SML4031
BAX Dimer Modulator 19, BDM19
≥98% (HPLC)
别名:
BDM-19, (E)-4-(6-Iodo-2-(3-methylstyryl)-4-oxoquinazolin-3(4H)-yl)benzoic acid, 4-[6-Iodo-2-[2-(3-methylphenyl)ethenyl]-4-oxo-3(4H)-quinazolinyl]benzoic acid, BDM 19, BDM19
InChI key
CQEADRMBOXGOAE-LFYBBSHMSA-N
SMILES string
IC1=CC=C2C(C(N(C(/C=C/C3=CC(C)=CC=C3)=N2)C4=CC=C(C=C4)C(O)=O)=O)=C1
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Potent and selective cytosolic BAX dimer modulator that effectively induces apoptosis in cancer cells by selectively modulating inactive BAX.
BDM19, a potent BAX dimer modulator with a Kd of 560 nM, selectively binds to the N-terminal trigger site of inactive BAX, thereby inhibiting its dimerization with an IC50 of 5 μM. By stabilizing the inactive conformation of BAX, BDM-19 allosterically activates it, targeting cells containing cytosolic inactive BAX monomers and dimers. This leads to a dose-dependent translocation of BAX to mitochondria, subsequent cytochrome c release, and induction of apoptosis.
BDM19, a potent BAX dimer modulator with a Kd of 560 nM, selectively binds to the N-terminal trigger site of inactive BAX, thereby inhibiting its dimerization with an IC50 of 5 μM. By stabilizing the inactive conformation of BAX, BDM-19 allosterically activates it, targeting cells containing cytosolic inactive BAX monomers and dimers. This leads to a dose-dependent translocation of BAX to mitochondria, subsequent cytochrome c release, and induction of apoptosis.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Nadege Gitego et al.
Nature communications, 14(1), 8381-8381 (2023-12-17)
The BCL-2 family protein BAX is a major regulator of physiological and pathological cell death. BAX predominantly resides in the cytosol in a quiescent state and upon stress, it undergoes conformational activation and mitochondrial translocation leading to mitochondrial outer membrane
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