Acevaltrate

Catalog No.E0244 Batch:E024401

Technical Data

Formula	C₂₄H₃₂O₁₀
Molecular Weight	480.51	CAS No.	25161-41-5
Solubility (25°C)*	In vitro	DMSO	96 mg/mL (199.78 mM)


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Acevaltrate, an active component derived from the herbal plant Valeriana jatamansi Jones, is strikingly potent to induce GBM cell apoptosis. Acevaltrate inhibits the Na+/K+-ATPase activity in the rat kidney and brain hemispheres with IC50 of 22.8 μM and 42.3 μM, respectively.

Targets

Na+/K+-ATPase ^[1] (in the rat kidney)	Na+/K+-ATPase ^[1] (in the rat brain hemispheres)
22.8 μM	42.3 μM

In vitro

Acevaltrate disrupts the interaction of Otub1/c-Maf thus inhibiting Otub1 activity and leading to c-Maf polyubiquitination and subsequent degradation in proteasomes. Consistently, acevaltrate inhibits c-Maf transcriptional activity and downregulates the expression of its target genes key for myeloma growth and survival.^[1]

In vivo

Acevaltrate displays potent anti-myeloma activity by triggering myeloma cell apoptosis in vitro and impairing myeloma xenograft growth in vivo but presents no marked toxicity.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MM cell lines (RPMI-8226, LP1, KMS11, OPM2, U266) Concentrations 1, 2, 4 µM Incubation Time 24 h Method RPMI-8226 cells are transfected with plasmids as indicated for 48 h. Cells are then re-plated and treated with 0.1% DMSO or acevaltrate for 24 h before being harvested for luciferase activity measurements. MM cells are treated with acevaltrate for 24 h, followed by WB or RT-PCR assays to evaluate the expression of specifc genes.
Animal Study:^{^[1]}	Animal Models Nude mice of myeloma xenograft model Dosages 50 mg/kg Administration p.o.

Cell Assay:^{^[1]}

Cell lines
MM cell lines (RPMI-8226, LP1, KMS11, OPM2, U266)
Concentrations
1, 2, 4 µM
Incubation Time
24 h
Method
RPMI-8226 cells are transfected with plasmids as indicated for 48 h. Cells are then re-plated and treated with 0.1% DMSO or acevaltrate for 24 h before being harvested for luciferase activity measurements. MM cells are treated with acevaltrate for 24 h, followed by WB or RT-PCR assays to evaluate the expression of specifc genes.

Animal Study:^{^[1]}

Animal Models
Nude mice of myeloma xenograft model
Dosages
50 mg/kg
Administration
p.o.

References

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SHIPPING AND STORAGE
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