SRT3025 HCl

Catalog No.S8481 Batch:S848101

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Technical Data

Formula

C31H31N5O2S2.HCl
Molecular Weight 606.2 CAS No. 2070015-26-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (164.96 mM)
Ethanol 5 mg/mL (8.24 mM)
Water Insoluble
* <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.)

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Biological Activity

Description SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.
Targets
SIRT1 [1]
(Cell-free assay)
In vitro SRT3025 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival. SRT3025 inhibits RANKL-induced osteoclastogenesis in bone marrow-derived macrophages (BMMs) by activating AMPK and deacetylating RelA/p65 lysine 310, critical for activation of the NF-κB signaling pathway[2]. SRT3025 acts faster than oxymetholone to improve hematopoiesis. It does not work by direct activation of Sirt1 in hematopoietic cells. SRT3025 might suppress p21 transcription through the down-regulation of Egr1[3]. SRT3025 is found to activate wild-type Sirt1 protein but failed to activate the E230K mutant, an activation-resistant Sirt1 protein (due to a mutation at position 230)[4].
In vivo SRT3025 treatment also inhibits tumor growth in Panc-1 xenografts, even though it is not as effective in inhibiting the viability of Panc-1 cells in culture. SRT3025 is well tolerated in mice and has the potential to be used in several diseases[1]. SRT3025 administration expands HSPCs and boosts blood counts while long term SRT3025 administration does not permanently increase or decrease HSC repopulating potential[3]. SRT3025 reduces plasma cholesterol, inflammation, and atherosclerosis in Apoe−/− mice, and it increases hepatic Ldlr expression and Pcsk9 accumulation[4].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    HPDE, Panc-1, SU86.86, Patu8988t cells

  • Concentrations

    0-5 μM

  • Incubation Time

    72 h

  • Method

    Cells are treated with vehicle or different concentrations of SRT3025 for 72 hours and submitted to MTT analysis. 
Animal Study:

[1]
  • Animal Models

    Female athymic nu/nu mice

  • Dosages

    50-200 mg/kg

  • Administration

    oral administration

Selleck's SRT3025 HCl has been cited by 3 publications

Sirtuin activation targets IDH-mutant tumors [ Neuro Oncol, 2021, 23(1):53-62] PubMed: 32710757
Geriatric Fragility Fractures Are Associated With a Human Skeletal Stem Cell Defect [ Aging Cell, 2020, e13164] PubMed: 32537886
Sirt1 in the Regulation of Interferon Gamma in Severe Aplastic Anemia. [ Acta Haematol, 2019, 142(3):142-148] PubMed: 31141802

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.