=NNC2=NC=CS2)C(C2=CC=CC=C2)=N1 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
BTSA1 is a BAX activator that binds to its N-terminal activation site with high affinity and specificity, induces a conformational change in BAX, and causes BAC-mediated apoptosis. It efficiently promotes apoptosis in leukemia cell lines and patient samples without affecting healthy cells. | [in vivo]
BTSA1 effectively inhibits human acute myeloid leukemia xenografts and enhances host survival without toxic side effects. In mice, it was well tolerated. | [target]
| Target | Value | Bax
() | [IC 50]
Bax: 250 nM (IC50); Bax: 144 nM (EC50) | [References]
[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. DOI:10.1016/j.ccell.2017.09.001 |
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| Company Name: |
Hui Chem Co., Ltd.
|
| Tel: |
021-34799779 13060007561 |
| Website: |
http://www.huichem.com |
| Company Name: |
BOC Sciences
|
| Tel: |
13060007561 |
| Website: |
www.bocsci.com |
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Tags:314761-14-3
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