Benfluron hydrochloride
Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC50 of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.
For research use only. We do not sell to patients.
- CAS No.: 80427-58-3
- Formula: C21H20ClNO2
- Molecular Weight:353.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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ERK1 |
ERK2 |
Chk1 |
Chk2 |
Caspase-8 |
Caspase-9 |
Caspase 3 |
Caspase-7 |
HIV-1 |
Benfluron (0.2-1 μM; 24-72 h) hydrochloride reduces the proliferation capacity and viability of MOLT-4 cells in a concentration-dependent manner: cells are completely eliminated at concentrations of 0.8 μM and 1 μM after 48 h and 72 h; the cell viability is 49% at 0.6 μM after 48 h, and 33% at 0.6 μM after 72 h[1].
Benfluron (0.4-0.6 μM; 48 h) hydrochloride induces dose-dependent apoptosis in MOLT-4 cells, with the proportion of apoptotic cells reaching 26% at 0.4 μM and 81% at 0.6 μM after 48 h[1].
Benfluron (0.4-0.6 μM; 48 h) hydrochloride induces dose-dependent morphological changes associated with apoptosis in MOLT-4 cells. After 48 h, 25% of cells exhibit apoptotic light-scattering characteristics at the concentration of 0.4 μM, while this proportion reaches 73% at 0.6 μM[1].
Benfluron (0.4-0.6 μM; 24-48 h) hydrochloride induces dose-dependent activation of caspase 3/7, 8 and 9 in MOLT-4 cells, with significantly elevated activities observed at concentrations of 0.4, 0.5 and 0.6 μM after 24 h and 48 h[1].
Benfluron hydrochloride binds to HIV-1 RRE subdomain IIB with a Kd value of 4.83 µM[2].
Benfluron hydrochloride inhibits the formation of the full-length HIV-1 RRE-Rev complex, with an IC50 of 5.0 µM[2].
Benfluron hydrochloride potently inhibits HIV-1 replication in MT-2 cells, with an EC50 of 0.830 µM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human leukemic T lymphocyte MOLT-4 cells
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Concentration:0.2-1 μM
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Incubation Time:24, 48, 72 h
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Result:Shows effect comparable to untreated control cells at 0.2 μM, increases percentage of dead cells to 16% after 72 h (vs. 5% in control) at 0.4 μM while total cell number still increases after 48 and 72 h, increases percentage of dead cells to 51% after 48 h and 67% after 72 h reducing viability to 49% and 33% respectively with almost complete inhibition of cell proliferation at 0.6 μM, and results in complete elimination of cells after 48 and 72 h at 0.8 μM and 1 μM.
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Cell Line:human leukemic T lymphocyte MOLT-4 cells
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Concentration:0.4-0.6 μM
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Incubation Time:48 h
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Result:Increases apoptotic cells to 26% (7% early apoptosis, 19% late apoptosis/death) at 0.4 μM (vs. 7% in control) and to 81% (14% early apoptosis, 67% late apoptosis/death) at 0.6 μM, an effect similar to the positive control mitoxantrone.\nIncreases population of cells with apoptotic light scatter properties to 25% at 0.4 μM (vs. 10% in control) and to 73% at 0.6 μM, consistent with Annexin V/PI staining results.
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Cell Line:human leukemic T lymphocyte MOLT-4 cells
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Concentration:0.4-0.6 μM
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Incubation Time:16 h
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Result:Results in 58% in G1 phase, 32% in S phase, and 10% in G2/M phase at 0.4 μM (vs. 62% G1, 31% S, 7% G2/M in control), and in 53% in G1 phase, 34% in S phase, and 13% in G2/M phase at 0.6 μM, showing dose-dependent accumulation in late S and G2/M phases.
Chemical Information
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CAS No. 80427-58-3
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Molecular Weight 353.84
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Formula C21H20ClNO2
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SMILES
O=C1C2=C(C3=C1C=C(OCCN(C)C)C4=C3C=CC=C4)C=CC=C2.Cl
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Synonyms
Benflurone hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Seifrtová M, et al. Benfluron Induces Cell Cycle Arrest, Apoptosis and Activation of p53 Pathway in MOLT-4 Leukemic Cells. Folia biologica. 2015;61(4):147-55. [Content Brief]
[2]. Chumillas S, et al. Exploring the HIV-1 Rev Recognition Element (RRE)-Rev Inhibitory Capacity and Antiretroviral Action of Benfluron Analogs. Molecules (Basel, Switzerland). 2023 Oct 11;28(20):7031. [Content Brief]
[3]. Skálová L, et al. Carbonyl reduction of the potential cytostatic drugs benfluron and 3,9-dimethoxybenfluron in human in vitro. Biochemical pharmacology. 2002 Jul 15;64(2):297-305. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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